Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
Crosstalk ID
M6ACROT03086
[1]
Histone modification H3K18la p300 FTO Direct Enhancement m6A modification CDK2 CDK2 FTO Demethylation : m6A sites
m6A Modification:
m6A Regulator Fat mass and obesity-associated protein (FTO) ERASER
m6A Target Cyclin-dependent kinase 2 (CDK2)
Epigenetic Regulation that have Cross-talk with This m6A Modification:
Epigenetic Regulation Type Histone modification (HistMod)
Epigenetic Regulator Histone acetyltransferase p300 (P300) WRITER View Details
Regulated Target Histone H3 lysine 18 lactylation (H3K18la) View Details
Downstream Gene FTO View Details
Crosstalk Relationship Histone modification  →  m6A Enhancement
Crosstalk Mechanism histone modification directly impacts m6A modification through modulating the level of m6A regulator
Crosstalk Summary FTO affected EC features via modulating Cyclin-dependent kinase 2 (CDK2) mRNA stability in an m6A-YTHDF2-dependent manner. FTO up-regulation under diabetic conditions was driven by p300-mediated Histone H3 lysine 18 lactylation (H3K18la). FB23-2, an inhibitor to FTO's m6A demethylase activity, suppressed angiogenic phenotypes in vitro.
Responsed Disease Diabetic retinopathy ICD-11: 9B71.0
Responsed Drug FB23-2
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
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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
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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
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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
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MOA Inhibitor
Activity IC50 = 170 nM
External Link
 Compound Name Palbociclib/ribociclib analog 1 Patented [16]
Synonyms
PMID26161698-Compound-4
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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
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MOA Inhibitor
Activity IC50 = 45 nM
External Link
 Compound Name N-phenyl-pyrimidin-4-amine derivative 1 Patented [16]
Synonyms
PMID26161698-Compound-30
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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
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MOA Inhibitor
Activity IC50 = 2 to 6 nM
External Link
 Compound Name Flavopiridol analog 1 Patented [16]
Synonyms
PMID26161698-Compound-5
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MOA Inhibitor
Activity IC50 = nM range
External Link
 Compound Name Isosteric imidazolyl pyrimidine derivative 1 Patented [16]
Synonyms
PMID26161698-Compound-37
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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
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MOA Inhibitor
Activity IC50 < 1 nM
External Link
 Compound Name Naphthyridine and isoquinoline derivative 1 Patented [16]
Synonyms
PMID26161698-Compound-51
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MOA Inhibitor
Activity IC50 = 40 nM
External Link
 Compound Name Nitrogen mustard derivative 1 Patented [16]
Synonyms
PMID26161698-Compound-55
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MOA Inhibitor
Activity IC50 = 2.7 nM
External Link
 Compound Name 4-(thiazol-5-yl)-pyrimidine derivative 2 Patented [16]
Synonyms
PMID26161698-Compound-36
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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
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MOA Inhibitor
Activity IC50 = 12 nM
External Link
 Compound Name Isoquinoline 1,3-dione derivative 1 Patented [16]
Synonyms
PMID26161698-Compound-49
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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
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MOA Inhibitor
Activity IC50 < 100 nM
External Link
 Compound Name SCH 727965 Discontinued in Phase 3 [4]
Synonyms
Dinaciclib; SCH-727965
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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
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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
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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
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MOA Inhibitor
External Link
 Compound Name INOC-005 Preclinical [19]
Synonyms
Capridine beta (prostate cancer), Prostagenics
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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
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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
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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
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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
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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
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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)-
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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
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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
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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
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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
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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-
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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)-
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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
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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
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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
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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,
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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
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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
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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
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MOA Inhibitor
Activity Ki = 396 nM
External Link
 Compound Name VER-54505 Investigative [25]
Synonyms
Cdk2 inhibitors, Vernalis; RBT-0049985
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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MOA Inhibitor
External Link
 Compound Name MERIOLIN 8 Investigative [39]
Synonyms
SCHEMBL2991886; CHEMBL406102
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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
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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
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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
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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
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MOA Inhibitor
External Link
 Compound Name MERIOLIN 4 Investigative [39]
Synonyms
SCHEMBL3001373; CHEMBL406464
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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
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MOA Inhibitor
External Link
 Compound Name MERIOLIN 6 Investigative [39]
Synonyms
CHEMBL406463; SCHEMBL2999009
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MOA Inhibitor
External Link
 Compound Name K00024 Investigative [43]
Synonyms
indolocarbazole deriv. 4(d)
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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
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MOA Inhibitor
External Link
 Compound Name aminopurvalanol A Investigative [44]
Synonyms
NG-97
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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
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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
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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
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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
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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
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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
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MOA Inhibitor
External Link
 Compound Name PMID18986805C9b Investigative [45]
Synonyms
GTPL8160; BDBM50246396; ZINC38224644
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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
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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
Histone acetyltransferase p300 (P300) 2 Compound(s) Regulating the Target Click to Show/Hide the Full List
 Compound Name CCS1477 Phase 1/2 [55]
Synonyms
CCS-1477; CBP-IN-1; 2222941-37-7; (S)-1-(3,4-Difluorophenyl)-6-(5-(3,5-dimethylisoxazol-4-yl)-1-((1r,4S)-4-methoxycyclohexyl)-1H-benzo[d]imidazol-2-yl)piperidin-2-one; SCHEMBL20094038; SCHEMBL21515367; SCHEMBL22134021; EX-A3687; NSC818619; NSC-818619; HY-111784; CS-0091862; (S)-1-(3,4-Difluorophenyl)-6-(5-(3,5-dimethylisoxazol-4-yl)-1-(trans-4-methoxycyclohexyl)-1H-benzo[d]imidazol-2-yl)piperidin-2-one
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name FT-7051 Phase 1 [56]
MOA Inhibitor
External Link
9B71: Retinopathy 12 Compound(s) Regulating the Disease Click to Show/Hide the Full List
 Compound Name SHP607 Phase 2 [57]
External Link
 Compound Name RST-001 Phase 1/2 [58]
Synonyms
ChR2 gene therapy (retinopathy), RetroSense; AAV-based ChR2 gene therapy (retinopathy), RetroSense; Channelrhodopsin-2 gene therapy (retinopathy), RetroSense
    Click to Show/Hide
External Link
 Compound Name ReN-003 Phase 1/2 [59]
Synonyms
Stem cell therapy (retinal diseases), ReNeuron
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External Link
 Compound Name PMID28621580-Compound-WO2015089220C70 Patented [60]
External Link
 Compound Name SIR-1076 Preclinical [61]
Synonyms
Antioxidants (topical, retinal oxidative stress), Sirion Therapeutics
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External Link
 Compound Name CytoRet Investigative [59]
Synonyms
Retinal cell therapy (retinal disease), International Stem Cell; Retinal layers (parthenogenetic stem-cell derived), ISCO
    Click to Show/Hide
External Link
 Compound Name LPO-1010CSR Investigative [59]
External Link
 Compound Name INDUS-815C Investigative [62]
Synonyms
VEGF modulator (age related macular degeneration/retinopathy), Indus Biotech; INDUS-815C (Huntington's disease), Indus Biotech; INDUS-815C (age related macular degeneration/retinopathy), Indus Biotech; SIRT2 inhibtior (Parkinson's disease/dementia/Huntington's disease), Indus Biotech; NAD-dependent deacetylase sirtuin-2inhibitor (Parkinson's disease/dementia/Huntington's disease), Indus Biotech
    Click to Show/Hide
External Link
 Compound Name SF-113 Investigative [59]
External Link
 Compound Name SF-106 Investigative [59]
External Link
 Compound Name Gene therapy, retinopathy, Investigative [59]
Synonyms
Gene therapy (retinopathy)
    Click to Show/Hide
External Link
 Compound Name Superoxide dismutase mimetics Investigative [59]
Synonyms
INO-6001; INO-6002; Superoxide dismutase mimetics (retinal disease); Superoxide dismutase mimetics (retinal disease), Inotek; Superoxide dismutase mimetics (age-related macular degeneration/diabetic retinopathy/diabetic macular edema), Inotek
    Click to Show/Hide
External Link
References
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Ref 58 ClinicalTrials.gov (NCT02556736) RST-001 Phase I/II Trial for Retinitis Pigmentosa.
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Ref 62 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: 2708).