Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
Crosstalk ID
M6ACROT00063
[1]
m6A modification ADAR1 ADAR1 METTL3 Methylation : m6A sites Direct Enhancement RNA modification CDK2 CDK2 ADAR1 Methylation : modification sites
m6A Modification:
m6A Regulator Methyltransferase-like 3 (METTL3) WRITER
m6A Target Interferon-inducible protein 4 (ADAR1)
Epigenetic Regulation that have Cross-talk with This m6A Modification:
Epigenetic Regulation Type RNA modification (RNAMod)  >> Adenosine-to-Inosine editing (A-to-I)
Epigenetic Regulator Interferon-inducible protein 4 (ADAR1) WRITER View Details
Regulated Target Cyclin-dependent kinase 2 (CDK2) View Details
Crosstalk Relationship m6A  →  A-to-I Enhancement
Crosstalk Mechanism m6A modification directly impacts RNA modification through modulating the expression level of RNA modification regulator
Crosstalk Summary METTL3, upregulated in glioblastoma, methylates Interferon-inducible protein 4 (ADAR1) mRNA and increases its protein level leading to a pro-tumorigenic mechanism connecting METTL3, YTHDF1, and ADAR1. We show that ADAR1 plays a cancer-promoting role independently of its deaminase activity by binding Cyclin-dependent kinase 2 (CDK2) mRNA, underlining the importance of ADARs as essential RNA-binding proteins for cell homeostasis as well as cancer progression.
Responsed Disease Brain cancer ICD-11: 2A00
Responsed Drug PHA848125
Pathway Response mRNA surveillance pathway hsa03015
RNA degradation hsa03018
Cell Process Cell proliferation
In-vivo Model 2 × 106 U87MG cells already expressing shscr or shADAR1 were subcutaneously injected in the flank of 6-week-old nude mice. For orthotopic mouse models, 2 × 105 shscr and shADAR1 U87MG glioblastoma cells were intracranially injected into male NOD/SCID mice.
Full List of Potential Compound(s) Related to This m6A-centered Crosstalk
Cyclin-dependent kinase 2 (CDK2) 138 Compound(s) Regulating the Target Click to Show/Hide the Full List
 Compound Name PHA848125 Phase 2 [2]
Synonyms
Milciclib; PHA-848125; 802539-81-7; PHA 848125; Milciclib (PHA-848125); UNII-688000M8S8; MMV676602; 4,5-dihydro-N,1,4,4-tetramethyl-8-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-1H-Pyrazolo[4,3-h]quinazoline-3-carboxamide; 688000M8S8; N,1,4,4-tetramethyl-8-(4-(4-methylpiperazin-1-yl)phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide; Milciclib [INN]; N,1,4,4-Tetramethyl-8-{[4-(4-Methylpiperazin-1-Yl)phenyl]amino}-4,5-Dihydro-1h-Pyrazolo[4,3-H]quinazoline-3-Carboxamide
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 45 nM
External Link
 Compound Name Ro 31-7453 Phase 2 [3]
Synonyms
Bisindolylmaleimide deriv. 44; MKC-1; Ro-31-7453; 3-(1-methylindol-3-yl)-4-(1-methyl-6-nitroindol-3-yl)pyrrole-2,5-dione
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name R-roscovitine Phase 2 [4]
Synonyms
Seliciclib; roscovitine; 186692-46-6; (R)-roscovitine; CYC202; CYC-202; CYC 202; 2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-benzylamino-9-isopropylpurine; UNII-0ES1C2KQ94; Roscovitine (Seliciclib,CYC202); NSC 701554; AL-39256; CHEMBL14762; 0ES1C2KQ94; CHEBI:45307; NSC701554; NSC-701554; (2R)-2-[[6-(benzylamino)-9-isopropyl-purin-2-yl]amino]butan-1-ol; (R)-2-((6-(Benzylamino)-9-isopropyl-9H-purin-2-yl)amino)butan-1-ol; (2R)-2-[[6-(benzylamino)-9-propan-2-ylpurin-2-yl]amino]butan-1-ol; RRC; Rosco; M02443; BMK1-E12; CYC202, Seliciclib, R-roscovitine, Roscovitine; (2r)-2-{[6-(benzylamino)-9-isopropyl-9h-purin-2-yl]amino}-1-butanol; 2-(R)-[[9-(1-Methylethyl)-6-[(phenylmethyl)amino]-9H-purin-2-yl]amino]-1-butanol; 2-[[9-(1-Methylethyl)-6-[(phenylmethyl)amino]-9H-purin-2-yl]amino]-(R)-1-butanol; 6-(Benzylamino)-2(R)-[[1-(hydroxymethyl)propyl]amino]-9-isopropylpurine
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 100 nM
External Link
 Compound Name TG02 Phase 1/2 [5]
Synonyms
SB1317; 937270-47-8; TG-02; TG02 (Double bond Z/E); UNII-40D08182TT; CHEMBL1944698; 40D08182TT; SB-1317; 1204918-72-8; C23H24N4O; Tube011; SB-1317 free base; TG02 (Double bond E); TG02 [WHO-DD]; SCHEMBL823947; SCHEMBL2298965; GTPL9095; SCHEMBL17595943; EX-A239; MolPort-039-139-793; AOB87361; BCP07033; ZINC68251500; BDBM50363196; 4029AH; AKOS030527020; AKOS032950000; SB1317(TG-02); SB14606; CS-0884; compound 26h [PMID: 22148278]; KB-80503; HY-15166; W-5884
    Click to Show/Hide
MOA Modulator
Activity IC50 = 3 nM
External Link
 Compound Name NUV-422 Phase 1/2 [6]
MOA Inhibitor
External Link
 Compound Name AZD-5438 Phase 1 [7]
Synonyms
602306-29-6; AZD5438; AZD 5438; 4-(1-isopropyl-2-methyl-1H-imidazol-5-yl)-N-(4-(methylsulfonyl)phenyl)pyrimidin-2-amine; CHEMBL488436; UNII-276Z913G29; MMV676604; 4-[2-METHYL-1-ISOPROPYL-1H-IMIDAZOL-5-YL]-N-[4-(METHYLSULFONYL)PHENYL]-2-PYRIMIDINAMINE; 2-Pyrimidinamine,4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-N-[4-(methylsulfonyl)phenyl]-; 276Z913G29; 4-(2-methyl-3-propan-2-ylimidazol-4-yl)-N-(4-methylsulfonylphenyl)pyrimidin-2-amine
    Click to Show/Hide
MOA Modulator
Activity IC50 < 6 nM
External Link
 Compound Name AT7519 Phase 1 [8]
Synonyms
LZE; AT 7519, AT7519; AT-7519; 4-[(2,6-dichlorobenzoyl)amino]-N-(4-piperidyl)-2H-pyrazole-3-carboxamide
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 47 nM
External Link
 Compound Name PF-07104091 Phase 1 [9]
MOA Inhibitor
External Link
 Compound Name CYC065 Phase 1 [10]
Synonyms
DLPIYBKBHMZCJI-WBVHZDCISA-N; 1070790-89-4; CYC-065; UNII-YET2XNU791; YET2XNU791; SCHEMBL13300946; CHEMBL3655762; BDBM106950; CS-7615; HY-101212; US8592581, 1; 2-Pentanol, 3-((6-(((4,6-dimethyl-3-pyridinyl)methyl)amino)-9-(1-methylethyl)-9H-purin-2-yl)amino)-, (2R,3S)-
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name AG-024322 Phase 1 [4]
Synonyms
AG-24322; N-[[5-[(3E)-3-(4,6-difluorobenzimidazol-2-ylidene)-1,2-dihydroindazol-5-yl]-4-methylpyridin-3-yl]methyl]ethanamine
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name PHA-793887 Phase 1 [11]
Synonyms
Cyclin-dependent kinase inhibitor (cancer), Nerviano
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name SNS-032 Phase 1 [12]
Synonyms
BMS-387032; BMS-387072; BMS-387032, SNS-032; N-[5-[[[5-(1,1-Dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4-piperidinecarboxamide L-tartaric acid salt (2:1); N-(5-(((5-(1,1-Dimethylethyl)-2-oxazolyl)methyl)thio)-2-thiazolyl)-4-piperidinecarboxamide; N-[5-[(5-tert-butyl-1,3-oxazol-2-yl)methylsulfanyl]-1,3-thiazol-2-yl]piperidine-4-carboxamide
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 38 nM
External Link
 Compound Name RGT-419B Phase 1 [13]
MOA Inhibitor
External Link
 Compound Name FN-1501 Phase 1 [14]
Synonyms
1429515-59-2; CHEMBL4077071; UNII-6MC966B505; TQR1001; BDBM50270304; NSC781143; 6MC966B505; NSC-781143; HY-111361; CS-0039834; 4((7HPyrrolo[2,3d]pyrimidin-4-yl)amino)N(4-((4-methylpiperazin-1-yl)methyl)phenyl)1Hpyrazole-3-carboxamide; 4-((7H-Pyrrolo (2,3-d)pyrimidin-4-yl)amino)-N-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrazole-3-carboxamide; 4-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-N-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrazole-5-carboxamide; 4a?(7Ha'Pyrrolo[2,3a'd]pyrimidin-4-yl)amino)a'Na?4-((4-methylpiperazin-1-yl)methyl)phenyl)a?Ha'pyrazole-3-carboxamide; N-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]-4-(7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-1H-pyrazole-5-carboxamide
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name RGB-286638 Phase 1 [15]
Synonyms
GPC-286199; RGB-286199; RGB-344064; Non-selective CDK inhibitors, Agennix; Non-selective CDK inhibitors, GPC Biotech; Non-selective cyclin dependent kinase inhibitors, Agennix; Non-selective cyclin dependent kinase inhibitors, GPC Biotech
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Fluorinated compound 1 Patented [16]
Synonyms
PMID26161698-Compound-15
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1.7 nM
External Link
 Compound Name 4-amino-3,5-di-substituted-thiazole derivative 1 Patented [16]
Synonyms
PMID26161698-Compound-54
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Indole-based analog 11 Patented [16]
Synonyms
PMID26161698-Compound-16
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 10 nM
External Link
 Compound Name N-(pyridin-2-yl)pyridine methylsulfone derivative 1 Patented [16]
Synonyms
PMID26161698-Compound-27
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 170 nM
External Link
 Compound Name Palbociclib/ribociclib analog 1 Patented [16]
Synonyms
PMID26161698-Compound-4
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Alkyl sulfone derivative 1 Patented [16]
Synonyms
PMID26161698-Compound-29
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Aniline derivative 1 Patented [16]
Synonyms
PMID26161698-Compound-33
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 39 nM
External Link
 Compound Name 4-(thiazol-5-yl)-pyrimidine derivative 1 Patented [16]
Synonyms
PMID26161698-Compound-35
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 45 nM
External Link
 Compound Name N-phenyl-pyrimidin-4-amine derivative 1 Patented [16]
Synonyms
PMID26161698-Compound-30
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1300 nM
External Link
 Compound Name PMID26161698-Compound-25 Patented [16]
MOA Inhibitor
Activity IC50 = 260 nM
External Link
 Compound Name Diaryl amine derivative 1 Patented [16]
Synonyms
PMID26161698-Compound-23
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 2 to 6 nM
External Link
 Compound Name Flavopiridol analog 1 Patented [16]
Synonyms
PMID26161698-Compound-5
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = nM range
External Link
 Compound Name Isosteric imidazolyl pyrimidine derivative 1 Patented [16]
Synonyms
PMID26161698-Compound-37
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 2 nM
External Link
 Compound Name N-(pyridin-2-yl)pyrimidin-4-amine derivative 2 Patented [16]
Synonyms
PMID26161698-Compound-31
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 63 nM
External Link
 Compound Name Pyrazolo-triazine derivative 2 Patented [16]
Synonyms
PMID26161698-Compound-14
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 1,5-di-substituted pyridine derivative 1 Patented [16]
Synonyms
PMID26161698-Compound-26
    Click to Show/Hide
MOA Inhibitor
Activity Kd < 100 nM
External Link
 Compound Name 5-fluoro-N-(pyridin-2-yl)pyridin-2-amine derivative 1 Patented [16]
Synonyms
PMID26161698-Compound-28
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 4 nM
External Link
 Compound Name Pyrrolo[2,3-d]pyrimidine derivative 9 Patented [16]
Synonyms
PMID26161698-Compound-1
    Click to Show/Hide
MOA Inhibitor
Activity IC50 < 1 nM
External Link
 Compound Name Naphthyridine and isoquinoline derivative 1 Patented [16]
Synonyms
PMID26161698-Compound-51
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 40 nM
External Link
 Compound Name Nitrogen mustard derivative 1 Patented [16]
Synonyms
PMID26161698-Compound-55
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 2.7 nM
External Link
 Compound Name 4-(thiazol-5-yl)-pyrimidine derivative 2 Patented [16]
Synonyms
PMID26161698-Compound-36
    Click to Show/Hide
MOA Inhibitor
Activity Ki = single digit nM
External Link
 Compound Name Diamidothiazole derivative 1 Patented [16]
Synonyms
PMID26161698-Compound-53
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Indole-based analog 13 Patented [16]
Synonyms
PMID26161698-Compound-20
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Pyrazolo[1,5-a]-1,3,5-triazine derivative 1 Patented [16]
Synonyms
PMID26161698-Compound-12
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 12 nM
External Link
 Compound Name Isoquinoline 1,3-dione derivative 1 Patented [16]
Synonyms
PMID26161698-Compound-49
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 3100 nM
External Link
 Compound Name Roscovitine derivative 1 Patented [16]
Synonyms
PMID26161698-Compound-8
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = nM range
External Link
 Compound Name PMID25991433-Compound-A1 Patented [17]
MOA Inhibitor
Activity IC50 = 300 nM
External Link
 Compound Name Oxazolyl methylthiothiazole derivative 1 Patented [16]
Synonyms
PMID26161698-Compound-52
    Click to Show/Hide
MOA Inhibitor
Activity IC50 < 100 nM
External Link
 Compound Name SCH 727965 Discontinued in Phase 3 [4]
Synonyms
Dinaciclib; SCH-727965
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1 nM
External Link
 Compound Name BAY 10-00394 Discontinued in Phase 2 [18]
Synonyms
roniciclib; BAY 1000394; KB-145902; 1223498-69-8; Tube010; SCHEMBL875845; GTPL7874
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name R547 Discontinued in Phase 1 [4]
Synonyms
LIA; R-547; [4-amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl]-(2,3-difluoro-6-methoxyphenyl)methanone
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 3 nM
External Link
 Compound Name ZK 304709 Discontinued in Phase 1 [4]
Synonyms
1010440-84-2; ZK CDK; UNII-87GI98VT0I; SCHEMBL955299; 87GI98VT0I; DTXSID20143701
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name INOC-005 Preclinical [19]
Synonyms
Capridine beta (prostate cancer), Prostagenics
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name L-751250 Preclinical [20]
Synonyms
Purvalanol B; 212844-54-7; PURVALANOL; Purvalanol B(NG-95); (R)-2-chloro-4-((2-((1-hydroxy-3-methylbutan-2-yl)amino)-9-isopropyl-9H-purin-6-yl)amino)benzoic acid; (2R)-2-[[6-[(3-CHLORO-4-CARBOXYPHENYL)AMINO]-9-(1-METHYLETHYL)-9H-PURIN-2-YL]AMINO]-3-METHYL-1-BUTANOL; CHEMBL23254; CHEBI:49840; NG 95; NG-95; C20H25ClN6O3; 2-chloro-4-[[2-[[(2R)-1-hydroxy-3-methylbutan-2-yl]amino]-9-propan-2-ylpurin-6-yl]amino]benzoic acid; J-502183; PVB
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 9 nM
External Link
 Compound Name Olomoucine Terminated [20]
Synonyms
101622-51-9; 4erk; UNII-6A839B2HYS; 2-(2-Hydroxyethylamino)-6-benzylamino-9-methylpurine; 6A839B2HYS; CHEMBL280074; 2-{[6-(benzylamino)-9-methyl-9h-purin-2-yl]amino}ethanol; 6-Benzylamino-2-(2-hydroxyethylamino)-9-methylpurine; 6-(Benzylamino)-2-(2-hydroxyethylamino)-9-methylpurine; Ethanol,2-[[9-methyl-6-[(phenylmethyl)amino]-9H-purin-2-yl]amino]-; OLO; 2-(Hydroxyethylamino)-6-benzylamino-9-methylpurine; 6-Benylamino-2-(2-hydroxyethylamino)-9-methylpurine
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1200 nM
External Link
 Compound Name PD-0183812 Terminated [21]
Synonyms
PETCVZZPKYJZAU-UHFFFAOYSA-N; PD183812; AC1NS8PJ; CHEMBL139653; SCHEMBL5268115; BDBM6280; PD 0183812; N8 Pyrido[2,3-d]pyrimidin-7-one deriv 72; 8-{bicyclo[221]heptan-2-yl}-2-({4-[4-(3-hydroxypropyl)piperidin-1-yl]phenyl}amino)-7H,8H-pyrido[2,3-d]pyrimidin-7-one; 8-(3-bicyclo[221]heptanyl)-2-[4-[4-(3-hydroxypropyl)piperidin-1-yl]anilino]pyrido[2,3-d]pyrimidin-7-one; PD0183813
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 4-[(6-chloropyrazin-2-yl)amino]benzenesulfonamide Investigative [22]
Synonyms
CHEMBL487738; 4-(6-chloropyrazin-2-ylamino)benzenesulfonamide; 642459-21-0; 2vtj; SCHEMBL6659290; BDBM24631; ZINC16052861; DB08134; FT-0723597; 4-[(6-chloropyrazin-2-yl)amino]benzene-1-sulfonamide; 4-[(6-chloropyrazin-2-yl)amino]benzenesulfonamide, 10
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1900 nM
External Link
 Compound Name PHENYLAMINOIMIDAZO(1,2-ALPHA)PYRIDINE Investigative [22]
Synonyms
4-{[6-(2,6-Dichlorobenzoyl)imidazo[1,2-A]pyridin-2-Yl]amino}benzenesulfonamide; 1ykr; 4-[[6-(2,6-dichlorobenzoyl)imidazo[1,2-a]pyridin-2-yl]amino]benzenesulfonamide; aminoimidazo[1,2-a]pyridine deriv. 2i; AC1NS9IQ; CHEMBL182260; BDBM6670; DB04607; 4-({6-[(2,6-dichlorophenyl)carbonyl]imidazo[1,2-a]pyridin-2-yl}amino)benzenesulfonamide
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 6-CYCLOHEXYLMETHOXY-2-(3'-CHLOROANILINO) PURINE Investigative [22]
Synonyms
N-(3-chlorophenyl)-6-(cyclohexylmethoxy)-7H-purin-2-amine; 444722-81-0; 1h1r; AC1L1IG7; CHEMBL341273; SCHEMBL6790651; BDBM5531; CTK1D2420; DTXSID10274437; O6-Cyclohexylmethylguanine deriv. 15; DB07203; 2-(3 -Chloroanilino)-6-cyclohexylmethoxypurine; N-(3-chlorophenyl)-6-(cyclohexylmethoxy)-9H-purin-2-amine; N-(3-Chlorophenyl)-6-(cyclohexylmethoxy)-9H-purine-2-amine; 1H-Purin-2-amine, N-(3-chlorophenyl)-6-(cyclohexylmethoxy)-
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name BOHEMINE Investigative [23]
Synonyms
189232-42-6; 3-((6-(Benzylamino)-9-isopropyl-9H-purin-2-yl)amino)propan-1-ol; 3-{[6-(benzylamino)-9-(propan-2-yl)-9h-purin-2-yl]amino}propan-1-ol; CHEMBL83980; CHEBI:86007; 2-(3-Hydroxypropylamino)-6-benzylamino-9-isopropylpurine; [6-Benzylamino-2-(3-hydroxypropylamino)-9-isopropylpurine; 2-[(3-hydroxypropyl)amino]-6-benzylamino-9-isopropylpurine; 3-{[6-(benzylamino)-9-isopropyl-9H-purin-2-yl]amino}propan-1-ol; purine deriv. 1; AC1L1DN2; SCHEMBL1443403; GTPL5938; BDBM10633; CTK8A4395; DTXSID00274365; EX-A931
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 800 nM
External Link
 Compound Name N-phenyl-1H-pyrazole-3-carboxamide Investigative [22]
Synonyms
124828-46-2; CHEMBL445420; N-phenyl-1H-pyrazole-5-carboxamide; 1H-Pyrazole-3-carboxylic Acid Phenylamide; MLS000519301; 2vtl; pyrazole amide, 15; pyrazole-5-carboxanilide; ChemDiv2_004267; AC1LE63W; SCHEMBL19748; N-phenylpyrazol-3-ylcarboxamide; SCHEMBL13373589; BDBM24636; MolPort-001-664-649; HMS2155C18; HMS3604B14; HMS1381B21; HMS3323C02; ALBB-018739; ZINC5286379; STK926745; BDBM50109707; AKOS000321787; DB08135; 1H-pyrazole-3-carboxamide, N-phenyl-; MCULE-7079696193; IDI1_002982; ST034406
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 97000 nM
External Link
 Compound Name 5-hydroxynaphthalene-1-sulfonamide Investigative [22]
Synonyms
17286-26-9; 5-Hydroxynaphthalene-1-sulphonamide; NFVBVKHGDDDCEA-UHFFFAOYSA-N; 5-Hydroxy-1-naphthalenesulfonamide; 5-hydroxy-naphthalene-1-sulfonic acid amide; 2vth; EINECS 241-319-7; AC1L3CSX; AC1Q6ULI; SCHEMBL588923; CHEMBL457047; CTK4D4388; NFVBVKHGDDDCEA-UHFFFAOYSA-; BDBM24628; DTXSID50169414; ZINC2242749; 5-hydroxy-1-naphthalenesulphonamide; 1-Naphthalenesulfonamide,5-hydroxy-; 1-Naphthalenesulfonamide, 5-hydroxy-; 5-hydroxynaphthalene-1-sulfonamide, 7; AKOS030618521; DB08132; TX-017211
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 120000 nM
External Link
 Compound Name N-(4-sulfamoylphenyl)-1H-indazole-3-carboxamide Investigative [22]
Synonyms
N-(4-Sulphamoylphenyl)-1H-indazole-3-carboxamide; 660822-60-6; 2vti; indazole amide, 14; CHEMBL455946; SCHEMBL4524087; BDBM24635; MNHPHKFLWAPNOV-UHFFFAOYSA-N; ZINC15270554; DB08133; DA-41761; FT-0707176; 1H-Indazole-3-carboxylic acid (4-sulphamoyl-phenyl)-amide
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 660 nM
External Link
 Compound Name N-(3-METHYLBUT-2-EN-1-YL)-9H-PURIN-6-AMINE Investigative [22]
Synonyms
2365-40-4; Isopentenyladenine; N6-Isopentenyladenine; N6-(2-Isopentenyl)adenine; Isopentenyl adenine; 6-(gamma,gamma-Dimethylallylamino)purine; IPADE; Dimethylallyladenine; N6-(2-Isopentenyl)-adenine; N6-Dimethylallyladenine; N6-(delta2-Isopentenyl)adenine; N-(3-Methyl-2-butenyl)adenine; N6-(3-Methyl-2-butenyl)adenine; N6-(delta 2-Isopentenyl)-adenine; N(6)-(delta(2)-Isopentenyl)adenine; 1H-Purin-6-amine, N-(3-methyl-2-butenyl)-; N-(3-methylbut-2-enyl)-7H-purin-6-amine; Adenine, N-
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 1-Amino-6-Cyclohex-3-Enylmethyloxypurine Investigative [24]
Synonyms
872556-74-6; 4-(cyclohexylmethoxy)-1H-imidazo[4,5-c]pyridin-6-amine; AC1L9IVC; CTK2I2667; DTXSID90332206; 3h-imidazo[4,5-c]pyridin-6-amine,4-(cyclohexylmethoxy)-; ZINC20149007; AKOS030619175; DB02603; KB-268453; 1H-Imidazo[4,5-c]pyridin-6-amine, 4-(cyclohexylmethoxy)-
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Benzyl-(9-isopropyl-9H-purin-6-yl)-amine Investigative [23]
Synonyms
CHEMBL85015; 111853-20-4; 9H-Purin-6-amine, 9-(1-methylethyl)-N-(phenylmethyl)-; purine deriv. 9; ACMC-20mewm; SCHEMBL754120; BDBM10641; CTK0D3360; DTXSID10444118; 6-(benzylamino)-9-isopropylpurine; ZINC13538226; AKOS030562149; 6-(Benzylamino)-9-isopropyl-9H-purine; N-benzyl-9-isopropyl-9H-purin-6-amine
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 4500 nM
External Link
 Compound Name N-(5-Cyclopropyl-1h-Pyrazol-3-Yl)Benzamide Investigative [24]
Synonyms
CHEMBL324942; N-(3-cyclopropyl-1H-pyrazol-5-yl)benzamide; N5B; 1vyz; AC1L9MPJ; SCHEMBL4314346; BDBM7127; LUCORKWTQSQFFU-UHFFFAOYSA-N; 3-Benzamidoaminopyrazole deriv. 4; DB02647
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 289.73 nM
External Link
 Compound Name TRIAZOLOPYRIMIDINE Investigative [22]
Synonyms
8-Azapurine; 273-40-5; 2H-triazolo[4,5-d]pyrimidine; 179268-22-5; 6H-1,2,3-Triazolo[4,5-d]pyrimidine; 2H-1,2,3-Triazolo[4,5-d]pyrimidine; 3H-1,2,3-Triazolo[4,5-d]pyrimidine; 3H-[1,2,3]triazolo[4,5-d]pyrimidine; triazolo[4,5-d]pyrimidine; triazolo(4,5-d)pyrimidine; 273-39-2; 99331-25-6; 3H-1,2,3-TRIAZOLO(4,5-D)PYRIMIDINE; ACMC-1CNOM; AC1L22AZ; SCHEMBL26606; 179268-21-4; SCHEMBL11026556; CTK1A0899; CTK0H1173; CTK0H1170; CTK3G7531; CTK0H1174; DTXSID80181745; GIIGHSIIKVOWKZ-UHFFFAOYSA-N; ZINC2020258; ACM273405; FCH907879; AKOS006372727
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 2-ANILINO-6-CYCLOHEXYLMETHOXYPURINE Investigative [22]
Synonyms
6-(cyclohexylmethoxy)-N-phenyl-7H-purin-2-amine; CHEMBL122264; 444722-80-9; 2A6; NU-6094; 1h1q; AC1L1BOU; SCHEMBL6791643; BDBM5530; CTK1D2421; DTXSID30274313; XWWRLKIBRPJQJX-UHFFFAOYSA-N; O6-Cyclohexylmethylguanine deriv 2; AKOS030619892; DB06948; N-Phenyl-6-(cyclohexylmethoxy)-9H-purine-2-amine; 6-(cyclohexylmethoxy)-N-phenyl-9H-purin-2-amine; 1H-Purin-2-amine,
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 2300 nM
External Link
 Compound Name SCH-546909 Investigative [25]
Synonyms
CDK2 inhibitors (cancer), Merck & Co; CDK2 inhibitors (cancer), Schering-Plough; Cyclindependent kinase 2 inhibitors (cancer), Schering-Plough
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 140 nM
External Link
 Compound Name PHA-690509 Investigative [26]
Synonyms
PHA-404611; PHA-533533; PNU-252808; PNU-292137; CDK inhibitors (cancer), Nerviano; Cyclin dependent kinase inhibitors (cancer), Nerviano; CDK-2 inhibitors (anticancer), Pfizer; CDK-2 inhibitors (anticancer), Pharmacia
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 4-(2,4-Dimethyl-Thiazol-5-Yl)-Pyrimidin-2-Ylamine Investigative [24]
Synonyms
364334-94-1; 4-(2,4-Dimethylthiazol-5-yl)pyrimidin-2-amine; 4-(2,4-DIMETHYL-1,3-THIAZOL-5-YL)PYRIMIDIN-2-AMINE; CTFDMGIBHFQWKB-UHFFFAOYSA-N; 4-(2,4-dimethylthiazol-5-yl)pyrimidin-2-ylamine; CK2; 4-(dimethyl-1,3-thiazol-5-yl)pyrimidin-2-amine; 1pxj; 2c5o; AC1L9LFI; Maybridge3_001247; CHEMBL47302; CS12; SCHEMBL4314069; BDBM8037; CTK4H6460; DTXSID70332264; MolPort-002-896-655; HMS1434I15; ZINC141286; HMS3604E21; ANW-58550; 4623AB; AKOS013063215; MCULE-3137548628; DB02091; CCG-243780
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 396 nM
External Link
 Compound Name VER-54505 Investigative [25]
Synonyms
Cdk2 inhibitors, Vernalis; RBT-0049985
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 2-Amino-6-Chloropyrazine Investigative [24]
Synonyms
33332-28-4; 6-chloropyrazin-2-amine; 2-chloro-6-aminopyrazine; Pyrazinamine, 6-chloro-; 2-Pyrazinamine, 6-chloro-; 6-Chloro-pyrazin-2-ylamine; 6-chloropyrazin-2-ylamine; 2-amino-6-chloro-pyrazine; CHEMBL191632; 6-CHLORO-2-PYRAZINAMINE; CIG; 6-chlorpyrazin-2-amin; 1wcc; PubChem8543; zlchem 1337; AI3-61778; AC1Q3PRB; AC1L3MZH; ACMC-209i0e; 6-chloropyrazine-2-ylamine; SCHEMBL67803; 6-chloro-pyrazin-2-yl-amine; 6-chloropyrazin-2-amine, 5; KSC222G6J; AC1Q52Q1; Jsp006119; DTXSID0067761; CTK1C2364; BDBM24626; ZLE0115
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 350000 nM
External Link
 Compound Name 6-cyclohexylmethyloxy-2-(4'-hydroxyanilino)purine Investigative [22]
Synonyms
CHEMBL340813; 4-{[6-(cyclohexylmethoxy)-9H-purin-2-yl]amino}phenol; N20; NU-6086; 1oi9; AC1L9L2Q; BDBM5541; SCHEMBL6792176; O6-Cyclohexylmethylguanine deriv 25; DB08233; 6-Cyclohexylmethoxy-2-(4 -hydroxyanilino)purine
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1000 nM
External Link
 Compound Name 6-(Cyclohex-3-enylmethoxy)-9H-purin-2-ylamine Investigative [27]
Synonyms
CHEMBL115498; O6-Substituted Guanine Deriv. 27; AC1NS6ZQ; 9H-Purin-2-amine, 6-(3-cyclohexen-1-ylmethoxy)-; SCHEMBL6267556; BDBM5487; 220035-95-0; 6-(cyclohex-3-en-1-ylmethoxy)-9H-purin-2-amine
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name (2'Z,3'E)-5-Chloro-5'-chloro-indirubin-3'-oxime Investigative [28]
MOA Inhibitor
External Link
 Compound Name 6-Cyclohexylmethoxy-pyrimidine-2,4,5-triamine Investigative [29]
Synonyms
6-(cyclohexylmethoxy)pyrimidine-2,4,5-triamine; pyrimidine deriv. 16; AC1NS76Q; CHEMBL71036; BDBM5588; SCHEMBL6263731; IMNSQZHRHASLAR-UHFFFAOYSA-N
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name (2'Z,3'E)-5-Chloro-5'-methyl-indirubin-3'-oxime Investigative [28]
MOA Inhibitor
External Link
 Compound Name 6-(3-Methyl-benzyloxy)-9H-purin-2-ylamine Investigative [27]
Synonyms
O6-Substituted Guanine Deriv. 32; CHEMBL405773; BDBM5492; AC1NS702; SCHEMBL12227591; O6-[3-(Methyl)Benzyl]Guanine; ZINC13475147; 2-Amino-6-(3 -methylbenzyl)oxypurine; 6-[(3-methylphenyl)methoxy]-9H-purin-2-amine
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name (2'Z,3'E)-5-Fluoro-5'-methoxy-indirubin-3'-oxime Investigative [28]
MOA Inhibitor
External Link
 Compound Name JNJ-7706621 Investigative [30]
Synonyms
443797-96-4; JNJ7706621; 4-((5-Amino-1-(2,6-difluorobenzoyl)-1H-1,2,4-triazol-3-yl)amino)benzenesulfonamide; UNII-74GK72DON8; RWJ-387252; 4-[[5-amino-1-(2,6-difluorobenzoyl)-1,2,4-triazol-3-yl]amino]benzenesulfonamide; CHEMBL191003; 74GK72DON8; 4-[[5-Amino-1-(2,6-difluorobenzoyl)-1H-1,2,4-triazol-3-yl]amino]benzenesulfonamide; JNJ 7706621; 4-(5-amino-1-(2,6-difluorobenzoyl)-1H-1,2,4-triazol-3-ylamino)benzenesulfonamide
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 2 nM
External Link
 Compound Name GW-8510 Investigative [31]
MOA Inhibitor
Activity IC50 = 9.7 nM
External Link
 Compound Name BMS-265246 Investigative [32]
Synonyms
BMS 265246; BMS265246
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name (2'Z,3'E)-5-Fluoro-5'-fluoro-indirubin-3'-oxime Investigative [28]
MOA Inhibitor
External Link
 Compound Name (2'Z,3'E)-5-Fluoro-5'-chloro-indirubin-3'-oxime Investigative [28]
MOA Inhibitor
External Link
 Compound Name RESCOVITINE Investigative [33]
Synonyms
CHEMBL1087791
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Cdk4 inhibitor III Investigative [34]
Synonyms
Ryuvidine; 265312-55-8; CHEMBL290904; 2-Methyl-5-[(4-methylphenyl)amino]benzothiazole-4,7-dione; 5-(N-(4-Methylphenyl)amino)-2-methyl-4,7-dioxobenzothiazole; 2-methyl-5-(4-methylanilino)-1,3-benzothiazole-4,7-dione; AC1Q6BBC; AC1LA59T; 2-Methyl-5-p-tolylamino-benzothiazole-4,7-dione; SCHEMBL2169284; GTPL5952; CTK4F8075; CHEBI:92119; AOB6479; MolPort-023-276-509; HMS3269F11; HMS3229E08; ZINC5930916; BDBM50086655; 2-METHYL-5-[(4-METHYLPHENYL)AMINO]-4,7-BENZOTHIAZOLEDIONE; AKOS024457195; CCG-206830
    Click to Show/Hide
MOA Inhibitor
Activity IC50 > 200000 nM
External Link
 Compound Name 6-(3-Amino-benzyloxy)-9H-purin-2-ylamine Investigative [27]
Synonyms
O6-Substituted Guanine Deriv. 33; BDBM5493; CHEMBL270977; AC1NS705; 2-Amino-6-(3 -aminobenzyl)oxypurine; 6-[(3-aminophenyl)methoxy]-9H-purin-2-amine
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name (2'Z,3'E)-5-Chloro-5'-fluoro-indirubin-3'-oxime Investigative [28]
MOA Inhibitor
External Link
 Compound Name 2-((3,5-diamino-1H-pyrazol-4-yl)diazenyl)phenol Investigative [35]
MOA Inhibitor
External Link
 Compound Name 5-nitroindirubin-3'-oxime Investigative [28]
MOA Inhibitor
External Link
 Compound Name (2'Z,3'E)-5-Nitro-5'-methyl-indirubin-3'-oxime Investigative [28]
MOA Inhibitor
External Link
 Compound Name (2'Z,3'E)-5-Nitro-5'-chloro-indirubin-3'-oxime Investigative [28]
MOA Inhibitor
External Link
 Compound Name (2'Z,3'E)-5-Fluoro-5'-hydroxy-indirubin-3'-oxime Investigative [28]
MOA Inhibitor
External Link
 Compound Name (2'Z,3'E)-5-Chloro-5'-hydroxy-indirubin-3'-oxime Investigative [28]
MOA Inhibitor
External Link
 Compound Name 4-[3-Hydroxyanilino]-6,7-Dimethoxyquinazoline Investigative [36]
Synonyms
whi-p180; 211555-08-7; 3-[(6,7-dimethoxyquinazolin-4-yl)amino]phenol; WHI-P180, Hydrochloride; JANEX 3; CHEMBL127907; 3-((6,7-Dimethoxyquinazolin-4-yl)amino)phenol; AK341047; DTQ; 4-(3&amp; -Hydroxyphenyl)amino-6,7-dimethoxyquinazoline, HCl; JANEX-3; 4btk; 1di8; AC1L1KWT; AC1Q4XVE; 3-(6,7-dimethoxyquinazolin-4-ylamino)phenol; Anilinoquinazoline deriv 5; WHI-P180(Janex 3); BDBM4622; SCHEMBL1180103; CTK4E5981; AOB5495; MolPort-000-672-017; BNDYIYYKEIXHNK-UHFFFAOYSA-N; HMS3229P15
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1000 nM
External Link
 Compound Name (2'Z,3'E)-5-Nitro-5'-fluoro-indirubin-3'-oxime Investigative [28]
MOA Inhibitor
External Link
 Compound Name (2'Z,3'E)-5-Nitro-5'-methoxy-indirubin-3'-oxime Investigative [28]
MOA Inhibitor
External Link
 Compound Name Oxindole 95 Investigative [20]
MOA Inhibitor
External Link
 Compound Name CVT-313 Investigative [25]
Synonyms
AC1OCFD4; NG 26
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 6-O-Cyclohexylmethyl Guanine Investigative [24]
Synonyms
6-(Cyclohexylmethoxy)-9H-purin-2-amine; nu2058; 161058-83-9; 2-amino-6-[(cyclohexylmethyl)oxy]purine; NU 2058; 2-amino-6-cyclohexylmethoxypurine; NU-2058; O6-Cyclohexylmethylguanine; CHEMBL269881; 1e1v; 1h1p; O-Cyclohexylmethylguanine; AC1Q4XUD; 9H-Purin-2-amine, 6-(cyclohexylmethoxy)-; O6-Cyclohexylmethyl guanine; AC1L1IG4; MLS001074898; SCHEMBL3462331; BDBM5485; CTK8D6642; CTK0E6580; EX-A790; AOB6207; MolPort-033-437-778; MolPort-003-958-993; MolPort-044-561-861; HMS3372K06; HMS3262L18; HMS2233F06
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 1200 nM
External Link
 Compound Name NU-6027 Investigative [29]
MOA Inhibitor
Activity Ki = 1300 nM
External Link
 Compound Name NSC-625987 Investigative [37]
Synonyms
NSC 625987
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name (2'Z,3'E)-5-Fluoro-5'-methyl-indirubin-3'-oxime Investigative [28]
MOA Inhibitor
External Link
 Compound Name (2'Z,3'E)-5-Nitro-5'-hydroxy-indirubin-3'-oxime Investigative [28]
MOA Inhibitor
External Link
 Compound Name aloisine Investigative [38]
Synonyms
IN1538; RP106
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name MERIOLIN 8 Investigative [39]
Synonyms
SCHEMBL2991886; CHEMBL406102
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name PYRAZOLOPYRIDAZINE 1 Investigative [40]
Synonyms
551920-54-8; GW810576X; n-(3-methoxyphenyl)-4-pyrazolo[1,5-b]pyridazin-3-yl-2-pyrimidinamine; pyrazolo[1,5-b]pyridazine deriv. 19; AC1O6ZIQ; CHEMBL187081; BDBM8128; SCHEMBL4489357; CTK1F7320; DTXSID60424889; HMS3305F24; HMS3303K24; ZINC13582569; NCGC00242229-01; DA-42106; FT-0707969; AB01092291-01; 2-Pyrimidinamine, N-(3-methoxyphenyl)-4-pyrazolo[1,5-b]pyridazin-3-yl-; N-(3-methoxyphenyl)-4-pyrazolo[1,5-b]pyridazin-3-ylpyrimidin-2-amine
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1.995 nM
External Link
 Compound Name Purvalanol A Investigative [41]
Synonyms
Purvalanola; AC1L1JD0; IN1131; 2-(1R-Isopropyl-2-hydroxyethylamino)-6-(3-chloroanilino)-9-isopropyl-purine; SCHEMBL3311119; GTPL6030; CTK8F1120; CHEBI:93781; HMS3229M14; KS-00001DB0; HSCI1_000128; AKOS030238850; CCG-206875; RT-015158; K00014; 2-[[6-(3-chloroanilino)-9-propan-2-ylpurin-2-yl]amino]-3-methylbutan-1-ol
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 70 nM
External Link
 Compound Name Cdk1/2 inhibitor III Investigative [42]
Synonyms
443798-55-8; CDK 1/2 INHIBITOR; UNII-LFR1253W75; LFR1253W75; 5-AMINO-3-{[4-(AMINOSULFONYL)PHENYL]AMINO}-N-(2,6-DIFLUOROPHENYL)-1H-1,2,4-TRIAZOLE-1-CARBOTHIOAMIDE; 5-amino-N-(2,6-difluorophenyl)-3-[(4-sulfamoylphenyl)amino]-1H-1,2,4-triazole-1-carbothioamide; 5-Amino-3-((4-(aminosulfonyl)phenyl)amino)-N-(2,6-difluorophenyl)-1H-1,2,4-triazole-1-carbothioamide; 2wu6; AC1NS9OB; CHEMBL261720; GTPL5946; BDBM6878; SCHEMBL1394721; CTK8E9250; DTXSID60416209; MolPort-044-561-528; HMS3229C16; ZINC12355112; DB07664
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name MERIOLIN 1 Investigative [39]
Synonyms
341998-55-8; 4-(1H-PYRROLO[2,3-B]PYRIDIN-3-YL)PYRIMIDIN-2-AMINE; 2-Pyrimidinamine, 4-(1H-pyrrolo[2,3-b]pyridin-3-yl)-; SCHEMBL2241315; CHEMBL405665; HQHSJJZIICGOIX-UHFFFAOYSA-; CTK1B7876; DTXSID60469811; BDBM50371404; ZINC29135178; AKOS027252841; 4-(7-aza-indol-3-yl)-2-amino pyrimidine; 3-(2-Amino-4-pyrimidinyl)-1H-pyrrolo[2,3-b]pyridine
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name MERIOLIN 4 Investigative [39]
Synonyms
SCHEMBL3001373; CHEMBL406464
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Lysine Nz-Carboxylic Acid Investigative [24]
Synonyms
N(6)-carboxylysine; N(6)-carboxy-L-lysine; (2S)-2-amino-6-(carboxyamino)hexanoic acid; N~6~-carboxy-L-lysine; SCHEMBL357483; CHEBI:43575; ZINC6753301
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name MERIOLIN 6 Investigative [39]
Synonyms
CHEMBL406463; SCHEMBL2999009
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name K00024 Investigative [43]
Synonyms
indolocarbazole deriv. 4(d)
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 10Z-Hymenialdisine Investigative [20]
Synonyms
Hymenialdisine; (Z)-Hymenialdisine; CHEMBL361708; 95569-43-0; 82005-12-7; (4Z)-4-(2-amino-4-oxo-1H-imidazol-5-ylidene)-2-bromo-1,5,6,7-tetrahydropyrrolo[2,3-c]azepin-8-one; Hymenialdisine, 1; 4-(2-Amino-4-oxo-2-imidazolidin-5-ylidene)-2-bromo-4,5,6,7-tetrahydropyrrolo[2,3-c]azepin-8-one; AC1MHZEP; SCHEMBL155899; STO156; BDBM7491; SCHEMBL15426167; MolPort-006-394-608; 4-(2-Amino-5-oxo-3,5-dihydro-imidazol-4-ylidene)-2-bromo-4,5,6,7-tetrahydro-1H-pyrrolo[2,3-c]azepin-8-one; NSC607173
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name aminopurvalanol A Investigative [44]
Synonyms
NG-97
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 9-Nitropaullone Investigative [20]
Synonyms
Alsterpaullone; 237430-03-4; NSC 705701; NSC-705701; CHEMBL50894; MLS002702475; 9-Nitro-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one; 9-nitro-7,12-dihydro-5H-indolo[3,2-d][1]benzazepin-6-one; 9-Nitro-7,12-dihydroindolo-[3,2-d][1]benzazepin-6(5)-one; 9-NITRO-5,12-DIHYDRO-7H-BENZO[2,3]AZEPINO[4,5-B]INDOL-6-ONE; Paullone Analog 1; AC1NMCUD; Kinome_3754; 1q3w; Alsterpaullone derivative, 2; Lopac0_000057; CBiol_001723; GTPL5925; BDBM7262; SCHEMBL2170104; CTK8F0374; ZINC23894; BDBM84528; DTXSID50407444
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 15 nM
External Link
 Compound Name MERIOLIN 5 Investigative [39]
Synonyms
1011711-76-4; 4-(4-Propoxy-1h-Pyrrolo[2,3-B]pyridin-3-Yl)pyrimidin-2-Amine; 4-{4-propoxy-1H-pyrrolo[2,3-b]pyridin-3-yl}pyrimidin-2-amine; SCHEMBL2997013; CHEMBL270687; ZINC16052674; BDBM50371400; DB08182
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name SU9516 Investigative [20]
Synonyms
377090-84-1; SU 9516; SU-9516; AC1NRD9P; 666837-93-0; (3Z)-3-(1H-IMIDAZOL-5-YLMETHYLENE)-5-METHOXY-1H-INDOL-2(3H)-ONE; (Z)-3-((1H-imidazol-5-yl)methylene)-5-methoxyindolin-2-one; (3Z)-3-(1H-imidazol-5-ylmethylidene)-5-methoxy-2,3-dihydro-1H-indol-2-one; 3-[1-(3H-Imidazol-4-yl)-meth-(Z)-ylidene]-5-methoxy-1,3-dihydro-indol-2-one; SU9; (Z)-1,3-DIHYDRO-3-(1H-IMIDAZOL-4-YLMETHYLENE)-5-METHOXY-2H-INDOL-2-ONE; 3py1; 3py0; imidazole indolinone driv.; MLS001074893; SCHEMBL1170686; BDBM7238; SCHEMBL1170687; CHEMBL258805
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 22 nM
External Link
 Compound Name PYRAZOLOPYRIDAZINE 2 Investigative [40]
Synonyms
pyrazolo[1,5-b]pyridazine deriv. 25; AC1O6ZJ2; BDBM8134; CHEMBL186054; N-(3,4-dimethoxyphenyl)-4-pyrazolo[1,5-b]pyridazin-3-ylpyrimidin-2-amine
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 50 nM
External Link
 Compound Name MERIOLIN 3 Investigative [39]
Synonyms
954143-48-7; 4-(4-Methoxy-1h-Pyrrolo[2,3-B]pyridin-3-Yl)pyrimidin-2-Amine; 4-{4-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl}pyrimidin-2-amine; SCHEMBL2996575; CHEMBL270686; BDBM50371402; ZINC16052675; DB08178; KB-274295
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name MERIOLIN 2 Investigative [39]
Synonyms
SCHEMBL2999865; CHEMBL270897; 1H-Pyrrolo[2,3-b]pyridin-4-ol, 3-(2-amino-4-pyrimidinyl)-; BDBM50371403; 954143-47-6
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name PMID18986805C9b Investigative [45]
Synonyms
GTPL8160; BDBM50246396; ZINC38224644
    Click to Show/Hide
MOA Inhibitor
Activity IC50 < 1 nM
External Link
 Compound Name 3-((3,5-diamino-1H-pyrazol-4-yl)diazenyl)phenol Investigative [35]
MOA Inhibitor
External Link
 Compound Name Indirubin-5-sulfonate Investigative [20]
Synonyms
indirubin-5-sulphonate; CHEMBL1207227; 2',3-DIOXO-1,1',2',3-TETRAHYDRO-2,3'-BIINDOLE-5'-SULFONIC ACID; INR; AC1NRBUE; AC1NZHHM; 1v0o; AC1O8NUW; Indirubin derivative, 20; SCHEMBL490806; BDBM84534; A05-A11B1-I; NSC717821; BDBM50023871; NSC-717821; DB02519; NCI60_040625; 2-oxo-3-(3-oxo-1H-indol-2-ylidene)-1H-indole-5-sulfonic acid; (3Z)-2-oxo-3-(3-oxoindolin-2-ylidene)indoline-5-sulfonic acid; (3E)-2-oxo-3-(3-oxo-1H-indol-2-ylidene)-1H-indole-5-sulfonic acid; (2Z)-2',3-dioxo-1,1',2',3-tetrahydro-2,3'-biindole-5'-sulfonic acid
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 22 nM
External Link
 Compound Name N-(4-amino-5-cyano-6-phenylpyridin-2-yl)acetamide Investigative [46]
Synonyms
Kinome_3019; CHEMBL210032; SCHEMBL1145340; BDBM15968; Aminopyridine-Based Inhibitor 24
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 1300 nM
External Link
 Compound Name NU-6102 Investigative [47]
Synonyms
nu6102; 444722-95-6; NU 6102; O6-CYCLOHEXYLMETHOXY-2-(4'-SULPHAMOYLANILINO) PURINE; Cdk1/2 Inhibitor II, NU6102; 6-Cyclohexylmethoxy-2-(4&amp; -sulfamoylanilino)purine; 4-{[6-(cyclohexylmethoxy)-9H-purin-2-yl]amino}benzenesulfonamide; 4SP; 1h1s; 4-[[6-(cyclohexylmethoxy)-7H-purin-2-yl]amino]benzenesulfonamide; 4-{[6-(cyclohexylmethoxy)-7h-purin-2-yl]amino}benzenesulfonamide; 4-[[6-(cyclohexylmethoxy)-9h-purin-2-yl]amino]benzenesulfonamide; 4eor; 4eok; 2iw9; 2c6o; 2iw8; AC1L1IGA; SCHEMBL2170816; CHEMBL319467
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 5 nM
External Link
 Compound Name PF-228 Investigative [48]
Synonyms
869288-64-2; PF-573228; PF 573228; PF573228; CHEMBL514554; 3,4-Dihydro-6-[[4-[[[3-(methylsulfonyl)phenyl]methyl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]-2(1H)-quinolinone; 6-((4-((3-(Methylsulfonyl)benzyl)amino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)-3,4-dihydroquinolin-2(1H)-one; 6-(4-(3-(methylsulfonyl)benzylamino)-5-(trifluoromethyl)pyrimidin-2-ylamino)-3,4-dihydroquinolin-2(1H)-one; 6-[4-(3-Methanesulfonyl-benzylamino)-5-trifluoromethyl-pyrimidin-2-ylamino]-3,4-dihydro-1H-quinolin-2-one
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name aloisine A Investigative [49]
Synonyms
4-(7-butyl-5H-pyrrolo[2,3-b]pyrazin-6-yl)phenol; 496864-16-5; RP107; 6-PHENYL[5H]PYRROLO[2,3-B]PYRAZINE; CHEMBL75680; 7-n-Butyl-6-(4-hydroxyphenyl)[5H]pyrrolo[2,3-b]pyrazine; RP-107; ALH; 4-{7-butyl-5H-pyrrolo[2,3-b]pyrazin-6-yl}phenol; 1ung; SCHEMBL80147; BDBM7377; GTPL5924; AC1NS169; 4-(7-Butyl-5H-pyrrolo[2,3-b]pyrazin-6-yl)-phenol; CHEBI:93641; CTK8D4068; DTXSID30416115; HMS3229A14; RM-39; BCP26893; ZINC2540737; ACT06534; IN1539; HSCI1_000219; MFCD04973541; AKOS005145972; CCG-206814; DB07364; RTC-063070; AJ-39131
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name NU6140 Investigative [50]
Synonyms
Cdk2 Inhibitor IV, NU6140; 444723-13-1; NU 6140; CHEMBL1802728; 4-(6-Cyclohexylmethoxy-9H-purin-2-ylamino)-N,N-diethylbenzamide; 4-{[6-(cyclohexylmethoxy)-7H-purin-2-yl]amino}-N,N-diethylbenzamide; Cdk2 inhibitor IV; SCHEMBL2169233; GTPL5949; CTK8E7940; DTXSID30436732; MolPort-023-276-742; MolPort-044-561-419; HMS3229E18; IN1369; ZINC22309248; BDBM50347924; AKOS024457537; CCG-206836; NCGC00370819-01; NU6140, &gt; RT-011957; 4-(6-cyclohexylmethoxy-9hpurin-2-ylamino)-N,N-diethyl-benzamide
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 400 nM
External Link
 Compound Name BX-912 Investigative [51]
Synonyms
BX 912; BX912
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name BX-795 Investigative [51]
Synonyms
BX795; BX 795
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name PMID19115845C89S Investigative [52]
Synonyms
3du8; GTPL8114; BDBM27380; DB07149
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 138 nM
External Link
 Compound Name Indirubin-3'-monoxime Investigative [20]
Synonyms
indirubin-3'-oxime; 160807-49-8; indirubin-3-oxime; Indirubin-3monoxime; Indirubin-3-monoxime; 3-[3-(Hydroxyamino)-1H-indol-2-yl]indol-2-one; CHEBI:43645; Indirubin 3'-monoxime; indirubin-3'-monooxime; Indirubin-3&amp; CHEMBL216543; CHEMBL126077; (Z)-1H,1'H-[2,3']BIINDOLYLIDENE-3,2'-DIONE-3-OXIME; UNM-0000305771; 3-[1,3-dihydro-3-(hydroxyimino)-2H-indol-2-ylidene]-1,3-dihydro-2H-indol-2-one; 667463-82-3; IXM; SR-01000075929; Indirubin-3; Indirubin 3-oxime; Tocris-1813; BiomolKI_000070
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Double Oxidized Cysteine Investigative [24]
MOA Inhibitor
External Link
 Compound Name 3-(indole-3-yl)-4-phenyl-1H-pyrrole-2,5-dione Investigative [53]
Synonyms
CHEMBL380598; SCHEMBL3148490; HVQJGNALTWNDMX-UHFFFAOYSA-N; BDBM50375058; 2-(1H-Indole-3-yl)-3-phenylmaleimide
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name BMS-536924 Investigative [54]
MOA Inhibitor
External Link
 Compound Name 3,4-di-(4-methoxyphenyl)-1H-pyrrole-2,5-dione Investigative [53]
Synonyms
1H-Pyrrole-2,5-dione, 3,4-bis(4-methoxyphenyl)-; 108774-82-9; ACMC-20mbs9; CHEMBL381099; CTK0G2626; DTXSID90449388
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 3,4-diphenyl-1H-pyrrole-2,5-dione Investigative [53]
Synonyms
2,3-diphenylmaleimide; 1H-Pyrrole-2,5-dione, 3,4-diphenyl-; 31295-36-0; AC1MBL6S; SCHEMBL114611; CHEMBL201949; CTK1B9880; 3,4-diphenylpyrrole-2,5-dione; DTXSID70372903; ZINC3847556
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 3-(4-methoxyphenyl)-4-phenyl-1H-pyrrole-2,5-dione Investigative [53]
Synonyms
CHEMBL372076; SCHEMBL3822337
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol Investigative [35]
MOA Inhibitor
External Link
2A00: Brain cancer 53 Compound(s) Regulating the Disease Click to Show/Hide the Full List
 Compound Name Zinostatin stimalamer Approved [55]
Synonyms
Smancs (TN)
    Click to Show/Hide
External Link
 Compound Name Motexafin gadolinium Approved [56]
Synonyms
Xcytrin; Gadolinium texaphyrin; GdT2B2; GD-Tex; Motexafin gadolinium (USAN); PCI-0120; Xcytrin (TN)
    Click to Show/Hide
External Link
 Compound Name Lomustine Approved [57]
Synonyms
Belustine; CCNU; CINU; Cecenu; CeeNU; Chloroethylcyclohexylnitrosourea; Lomustina; Lomustinum; Bristol Myers Squibb Brand of Lomustine; CCNU [Chloroethyl nitrosoureas]; Cyclohexyl chloroethyl nitrosourea; Lomustine medac Brand; Medac Brand of Lomustine; Rhone Poulenc Rorer Brand of Lomustine; OR5087; RB 1509; SRI 2200; Bristol-Myers Squibb Brand of Lomustine; CeeNU (TN); Lomustina [INN-Spanish]; Lomustinum [INN-Latin]; NPFAPI-06; Rhone-Poulenc Rorer Brand of Lomustine; CeeNU, CCNU, Lomustine; Lomustine (USAN/INN); Lomustine [USAN:BAN:INN]; N-(2-Chloroethyl)-N'-cyclohexyl-N-nitrosourea; (Chloro-2-ethyl)-1-cyclohexyl-3-nitrosourea; (Cloro-2-etil)-1-cicloesil-3-nitrosourea; (Cloro-2-etil)-1-cicloesil-3-nitrosourea [Italian];1-(2-Chloroethyl)-3-cyclohexyl-1-nitrosourea; 1-(2-Chloroethyl)-3-cyclohexyl-1-nitrosourea [Chloroethyl nitrosoureas]; 1-(2-Chloroethyl)-3-cyclohexylnitrosourea
    Click to Show/Hide
External Link
 Compound Name Borocaptate sodium B 10 Approved [55]
External Link
 Compound Name DTI-015 Approved [58]
Synonyms
Carmustine; 154-93-8; 1,3-Bis(2-chloroethyl)-1-nitrosourea; BCNU; Carmustin; Nitrumon; Carmubris; Gliadel; BiCNU; Bi CNU; Carmustinum; Bischlorethylnitrosurea; Bischlorethylnitrosourea; Carmustina; Becenun; Becenum; Bischloroethyl nitrosourea; N,N'-BIS(2-CHLOROETHYL)-N-NITROSOUREA; Bis(2-chloroethyl)nitrosourea; Urea, N,N'-bis(2-chloroethyl)-N-nitroso-; Gliadel Wafer; FDA 0345; Bischloroethylnitrosourea; SRI 1720; 1,3-Bis(2-chloroethyl)nitrosourea; BiCNU (TN); Carmustinum [INN-Latin]; Carmustina [INN-Spanish]; DTI 015; NCI-C04773; SK; Injectable carmustine, Direct Therapeutics
    Click to Show/Hide
External Link
 Compound Name Prinomastat Approved [59]
Synonyms
AG-3354; AG-3362; Prinomastat (USAN/INN); (3S)-N-hydroxy-2,2-dimethyl-4-(4-pyridin-4-yloxyphenyl)sulfonylthiomorpholine-3-carboxamide
    Click to Show/Hide
External Link
 Compound Name INO-1001 Phase 3 [60]
Synonyms
Hypoxanthine arabinoside; LT00454797; 9-[(3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-3H-purin-6-one
    Click to Show/Hide
External Link
 Compound Name GliAtak Phase 3 [61]
Synonyms
GliAtak (TN)
    Click to Show/Hide
External Link
 Compound Name SOT-107 Phase 3 [62]
Synonyms
TransMID
    Click to Show/Hide
External Link
 Compound Name ICT-107 Phase 3 [63]
External Link
 Compound Name Cintredekin besudotox Phase 3 [64]
External Link
 Compound Name Rindopepimut Phase 3 [65]
External Link
 Compound Name DCVax-Ovarian Phase 3 [66]
Synonyms
DCVax-L; Dendritic cell-based immunotherapy (ovarian cancer), Northwest Biotherapeutics
    Click to Show/Hide
External Link
 Compound Name DCVax-Brain Phase 3 [67]
Synonyms
Dendritic cell-based immunotherapy (brain cancer), Northwest Biotherapeutics
    Click to Show/Hide
External Link
 Compound Name TVI-Brain-1 Phase 2/3 [68]
External Link
 Compound Name NLG8189 Phase 2/3 [10]
Synonyms
1-Methyl-D-tryptophan; Indoximod; 110117-83-4; D-Tryptophan, 1-methyl-; D-1MT; Indoximod (NLG-8189); D-1-methyltryptophan; UNII-TX5CYN1KMZ; D-(+)-1-Methyltryptophan; TX5CYN1KMZ; (R)-2-amino-3-(1-methyl-1H-indol-3-yl)propanoic acid; (2R)-2-amino-3-(1-methylindol-3-yl)propanoic acid; NSC-721782; (2R)-2-amino-3-(1-methyl-3-indolyl)propanoic acid; 1-MT; (2R)-2-azanyl-3-(1-methylindol-3-yl)propanoic acid; (2R)-2-amino-3-(1-methyl-1H-indol-3-yl)propanoic acid; D-l-Methyltryptophan; Indoximod [USAN:INN]; NLG-8189; NLG 8189
    Click to Show/Hide
External Link
 Compound Name Synthetic survivin peptide vaccine Phase 2 [69]
External Link
 Compound Name Fresolimumab Phase 2 [70]
Synonyms
GC-1008
    Click to Show/Hide
External Link
 Compound Name DNX-2401 Phase 2 [71]
Synonyms
Tasadenoturev
    Click to Show/Hide
External Link
 Compound Name TVI-Brain-1 cancer vaccine Phase 2 [72]
External Link
 Compound Name PDT with Photofrin Phase 2 [10]
External Link
 Compound Name F18-ML-10 Phase 2 [73]
External Link
 Compound Name PT2385 Phase 2 [74]
Synonyms
ONBSHRSJOPSEGS-INIZCTEOSA-N; PT-2385; UNII-6O16716DXP; 1672665-49-4; 6O16716DXP; SCHEMBL16555810; ZINC230453533; AKOS030526641; HY-12867; PT2385,1672665-49-4, PT 2385,PT-2385; Benzonitrile, 3-(((1S)-2,2-difluoro-2,3-dihydro-1-hydroxy-7-(methylsulfonyl)-1H-inden-4-yl)oxy)-5-fluoro-; 3-{[(1s)-2,2-Difluoro-1-Hydroxy-7-(Methylsulfonyl)-2,3-Dihydro-1h-Inden-4-Yl]oxy}-5-Fluorobenzonitrile; 3-(((1S)-2,2-Difluoro-1-hydroxy-7-methanesulfonyl-2,3-dihydro-1hinden-4-yl)oxy)-5-fluorobenzonitrile; 79A
    Click to Show/Hide
External Link
 Compound Name ABT-414 Phase 2 [75]
External Link
 Compound Name CLR1404-I-124 Phase 1/2 [76]
External Link
 Compound Name DM-CHOC-PEN Phase 2 [77]
External Link
 Compound Name L-alanosine Phase 2 [78]
Synonyms
SDX-102
    Click to Show/Hide
External Link
 Compound Name APX005M Phase 2 [10]
External Link
 Compound Name WP-1066 Phase 1/2 [72]
Synonyms
WP1066; 857064-38-1; (S,E)-3-(6-Bromopyridin-2-yl)-2-cyano-N-(1-phenylethyl)acrylamide; WP 1066; UNII-63V8AIE65T; 63V8AIE65T; AK-99218; C17H14BrN3O; (E)-3-(6-bromopyridin-2-yl)-2-cyano-N-[(1S)-1-phenylethyl]prop-2-enamide; MLS006010178; SCHEMBL1315826; QCR-16; SCHEMBL1315831; GTPL7972; CHEMBL1923234; EX-A760; AOB1497; DTXSID50235007; MolPort-044-723-708; MolPort-023-219-149; ZINC13983221; AKOS016007983; WP1066/WP-1066; CS-2736; DB12679; 2-Propenamide, 3-(6-bromo-2-pyridinyl)-2-cyano-N-((1S)-1-phenylethyl)-, (2E)-; HY-15312
    Click to Show/Hide
External Link
 Compound Name Anti-EGFRvIII CAR transduced PBL Phase 1/2 [79]
External Link
 Compound Name RG6156 Phase 1 [80]
External Link
 Compound Name rhenium-186 Phase 1 [81]
Synonyms
(~186~Re)Rhenium; 14998-63-1; 186Re; DTXSID60933825; Q18882928; RHENIUM (186-RE); Rhenium Re-186; Rhenium, isotope of mass 186; Rhenium-186; RHENIUM-186 [WHO-DD]; UNII-ZU7F1ET6TM; ZU7F1ET6TM
    Click to Show/Hide
External Link
 Compound Name IGV-001 Phase 1 [82]
External Link
 Compound Name DA-3607 Phase 1 [83]
Synonyms
Ad-stTRAIL; TRAIL adenoviral gene therapy (cancer), Dong-A
    Click to Show/Hide
External Link
 Compound Name DC/I540/KLH vaccine Phase 1 [84]
Synonyms
HTERT:540-548; Telomerase: 540-548 peptide vaccine; DC/I540/KLH vaccine (cancer); Dendritic cell/hTERT peptide I540/keyhole limpet hemocyanin vaccine, Dana-Farber; DC/I540/KLH vaccine (cancer), Dana-Farber
    Click to Show/Hide
External Link
 Compound Name KX2-361 Phase 1 [85]
Synonyms
KX-02
    Click to Show/Hide
External Link
 Compound Name MR1-1 Phase 1 [86]
Synonyms
MR1-1KDEL; EGFR-specific immunotoxin, IVAX; Anticancer immunotoxin (EGFR-specific), IVAX
    Click to Show/Hide
External Link
 Compound Name INdoximod + temozolomide Phase 1 [72]
External Link
 Compound Name Anti-CD133-CAR vector-transduced T cells Phase 1 [87]
External Link
 Compound Name 8H9 Phase 1 [88]
External Link
 Compound Name CC-8490 Phase 1 [89]
External Link
 Compound Name Sitimagene ceradenovec Discontinued in Phase 3 [90]
Synonyms
Cerepro; EG-009; HSV thymidine kinase gene therapy, Ark
    Click to Show/Hide
External Link
 Compound Name Ranagengliotucel-T Discontinued in Phase 3 [91]
Synonyms
Glionix; Brain tumor vaccine, NovaRx; Antisense (TGFbeta) brain tumor vaccine, NovaRx
    Click to Show/Hide
External Link
 Compound Name Oncolysin S Discontinued in Phase 2 [92]
Synonyms
N901-bR
    Click to Show/Hide
External Link
 Compound Name Labradimil Discontinued in Phase 2 [93]
Synonyms
Cereport; Lobradimil; Receptor mediated permeabilizer; RMP 7; DRG-0182; RMP-7; N2-((S)-2-(L-Arginyl-L-prolyl-trans-4-hydroxy-L-prolylglycyl-3-(2-thienyl)-L-alanyl-L-seryl-L-prolinamido)-3-(p-methoxyphenyl)propyl)-L-arginine; (S-(R*,R*))-L-Arginyl-L-prolyl-trans-4-hydroxy-L-prolyl-3-(2-thienyl)-L-alanylglycyl-L-seryl-N-(2-((4-((aminoiminomethyl)amino)-1-carboxybutyl)amino)-1-((4-methoxyphenyl)methyl)ethyl)-L-prolinamide
    Click to Show/Hide
External Link
 Compound Name Brain tumor vaccine Discontinued in Phase 1 [94]
Synonyms
Brain cancer vaccine, IRC; Brain tumor vaccine, IRC; IR-850; Established cancer cell line therapy (brain cancer), IRC; GM-CSF vaccine (brain cancer), IRC
    Click to Show/Hide
External Link
 Compound Name PCNU Terminated [95]
Synonyms
NSC-95466
    Click to Show/Hide
External Link
 Compound Name 131I-81C6 Terminated [96]
Synonyms
Neuradiab; MAb-81C6; Iodine-131-81C6; Astatine-211-MAb-81C6; Iodine-131-MAb-81C6; Iodine-131-ch-81C6; Iodine-131-ch-81C6-F(ab)2; 211At-MAb-81C6
    Click to Show/Hide
External Link
 Compound Name NSD-551 Terminated [97]
Synonyms
BK channel activator (cancer), NeuroSearch/TopoTarget
    Click to Show/Hide
External Link
 Compound Name AGT-2000 Investigative [98]
Synonyms
Gene therapy (intravenous, brain cancer), ArmaGen
    Click to Show/Hide
External Link
 Compound Name NV.XOD.09 Investigative [99]
External Link
 Compound Name EDP-19 Investigative [99]
Synonyms
SiRNA (convection-enhanced delivery, brain tumor), Sheba Medical Center/BioLineRx
    Click to Show/Hide
External Link
 Compound Name MIQ-004 Investigative [99]
Synonyms
M-IQ-004
    Click to Show/Hide
External Link
References
Ref 1 ADAR1 is a new target of METTL3 and plays a pro-oncogenic role in glioblastoma by an editing-independent mechanism. Genome Biol. 2021 Jan 28;22(1):51. doi: 10.1186/s13059-021-02271-9.
Ref 2 Identification of N,1,4,4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a potent, orally available cyclin dependent kinase inhibitor. J Med Chem. 2009 Aug 27;52(16):5152-63. doi: 10.1021/jm9006559.
Ref 3 A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
Ref 4 Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66. doi: 10.1038/nrd2907.
Ref 5 Preclinical metabolism and pharmacokinetics of SB1317 (TG02), a potent CDK/JAK2/FLT3 inhibitor. Drug Metab Lett. 2012 Mar;6(1):33-42. doi: 10.2174/187231212800229336.
Ref 6 ClinicalTrials.gov (NCT04541225) Phase 1/2 Dose Escalation, Safety, Pharmacokinetics, and Efficacy Study of NUV-422 in Adults With Recurrent or Refractory High-grade Gliomas and Solid Tumors. U.S.National Institutes of Health.
Ref 7 AZD5438, an inhibitor of Cdk1, 2, and 9, enhances the radiosensitivity of non-small cell lung carcinoma cells. Int J Radiat Oncol Biol Phys. 2012 Nov 15;84(4):e507-14. doi: 10.1016/j.ijrobp.2012.05.035. Epub 2012 Jul 12.
Ref 8 Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines. Mol Cancer Ther. 2009 Feb;8(2):324-32. doi: 10.1158/1535-7163.MCT-08-0890. Epub 2009 Jan 27.
Ref 9 ClinicalTrials.gov (NCT04553133) PF-07104091 as a Single Agent and in Combination Therapy. U.S. National Institutes of Health.
Ref 10 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 11 A first in man, phase I dose-escalation study of PHA-793887, an inhibitor of multiple cyclin-dependent kinases (CDK2, 1 and 4) reveals unexpected hepatotoxicity in patients with solid tumors. Cell Cycle. 2011 Mar 15;10(6):963-70. doi: 10.4161/cc.10.6.15075. Epub 2011 Mar 15.
Ref 12 Mechanism of action of SNS-032, a novel cyclin-dependent kinase inhibitor, in chronic lymphocytic leukemia. Blood. 2009 May 7;113(19):4637-45. doi: 10.1182/blood-2008-12-190256. Epub 2009 Feb 20.
Ref 13 Clinical pipeline report, company report or official report of Regor Therapeutics
Ref 14 Discovery of 4-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-N-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrazole-3-carboxamide (FN-1501), an FLT3- and CDK-Kinase Inhibitor with Potentially High Efficiency against Acute Myelocytic Leukemia. J Med Chem. 2018 Feb 22;61(4):1499-1518. doi: 10.1021/acs.jmedchem.7b01261. Epub 2018 Feb 12.
Ref 15 Small-molecule multi-targeted kinase inhibitor RGB-286638 triggers P53-dependent and -independent anti-multiple myeloma activity through inhibition of transcriptional CDKs. Leukemia. 2013 Dec;27(12):2366-75. doi: 10.1038/leu.2013.194. Epub 2013 Jun 28.
Ref 16 Cyclin-dependent kinase inhibitors for cancer therapy: a patent review (2009 - 2014). Expert Opin Ther Pat. 2015;25(9):953-70. doi: 10.1517/13543776.2015.1045414. Epub 2015 Jul 13.
Ref 17 c-Jun N-terminal kinase inhibitors: a patent review (2010 - 2014). Expert Opin Ther Pat. 2015;25(8):849-72. doi: 10.1517/13543776.2015.1039984. Epub 2015 May 19.
Ref 18 National Cancer Institute Drug Dictionary (drug id 770319).
Ref 19 What are next generation innovative therapeutic targets? Clues from genetic, structural, physicochemical, and systems profiles of successful targets. J Pharmacol Exp Ther. 2009 Jul;330(1):304-15. doi: 10.1124/jpet.108.149955. Epub 2009 Apr 8.
Ref 20 Pharmacological inhibitors of cyclin-dependent kinases. Trends Pharmacol Sci. 2002 Sep;23(9):417-25. doi: 10.1016/s0165-6147(02)02071-0.
Ref 21 Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases. J Med Chem. 2000 Nov 30;43(24):4606-16. doi: 10.1021/jm000271k.
Ref 22 The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. doi: 10.1093/nar/28.1.235.
Ref 23 Docking-based development of purine-like inhibitors of cyclin-dependent kinase-2. J Med Chem. 2000 Jun 29;43(13):2506-13. doi: 10.1021/jm990506w.
Ref 24 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
Ref 25 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1973).
Ref 26 Discovery of drug mode of action and drug repositioning from transcriptional responses. Proc Natl Acad Sci U S A. 2010 Aug 17;107(33):14621-6. doi: 10.1073/pnas.1000138107. Epub 2010 Aug 2.
Ref 27 Probing the ATP ribose-binding domain of cyclin-dependent kinases 1 and 2 with O(6)-substituted guanine derivatives. J Med Chem. 2002 Aug 1;45(16):3381-93. doi: 10.1021/jm020056z.
Ref 28 5,5'-substituted indirubin-3'-oxime derivatives as potent cyclin-dependent kinase inhibitors with anticancer activity. J Med Chem. 2010 May 13;53(9):3696-706. doi: 10.1021/jm100080z.
Ref 29 4-Alkoxy-2,6-diaminopyrimidine derivatives: inhibitors of cyclin dependent kinases 1 and 2. Bioorg Med Chem Lett. 2003 Jan 20;13(2):217-22. doi: 10.1016/s0960-894x(02)00884-3.
Ref 30 Synthesis and evaluation of N-acyl sulfonamides as potential prodrugs of cyclin-dependent kinase inhibitor JNJ-7706621. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3639-41. doi: 10.1016/j.bmcl.2006.04.071. Epub 2006 May 6.
Ref 31 Discovery and in vitro evaluation of potent TrkA kinase inhibitors: oxindole and aza-oxindoles. Bioorg Med Chem Lett. 2004 Feb 23;14(4):953-7. doi: 10.1016/j.bmcl.2003.12.002.
Ref 32 A robust high-content imaging approach for probing the mechanism of action and phenotypic outcomes of cell-cycle modulators. Mol Cancer Ther. 2011 Feb;10(2):242-54. doi: 10.1158/1535-7163.MCT-10-0720. Epub 2011 Jan 7.
Ref 33 Design, synthesis, and biological evaluation of novel pyrimidine derivatives as CDK2 inhibitors. Eur J Med Chem. 2010 Mar;45(3):1158-66. doi: 10.1016/j.ejmech.2009.12.026. Epub 2009 Dec 21.
Ref 34 5-Arylamino-2-methyl-4,7-dioxobenzothiazoles as inhibitors of cyclin-dependent kinase 4 and cytotoxic agents. Bioorg Med Chem Lett. 2000 Mar 6;10(5):461-4. doi: 10.1016/s0960-894x(00)00014-7.
Ref 35 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. J Med Chem. 2006 Nov 2;49(22):6500-9. doi: 10.1021/jm0605740.
Ref 36 DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Nucleic Acids Res. 2011 Jan;39(Database issue):D1035-41. doi: 10.1093/nar/gkq1126. Epub 2010 Nov 8.
Ref 37 The p16 status of tumor cell lines identifies small molecule inhibitors specific for cyclin-dependent kinase 4. Clin Cancer Res. 1999 Dec;5(12):4279-86.
Ref 38 Identification of binding specificity-determining features in protein families. J Med Chem. 2012 Mar 8;55(5):1926-39.
Ref 39 Meriolins (3-(pyrimidin-4-yl)-7-azaindoles): synthesis, kinase inhibitory activity, cellular effects, and structure of a CDK2/cyclin A/meriolin complex. J Med Chem. 2008 Feb 28;51(4):737-51. doi: 10.1021/jm700940h. Epub 2008 Jan 31.
Ref 40 N-Phenyl-4-pyrazolo[1,5-b]pyridazin-3-ylpyrimidin-2-amines as potent and selective inhibitors of glycogen synthase kinase 3 with good cellular efficacy. J Med Chem. 2004 Sep 9;47(19):4716-30. doi: 10.1021/jm040063i.
Ref 41 The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315. doi: 10.1042/BJ20070797.
Ref 42 1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities. J Med Chem. 2005 Jun 30;48(13):4208-11. doi: 10.1021/jm050267e.
Ref 43 Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors. J Med Chem. 2003 May 22;46(11):2027-30. doi: 10.1021/jm0256169.
Ref 44 A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. Proc Natl Acad Sci U S A. 2007 Dec 18;104(51):20523-8. doi: 10.1073/pnas.0708800104. Epub 2007 Dec 11.
Ref 45 Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors. Bioorg Med Chem Lett. 2008 Dec 15;18(24):6486-9. doi: 10.1016/j.bmcl.2008.10.075. Epub 2008 Oct 22.
Ref 46 Aminopyridine-based c-Jun N-terminal kinase inhibitors with cellular activity and minimal cross-kinase activity. J Med Chem. 2006 Jun 15;49(12):3563-80. doi: 10.1021/jm060199b.
Ref 47 Dissecting the determinants of cyclin-dependent kinase 2 and cyclin-dependent kinase 4 inhibitor selectivity. J Med Chem. 2006 Sep 7;49(18):5470-7. doi: 10.1021/jm060216x.
Ref 48 Cellular characterization of a novel focal adhesion kinase inhibitor. J Biol Chem. 2007 May 18;282(20):14845-52. doi: 10.1074/jbc.M606695200. Epub 2007 Mar 28.
Ref 49 Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects. J Med Chem. 2003 Jan 16;46(2):222-36. doi: 10.1021/jm020319p.
Ref 50 Potentiation of paclitaxel-induced apoptosis by the novel cyclin-dependent kinase inhibitor NU6140: a possible role for survivin down-regulation. Mol Cancer Ther. 2005 Sep;4(9):1328-37. doi: 10.1158/1535-7163.MCT-05-0022.
Ref 51 Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J Biol Chem. 2005 May 20;280(20):19867-74. doi: 10.1074/jbc.M501367200. Epub 2005 Mar 16.
Ref 52 First Cdc7 kinase inhibitors: pyrrolopyridinones as potent and orally active antitumor agents. 2. Lead discovery. J Med Chem. 2009 Jan 22;52(2):293-307. doi: 10.1021/jm800977q.
Ref 53 Design, synthesis, and biological evaluation of 3,4-diarylmaleimides as angiogenesis inhibitors. J Med Chem. 2006 Feb 23;49(4):1271-81. doi: 10.1021/jm0580297.
Ref 54 Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. J Med Chem. 2005 Sep 8;48(18):5639-43. doi: 10.1021/jm050392q.
Ref 55 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 56 Photodynamic therapy: applications in atherosclerotic vascular disease with motexafin lutetium. Catheter Cardiovasc Interv. 2002 Nov;57(3):387-94.
Ref 57 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7214).
Ref 58 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6800).
Ref 59 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6505).
Ref 60 Therapeutic injection of PARP inhibitor INO-1001 preserves cardiac function in porcine myocardial ischemia and reperfusion without reducing infarct size. Shock. 2010 May;33(5):507-12.
Ref 61 ClinicalTrials.gov (NCT01436968) Phase 3 Study of ProstAtak Immunotherapy With Standard Radiation Therapy for Localized Prostate Cancer. U.S. National Institutes of Health.
Ref 62 ClinicalTrials.gov (NCT00088400) Comparison of TransMID vs Standard Treatment of Cancerous Brain Tumors. U.S. National Institutes of Health.
Ref 63 ClinicalTrials.gov (NCT01280552) A Study of ICT-107 Immunotherapy in Glioblastoma Multiforme (GBM). U.S. National Institutes of Health.
Ref 64 ClinicalTrials.gov (NCT00076986) The PRECISE Trial: Study of IL13-PE38QQR Compared to GLIADEL Wafer in Patients With Recurrent Glioblastoma Multiforme. U.S. National Institutes of Health.
Ref 65 ClinicalTrials.gov (NCT01480479) Phase III Study of Rindopepimut/GM-CSF in Patients With Newly Diagnosed Glioblastoma. U.S. National Institutes of Health.
Ref 66 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 67 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017222)
Ref 68 ClinicalTrials.gov (NCT05685004) Randomized Phase 2b Study of Safety And Efficacy Of TVI-Brain-1 Combined With Conformal Radiotherapy And Temozolomide Vs Standard Therapy In Newly Diagnosed MGMT Negative Glioblastoma Multiforme (GBM). U.S.National Institutes of Health.
Ref 69 ClinicalTrials.gov (NCT05163080) Prospective Randomized Placebo-Controlled Trial of SurVaxM Plus Adjuvant Temozolomide for Newly Diagnosed Glioblastoma (SURVIVE). U.S.National Institutes of Health.
Ref 70 ClinicalTrials.gov (NCT01472731) Safety and Imaging Study of GC1008 in Glioma. U.S. National Institutes of Health.
Ref 71 ClinicalTrials.gov (NCT02798406) Combination Adenovirus + Pembrolizumab to Trigger Immune Virus Effects (CAPTIVE). U.S. National Institutes of Health.
Ref 72 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 73 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800037619)
Ref 74 Hypoxia-inducible factor 2: a novel target in gliomas.Future Med Chem. 2018 Sep 1;10(18):2227-2236.
Ref 75 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 76 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800034046)
Ref 77 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029242)
Ref 78 ClinicalTrials.gov (NCT00062283) Alanosine in Treating Patients With Cancer. U.S. National Institutes of Health.
Ref 79 ClinicalTrials.gov (NCT01454596) CAR T Cell Receptor Immunotherapy Targeting EGFRvIII for Patients With Malignant Gliomas Expressing EGFRvIII. U.S. National Institutes of Health.
Ref 80 Clinical pipeline report, company report or official report of Roche
Ref 81 ClinicalTrials.gov (NCT05460507) A Single Arm Open Label Study to Determine the Safety and Efficacy/Tolerability of Rhenium-186 NanoLiposomes (186RNL) for Recurrence of Glioma in Patients Who Received a Prior Treatment With 186RNL. U.S.National Institutes of Health.
Ref 82 ClinicalTrials.gov (NCT04485949) A Randomized, Multicenter, Double-Blind, Placebo-Controlled, Phase 2b Study to Assess the Safety and Efficacy of IGV-001, an Autologous Cell Immunotherapy With Antisense Oligonucleotide (IMV-001) Targeting IGF-1R, in Newly Diagnosed Patients With Glioblastoma. U.S.National Institutes of Health.
Ref 83 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026657)
Ref 84 Identification of an immunogenic CD8+ T-cell epitope derived from gamma-globin, a putative tumor-associated antigen for juvenile myelomonocytic leu... Blood. 2006 Oct 15;108(8):2662-8.
Ref 85 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800041844)
Ref 86 ClinicalTrials.gov (NCT01009866) Study of Immunotoxin, MR1-1. U.S. National Institutes of Health.
Ref 87 ClinicalTrials.gov (NCT02541370) Treatment of Relapsed and/or Chemotherapy Refractory Advanced Malignancies by CART133
Ref 88 ClinicalTrials.gov (NCT01502917) Convection-Enhanced Delivery of 124I-8H9 for Patients With Non-Progressive Diffuse Pontine Gliomas Previously Treated With External Beam Radiation Therapy. U.S. National Institutes of Health.
Ref 89 ClinicalTrials.gov (NCT00074646) Phase I Trial of CC-8490 for the Treatment of Subjects With Recurrent/Refractory High-Grade Gliomas. U.S. National Institutes of Health.
Ref 90 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015264)
Ref 91 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017210)
Ref 92 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006625)
Ref 93 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 672).
Ref 94 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007949)
Ref 95 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000870)
Ref 96 Human IgG2 constant region enhances in vivo stability of anti-tenascin antibody 81C6 compared with its murine parent. Clin Cancer Res. 1998 Oct;4(10):2495-502.
Ref 97 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019960)
Ref 98 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1797).
Ref 99 The ChEMBL database in 2017. Nucleic Acids Res. 2017 Jan 4;45(D1):D945-D954.