Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
Crosstalk ID
M6ACROT02163
[1], [2]
DNA methylation DNMT3B METTL3 Direct Inhibition m6A modification AKT1 AKT1 METTL3 Methylation : m6A sites
m6A Modification:
m6A Regulator Methyltransferase-like 3 (METTL3) WRITER
m6A Target RAC-alpha serine/threonine-protein kinase (AKT1)
Epigenetic Regulation that have Cross-talk with This m6A Modification:
Epigenetic Regulation Type DNA methylation (DNAMeth)
Epigenetic Regulator DNA (cytosine-5)-methyltransferase 3B (DNMT3B) WRITER View Details
Regulated Target Methyltransferase-like protein 3 (METTL3) View Details
Crosstalk Relationship DNA methylation  →  m6A Inhibition
Crosstalk Mechanism DNA methylation directly impacts m6A modification through modulating the expression level of m6A regulator
Crosstalk Summary Methyltransferase-like 3 (METTL3) increased the pri-Let-7b, decreased both the pre-Let-7b and mature Let-7b, attenuating the Let-7b controlling of stem cell renewal. The addition of Metformin increased the bindings of DNA methyltransferase-3a/b (DNMT3A/DNMT3B) to the METTL3 promoter. With the help of the readers of NKAP and HNRNPA2B1, the cluster mediated m6A formation on pri-Let-7b processing increased the mature Let-7b, the key player in suppressing Notch signaling and re-captivating Osimertinib treatment. METTL3-mediated m6A methylation promotes lung cancer progression via activating PI3K/RAC-alpha serine/threonine-protein kinase (AKT1)/mTOR pathway.
Responsed Disease Lung cancer ICD-11: 2C25
Responsed Drug Metformin
Pathway Response mTOR signaling pathway hsa04150
PI3K-Akt signaling pathway hsa04151
In-vitro Model
NCI-H1975 Lung adenocarcinoma Homo sapiens CVCL_1511
HCC827 Lung adenocarcinoma Homo sapiens CVCL_2063
In-vivo Model 5 × 106 A549 cells overexpressing METTL3 (Lv-METTL3) or control (Lv-Ctrl) were suspended in 100 uL phosphate-buffered saline (PBS), and were subcutaneously injected into mouse lower right flank. Drug treatment started in the Lv-METTL3 group when the tumour volume reached around 100 mm3. Mice were randomly divided into three groups to receive vehicle, GSK2536771 (30 mg/kg) or rapamycin (1 mg/kg). Drugs were administrated daily through intraperitoneal injection for 18 days. Treatment conditions were chosen as previously reported.
Full List of Potential Compound(s) Related to This m6A-centered Crosstalk
DNA (cytosine-5)-methyltransferase 3B (DNMT3B) 22 Compound(s) Regulating the Target Click to Show/Hide the Full List
 Compound Name Curcumin Phase 3 [3]
Synonyms
458-37-7; Diferuloylmethane; Natural yellow 3; Turmeric yellow; Turmeric; Curcuma; Kacha haldi; Gelbwurz; Indian saffron; Curcumin I; Souchet; Halud; Halad; Haidr; Haldar; Merita earth; Yellow Ginger; Terra Merita; Yellow Root; Safran d'Inde; Yo-Kin; Golden seal; Curcuma oil; Orange Root; Oils, curcuma; CI Natural Yellow 3; Curcumine; Hydrastis; Indian turmeric; Yellow puccoon; Turmeric extract; Diferaloylmethane; Kurkumin [Czech]; (1E,6E)-1,7-Bis(4-hydroxy-3-methoxyphenyl)hepta-1,6-diene-3,5-dione; Tumeric yellow; Turmeric oil
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name PMID27376512-Compound-MTC-424 Patented [4]
MOA Inhibitor
Activity IC50 = 1940 nM
External Link
 Compound Name PMID27376512-Compound-MTC-427 Patented [4]
MOA Inhibitor
Activity IC50 = 295 nM
External Link
 Compound Name PMID27376512-Compound-MTC-422 Patented [4]
MOA Inhibitor
Activity IC50 = 1430 nM
External Link
 Compound Name PMID27376512-Compound-MTC-423 Patented [4]
MOA Inhibitor
Activity IC50 = 363 nM
External Link
 Compound Name NSC-622444 Investigative [3]
Synonyms
NSC622444; CHEMBL116347; AC1Q3LXD; AC1L7GK5; SCHEMBL9755151; dichlorinated diacylmethane fragment; ZINC1616868; BDBM50048522; 5,3'-dicarboxy-4,4'-dihydrodiphenylmethane; 5,5''-methylenebis(3-chloro-2-hydroxybenzoic acid); 5,5'-Methylenebis(3-chloro-2-hydroxybenzoic acid); 3,3'-methanediylbis(5-chloro-6-hydroxybenzoic acid); 5-(3-carboxy-5-chloro-4-hydroxybenzyl)-3-chloro-2-hydroxybenzoic acid; 3',3-Dichloro-4',4-dimethoxy-5',5-bis(methoxycarbonyl)-1,1-diphenylmethane
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name NSC-138419 Investigative [3]
Synonyms
NSC138419; n-[4-(methylamino)benzoyl]glutamic acid; AC1Q5SG8; AC1L5YW4; SCHEMBL5925511; CHEMBL591443; CTK1H0013; 2-[(4-methylaminobenzoyl)amino]pentanedioic acid; A816490; 2-[[4-(methylamino)benzoyl]amino]pentanedioic acid; 2-[[4-(methylamino)phenyl]carbonylamino]pentanedioic acid; 2-[[[4-(methylamino)phenyl]-oxomethyl]amino]pentanedioic acid
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name NSC-319745 Investigative [3]
Synonyms
61629-60-5; HB 093; BRN 2168571; 4-(2-((5-Chloro-2-methoxybenzoyl)amino)ethyl)hydrocinnamic acid; 3-[4-[2-[(5-CHLORO-2-METHOXY-BENZOYL)AMINO]ETHYL]PHENYL]PROPANOIC ACID; 3-(4-(2-(5-Chlor-2-methoxy-benzamido)-aethyl)phenyl)-propionsaeure [German]; 3-[4-[2-[(5-chloro-2-methoxybenzoyl)amino]ethyl]phenyl]propanoic acid; HYDROCINNAMIC ACID, 4-(2-((5-CHLORO-2-METHOXYBENZOYL)AMINO)ETHYL)-; AC1L2AFL; CHEMBL597112; SCHEMBL11481071; CTK5B3505; DTXSID00210642; AIEFQKOARQRACO-UHFFFAOYSA-N; ZINC1572211; HB-093; NSC319745
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name NSC-348926 Investigative [3]
Synonyms
NSC348926; 2-phthalimidoadipic acid; AC1L7IP1; SCHEMBL9741723; CHEMBL599367; 2-(1,3-dioxoisoindol-2-yl)hexanedioic acid
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name NSC-401077 Investigative [3]
Synonyms
NSC401077; MLS000757170; DNA Methyltransferase Inhibitor; CHEMBL383475; 32675-71-1; 2-(1,3-Dioxo-1,3-dihydro-isoindol-2-yl)-3-(1H-indol-3-yl)-propionic acid; 2-(1,3-dioxo-2,3-dihydro-1H-isoindol-2-yl)-3-(1H-indol-3-yl)propanoic acid; 2-(1,3-Dioxo-1,3-dihydro-2H-isoindol-2-yl)-3-(1H-indol-3-yl)propanoic acid; 2-(1,3-Dioxo-1,3-dihydro-2H-isoindol-2-yl)-3-(1H-indol-3-yl)propionic acid; SMR000413613; AC1Q71QA; Oprea1_475901; Oprea1_410805; MLS000777218; MLS006011919; SCHEMBL562060
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name S-tubercidinylhomocysteine Investigative [5]
Synonyms
CHEMBL552309; 57344-98-6; AC1L3YAS; AC1Q5QMO; (S)-7-(5-S-(3-amino-3-carboxypropyl)-5-thio-beta-D-ribofuranosyl)-7H-pyrrolo(2,3-d)pyrimidin-4-amine; (2s)-2-amino-4-({[(2s,3s,4r,5r)-5-(4-amino-7h-pyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydroxytetrahydrofuran-2-yl]methyl}sulfanyl)butanoic acid(non-preferred name); BDBM50294482; (2S)-2-amino-4-[[(2S,3S,4R,5R)-5-(4-aminopyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]butanoic acid
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 300 nM
External Link
 Compound Name NSC-106084 Investigative [3]
Synonyms
CHEMBL597113; NSC106084; AC1L6H8Q; CTK7J5419; ZINC1868549; BDBM50308983; {4-[5-bromo-2-(carboxymethoxy)benzoyl]phenoxy}acetic acid; 2-(4-bromo-2-(4-(carboxymethoxy)benzoyl)phenoxy)acetic acid; 2-[4-[5-bromo-2-(carboxymethyloxy)benzoyl]phenoxy]acetic acid
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name NSC-154957 Investigative [3]
Synonyms
NSC154957; AC1L6EF2; CHEMBL586418; 3-benzhydrylsulfanyl-2-formamidopropanoic acid
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name NSC-54162 Investigative [3]
Synonyms
NSC54162; AC1Q5WTA; AC1L6CM2; CHEMBL611994; 2,2'-{[(2-hydroxyphenyl)methanediyl]disulfanediyl}diacetic acid; ZINC1685025; Acetic acid, (salicylidenedithio)di-; 4265-51-4; Acetic acid, [(o-hydroxybenzylidene)dithio]di-; Acetic acid,2'-[[(2-hydroxyphenyl)methylene]bis(thio)]bis-; 2-[carboxymethylsulfanyl-(2-hydroxyphenyl)methyl]sulfanylacetic acid
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name NSC-57893 Investigative [3]
Synonyms
MLS002667915; 7399-94-2; 4-[(1h-benzimidazol-2-ylmethyl)(formyl)amino]benzoic acid; NSC57893; AC1L6GFK; AC1Q5TWY; NCIOpen2_002368; CHEMBL599366; 4-[1H-benzimidazol-2-ylmethyl(formyl)amino]benzoic acid; CTK5D9099; DTXSID30288854; HMS3089M13; ZINC1688755; AKOS030547711
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name NSC-56071 Investigative [3]
Synonyms
32230-52-7; NSC56071; AC1L6EJV; AC1Q7ES0; NCIOpen2_007380; CHEMBL596910; CTK4G8394; DTXSID80288485; ZINC1686711; 2,2'-[piperazine-1,4-diylbis(carbonothioylsulfanediyl)]diacetic acid; AKOS030574801; Acetic acid,2,2'-[1,4-piperazinediylbis(carbonothioylthio)]bis- (9CI); 2-[4-(carboxymethylsulfanylcarbothioyl)piperazine-1-carbothioyl]sulfanylacetic acid
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name NSC-137546 Investigative [3]
Synonyms
NSC137546; CHEMBL591202; AC1L5Y49; AKOS008984447; 2-[(2,6-dichlorobenzoyl)amino]pentanedioic acid
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name NSC-623548 Investigative [3]
Synonyms
2581-36-4; NSC 408488; o-Cresotic acid, 5,5'-methylenedi-; 2,3-CRESOTIC ACID, 5,5'-METHYLENEDI-; UNII-S3D8KC88KC; 5,5'-Methylenedi-2,3-cresotic acid; NSC 623548; BRN 3433298; S3D8KC88KC; CHEMBL113835; 5,5'-Methylenedi-o-cresotic acid; NSC623548; NSC408488; 5,5'-Methylenebis(2-hydroxy-3-methylbenzoic acid); 2, 5,5'-methylenedi-; AC1L29YK; Oprea1_231968; 2-10-00-00398 (Beilstein Handbook Reference); SCHEMBL9755153; CTK4F6504; DTXSID90180466; o-Cresotic acid,5'-methylenedi-; MolPort-000-698-522; ZINC4028795; STL511095
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name NSC-345763 Investigative [3]
Synonyms
7-(8-hydroxyquinolin-5-yl)-4,7-dioxoheptanoic acid; NSC345763; AC1L7HSU; CHEMBL597114
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name NSC-158324 Investigative [3]
Synonyms
Acediasulfone; UNII-30YP2YHH8W; 30YP2YHH8W; CHEMBL48396; N-[4-[(4-AMINOPHENYL)SULPHONYL]PHENYL]GLYCINE; 2-[4-(4-aminophenyl)sulfonylanilino]acetic acid; Acediasulfonum; N-(4-((4-Aminophenyl)sulphonyl)phenyl)glycine; EINECS 201-243-7; AC1L25EF; ZINC862; SCHEMBL143660; CTK5E7379; DTXSID00229991; CHEBI:135300; BDBM50099670; AKOS027327086; DB08926; Glycine,N-[4-[(4-aminophenyl)sulfonyl]phenyl]-; {4-[(4-aminophenyl)sulfonyl]anilino}acetic acid; 2-(4-(4-aminophenylsulfonyl)phenylamino)acetic acid
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name (L-)-S-adenosyl-L-homocysteine Investigative [6]
Synonyms
S-Adenosyl-L-homocysteine; S-adenosylhomocysteine; 979-92-0; AdoHcy; S-(5'-adenosyl)-L-homocysteine; adenosylhomocysteine; Formycinylhomocysteine; Adenosyl-L-homocysteine; S-(5'-deoxyadenosin-5'-yl)-L-homocysteine; 2-S-adenosyl-L-homocysteine; 5'-Deoxy-S-adenosyl-L-homocysteine; S-adenosyl-homocysteine; S-Adenosyl Homocysteine; L-S-Adenosylhomocysteine; L-Homocysteine, S-(5'-deoxyadenosin-5'-yl)-; adenosylhomo-cys; adenosyl-homo-cys; UNII-8K31Q2S66S; (S)-5'-(S)-(3-Amino-3-carboxypropyl)-5'-thioadenosine; BRN 5166233; SAH
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 200 nM
External Link
 Compound Name NSC-622445 Investigative [3]
Synonyms
5,5'-Methylenedisalicylic acid; 122-25-8; 5,5'-Methylenebis(2-hydroxybenzoic acid); Methylenebis(salicylic acid); 5,5-Methylenebis(salicylic acid); UNII-2KF4FVV76N; 5,5-Methylenedisalicylic acid; 5-(3-Carboxy-4-hydroxybenzyl)salicylic acid; 4,4'-Dihydroxy-3,3'-dicarboxydiphenylmethane; 3,3'-Dicarboxy-4,4'-dihydroxydiphenylmethane; NSC 14778; 2KF4FVV76N; 4,4'-Dihydroxydiphenylmethane-3,3'-dicarboxylic acid; 3,3'-Methylenebis(6-hydroxybenzoic acid); CHEMBL115145; Benzoic acid, 3,3'-methylenebis[6-hydroxy-
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 17000 nM
External Link
RAC-alpha serine/threonine-protein kinase (AKT1) 40 Compound(s) Regulating the Target Click to Show/Hide the Full List
 Compound Name Capivasertib Approved [7]
Synonyms
1143532-39-1; AZD-5363; capivasertib; AZD 5363; UNII-WFR23M21IE; WFR23M21IE; cc-638; 4-Amino-N-[(1s)-1-(4-Chlorophenyl)-3-Hydroxypropyl]-1-(7h-Pyrrolo[2,3-D]pyrimidin-4-Yl)piperidine-4-Carboxamide; C21H25ClN6O2; (S)-4-AMINO-N-(1-(4-CHLOROPHENYL)-3-HYDROXYPROPYL)-1-(7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)PIPERIDINE-4-CARBOXAMIDE; 4-Amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-4-piperidinecarboxamide; 4-Piperidinecarboxamide, 4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 3 nM
External Link
 Compound Name GDC-0068 Phase 3 [8]
Synonyms
RG7440
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 157 nM
External Link
 Compound Name Enzastaurin Phase 3 [8]
Synonyms
LY317615; LE-0014; LY317615, Enzastaurin; 3-(1-methyl-1H-indol-3-yl)-4-{1-[1-(pyridin-2-ylmethyl)piperidin-4-yl]-1H-indol-3-yl}-1H-pyrrole-2,5-dione; 3-(1-methylindol-3-yl)-4-[1-[1-(pyridin-2-ylmethyl)piperidin-4-yl]indol-3-yl]pyrrole-2,5-dione
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name GSK2110183 Phase 2 [9]
MOA Modulator
External Link
 Compound Name RX-0201 Phase 2 [10]
MOA Inhibitor
External Link
 Compound Name Trametinib + 2141795 Phase 2 [9]
MOA Modulator
External Link
 Compound Name PTX-200 Phase 2 [8]
Synonyms
Plant-derived antiparkinsonian, Phytrix
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name CMX-2043 Phase 2 [11]
MOA Modulator
External Link
 Compound Name ARQ 092 Phase 2 [12]
Synonyms
Miransertib
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name CI-1033 Phase 2 [13]
Synonyms
Canertinib; Canertinib HCl; Canertinib dihydrochloride; Canertinib dihydrochloride [USAN]; CI1033; PD 183805; Canertinib dihydrochloride (USAN); PD-0183805; PD-183805; Canertinib, PD-183805, CI1033, PD183805; N-[4-(3-Chloro-4-fluorophenylamino)-7-(3-morpholin-4-ylpropoxy)quinazolin-6-yl]acrylamide dihydrochloride; N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[3-(4-morpholinyl)propoxy]-6-quinazolinyl]-2-propenamide dihydrochloride; N-[4-(3-chloro-4-fluoroanilino)-7-(3-morpholin-4-ylpropoxy)quinazolin-6-yl]prop-2-enamide; N-[4-(3-chloro-4-fluoroanilino)-7-(3-morpholin-4-ylpropoxy)quinazolin-6-yl]prop-2-enamide dihydrochloride; N-(4-(3-chloro-4-fluorophenyl)amino)-7-(3-morpholin-4-yl)propoxy)quinazolin-6-yl)prop-2-enamide dihydrochloride; N-{4-[(3-chloro-4-fluorophenyl)amino]-7-[3-(morpholin-4-yl)propoxy]quinazolin-6-yl}prop-2-enamide; N-(4-((3-Chloro-4-fluorophenyl)amino)-7-(3-(morpholin-4-yl)propoxy)quinazolin-6-yl)prop-2-enamide; 2-Propenamide, N-(4-((3-chloro-4-fluorophenyl) amino)-7-(3-(4-morpholinyl) propoxy)-6-quinazolinyl)-, dihydrochloride; 2-Propenamide, N-(4-((3-chloro-4-fluorophenyl)amino)-7-(3-(4-morpholinyl)propoxy)-6-quinazolinyl)-, dihydrochloride
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Triciribine prodrug Phase 1/2 [9]
Synonyms
TSR-826; Triciribine prodrug (oral, cancer); Triciribine prodrug (oral, cancer), TSRL
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name BMS-754807 Phase 1 [14]
Synonyms
1001350-96-4; BMS 754807; BMS754807; UNII-W9E3353E8J; CHEMBL575448; CHEBI:88339; W9E3353E8J; 1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl}-N-(6-fluoropyridin-3-yl)-2-methyl-L-prolinamide; W-204348; J-501009; 2-Pyrrolidinecarboxamide, 1-[4-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]-N-(6-fluoro-3-pyridinyl)-2-methyl-, (2S)-;2-Pyrrolidinecarboxamide, 1-[4-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]-N-(6-fluoro-3-pyridin
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name ARQ 751 Phase 1 [8]
MOA Inhibitor
External Link
 Compound Name M2698 Phase 1 [8]
Synonyms
HXAUJHZZPCBFPN-QGZVFWFLSA-N; 1379545-95-5; SCHEMBL15262358; EX-A1187; AKOS030627134; M2698(MSC-2363318A)
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name PMID28460551-Compound-6 Patented [15]
MOA Inhibitor
External Link
 Compound Name Squalestatin 1 Terminated [16]
Synonyms
Zaragozic acid A; Squalestatin; 142561-96-4; ZARAGOZIC ACIDS A; UNII-1117HVX02L; CHEMBL280978; CHEBI:75170; 1117HVX02L; 1S-((4S-acetoxy-5R-methyl-3-methylene-6-phenylhexyl)-6-(E)-4S,6S-dimethyloct-2-enoyloxy)-4,7S-dihydroxy-2,8-dioxabicyclo[321]octane-3S,4S,5R-tricarboxylic acid; L-erythro-L-glycero-D-altro-7-Trideculo-7,4-furanosonic acid, 2,7-anhydro-3,4-di-C-carboxy-8,9,10,12,13-pentadeoxy-10-methylene-12-(phenylmethyl)-, 11-acetate 5-(4,6-dimethyl-2-octenoate), (5(2E,4S,6S),7S)-; Squalestatin 1, Glaxo; Zaragozic acid A, Glaxo
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name MYRIOCIN Investigative [16]
Synonyms
thermozymocidin; 35891-70-4; ISP-I; ISP-1; UNII-YRM4E8R9ST; (2S,3R,4R,6E)-2-Amino-3,4-dihydroxy-2-(hydroxymethyl)-14-oxo-6-eicosenoic acid; YRM4E8R9ST; Myriocin, Mycelia sterilia; Myriocin from Mycelia sterilia; CHEBI:582124; NCGC00163597-02; NCGC00163597-03; DSSTox_CID_26360; DSSTox_RID_81561; (2S,3R,4R,6E)-2-amino-3,4-dihydroxy-2-(hydroxymethyl)-14-oxoicos-6-enoic acid; DSSTox_GSID_46360; [2S,3R,4R]-(E)-2-Amino-3,4-dihydroxy-2-[hydroxymethyl]-14-oxo-6-eicosenoic Acid
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name LD-101 Investigative [9]
Synonyms
AKT-SI-1
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name A-674563 Investigative [17]
Synonyms
A 674563; A674563
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 11 nM
External Link
 Compound Name Lactoquinomycin Investigative [18]
Synonyms
SCHEMBL12324296
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 149 nM
External Link
 Compound Name VLI-27 Investigative [9]
Synonyms
AKT inhibitor (pancreatic cancer), NovaLead Pharma
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name A-443654 Investigative [19]
Synonyms
A-4436554
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 0.16 nM
External Link
 Compound Name NU-1001-41 Investigative [9]
Synonyms
Anti-phospho-AKT monoclonal antibodies (cancer), Nuclea Biotechnologies
    Click to Show/Hide
External Link
 Compound Name 4,5,6-trihydroxy-3-methylphthalide Investigative [20]
Synonyms
CHEMBL486813; AGUVVAYMPQDJDX-UHFFFAOYSA-; BDBM50242174; 3-methyl-4,5,6-trihydroxy-phthalide; 4,5,6-Trihydroxy-3-methylisobenzofuran-1(3H)-one
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 19700 nM
External Link
 Compound Name ALM-301 Investigative [9]
Synonyms
Akt inhibitors (cancer), Almac
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name BX-517 Investigative [21]
Synonyms
BX517; 850717-64-5; UNII-SYV8VN8W5K; SYV8VN8W5K; pdk-1 inhibitors; BX517(PDK1 inhibitor2); Indolinone based inhibitor, 4i; SCHEMBL5567818; CHEMBL228654; 5-Ureido-3-(1-(pyrrol-2-yl)ethylidene)indolin-2-one; BDBM17004; MolPort-046-033-615; BCP16225; EX-A2243; ZINC14962724; AKOS032945106; CS-6066; Urea, N-(2,3-dihydro-2-oxo-3-((3Z)-1-(1H-pyrrol-2-yl)ethylidene)-1H-indol-5-yl)-; Urea, N-(2,3-dihydro-2-oxo-3-(1-(1H-pyrrol-2-yl)ethylidene)-1H-indol-5-yl)-; Urea, (2,3-dihydro-2-oxo-3-(1-(1H-pyrrol-2-yl)ethylidene)-1H-indol-5-
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Inositol 1,3,4,5-Tetrakisphosphate Investigative [22]
Synonyms
Inositol-1,3,4,5-tetraphosphate; Ins-1,3,4,5-P4; 1D-myo-inositol 1,3,4,5-tetrakisphosphate; Inositol-1,3,4,5-tetrakisphosphate; inositol-(1,3,4,5)-tetrakisphosphate; Inositol 1,3,4,5-tetraphosphate; myo-Inositol-1,3,4,5-tetrakisphosphate; CHEMBL23552; D-myo-inositol 1,3,4,5-tetrakisphosphate; CHEBI:16783; myo-Inositol, 1,3,4,5-tetrakis(dihydrogen phosphate); 1D-myo-inositol 1,3,4,5-tetrakis(dihydrogen phosphate); Ins(1,3,4,5)P4; 1bwn; 4IP; 102850-29-3; myo-Inositol 1,3,4,5-tetraphosphate
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name (Z)-3-((1H-pyrrol-2-yl)methylene)indolin-2-one Investigative [21]
Synonyms
oxindole i; CHEMBL86755; 3-(1H-Pyrrol-2-ylmethylene)-1,3-dihydroindol-2-one; oxindole 1; AC1NZGXV; K00027; Indolinone based inhibitor, 1; SCHEMBL1162655; SCHEMBL13819612; BDBM17015; MolPort-023-197-743; SEZFNTZQMWJIAI-FLIBITNWSA-N; ZINC3874586; HSCI1_000049; NCGC00343760-01; BRD-K51816706-001-01-7; (3Z)-3-(1H-pyrrol-2-ylmethylidene)-1H-indol-2-one; 3-[(1H-Pyrrole-2-yl)methylene]-1H-indole-2(3H)-one; Z-(1H-Pyrrol-2-ylmethylene)-1,3-dihydro-indol-2-one
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 2300 nM
External Link
 Compound Name Akt inhibitor VIII Investigative [23]
Synonyms
isozyme-selective, Akti-1/2
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 58 nM
External Link
 Compound Name SB-747651A Investigative [24]
Synonyms
CHEMBL188434; compound 26; SCHEMBL4719834; GTPL8130; BDBM24996; oxadiazole-containing compound, 9; MBCJUIJWPYUEBX-UHFFFAOYSA-N; ZINC13998530; NCGC00273984-05; NCGC00273984-03; SB-747651; 4-{1-ethyl-7-[(piperidin-4-ylamino)methyl]-1H-imidazo[4,5-c]pyridin-2-yl}-1,2,5-oxadiazol-3-amine; [2-(4-Amino-furazan-3-yl)-1-ethyl-1H-imidazo[4,5-c]pyridin-7-ylmethyl]-piperidin-4-yl-amine
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 200 nM
External Link
 Compound Name PMID20005102C1 Investigative [25]
Synonyms
GTPL8181; BDBM50305878; B99
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1 nM
External Link
 Compound Name STAUROSPORINONE Investigative [26]
MOA Inhibitor
External Link
 Compound Name Ro31-8220 Investigative [26]
Synonyms
Bisindolylmaleimide IX; ro 31-8220; 125314-64-9; Ro 31 8220; Ro 318220; UNII-W9A0B5E78O; Ro-318220; Ro-31-8220; CHEMBL6291; W9A0B5E78O; CHEBI:38912; 3-{3-[4-(1-methyl-1H-indol-3-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]-1H-indol-1-yl}propyl carbamimidothioate; 3-{3-[4-(1-methyl-1H-indol-3-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]-1H-indol-1-yl}propyl imidothiocarbamate; CHEMBL1591531; Carbamimidothioic acid, 3-(3-(2,5-dihydro-4-(1-methyl-1H-indol-3-yl)-2,5-dioxo-1H-pyrrol-3-yl)-1H-indol-1-yl)propyl; bisindolymaleimide IX
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name BMS-536924 Investigative [27]
MOA Inhibitor
External Link
 Compound Name KN-62 Investigative [26]
Synonyms
KN-62 (non-isomeric); GTPL6001; HMS3229A04; CCG-206863
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name CI-1040 Investigative [26]
MOA Inhibitor
External Link
 Compound Name 4,5,6,7-tetrabromo-1H-benzo[d][1,2,3]triazole Investigative [28]
Synonyms
4,5,6,7-tetrabromobenzotriazole
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol Investigative [29]
MOA Inhibitor
External Link
 Compound Name Bisindolylmaleimide-I Investigative [26]
Synonyms
Bisindolylmaleimide i; 133052-90-1; GF 109203X; GF109203X; Go 6850; GF-109203X; RBT205 INHIBITOR; Go-6850; UNII-L79H6N0V6C; Bisindolylmaleimide I (GF 109203X); CHEMBL7463; 3-{1-[3-(DIMETHYLAMINO)PROPYL]-1H-INDOL-3-YL}-4-(1H-INDOL-3-YL)-1H-PYRROLE-2,5-DIONE; 3-(1-(3-(Dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione; L79H6N0V6C; QMGUOJYZJKLOLH-UHFFFAOYSA-N; 2-[1-(3-dimethylaminopropyl)indol-3-yl]-3-(indol-3-yl)maleimide; GF-109203; Go6850
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name RO-316233 Investigative [26]
Synonyms
119139-23-0; bisindolylmaleimide iv; 3,4-di(1H-indol-3-yl)-1H-pyrrole-2,5-dione; Arcyriarubin A; 3,4-Bis(3-indolyl)maleimide; 3,4-Di-1H-indol-3-yl-1H-pyrrole-2,5-dione; UNII-MBK3OO5K8T; BIM IV; 3,4-bis(1H-indol-3-yl)pyrrole-2,5-dione; MBK3OO5K8T; CHEMBL266487; 3,4-bis(1H-indol-3-yl)-2,5-dihydro-1H-pyrrole-2,5-dione; DQYBRTASHMYDJG-UHFFFAOYSA-N; 2,3-bis(1H-Indol-3-yl)maleimide; 1H-Pyrrole-2,5-dione, 3,4-di-1H-indol-3-yl-; Ro-31-6233; AK-15401; 3,4-bis(3-indolyl)-1H-pyrrole-2,5-dione; Bisindoylmaleimide; Bisindolyl deriv. 3
    Click to Show/Hide
MOA Inhibitor
External Link
2C25: Lung cancer 52 Compound(s) Regulating the Disease Click to Show/Hide the Full List
 Compound Name Adagrasib Approved [30]
Synonyms
2326521-71-3; MRTX-849; UNII-8EOO6HQF8Y; 8EOO6HQF8Y; 2-((S)-4-(7-(8-Chloronaphthalen-1-yl)-2-(((S)-1-methylpyrrolidin-2-yl)methoxy)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)-1-(2-fluoroacryloyl)piperazin-2-yl)acetonitrile; CHEMBL4594350; SCHEMBL20974691; GTPL10888; Kras G12C inhibitor MRTX849; BCP31538; EX-A3258; MRTX 849; MFCD32263433; s8884; compound 20 [PMID: 32250617]; BS-16211; HY-130149; CS-0105265; 2-Piperazineacetonitrile, 4-(7-(8-chloro-1-naphthalenyl)-5,6,7,8-tetrahydro-2-(((2S)-1-methyl-2-pyrrolidinyl)methoxy)pyrido(3,4-d)pyrimidin-4-yl)-1-(2-fluoro-1-oxo-2-propen-1-yl)-, (2S)-
    Click to Show/Hide
External Link
 Compound Name Amivantamab Approved [31]
External Link
 Compound Name Mobocertinib Approved [32]
Synonyms
1847461-43-1; TAK-788; TAK788; AP32788; UNII-39HBQ4A67L; 39HBQ4A67L; propan-2-yl 2-[4-{[2-(dimethylamino)ethyl](methyl)amino}-2-methoxy-5-(prop-2-enamido)anilino]-4-(1-methyl-1H-indol-3-yl)pyrimidine-5-carboxylate; Mobocertinib [INN]; Mobocertinib [USAN]; AP-32788; Mobocertinib (TAK788); Mobocertinib(TAK-788); SCHEMBL17373133; GTPL10468; BDBM368374; BCP31045; EX-A3392; US10227342, Example 10; MFCD32669806; NSC825519; s6813; TAK-788;AP32788; WHO 11183; NSC-825519; example 94 [WO2015195228A1]; HY-135815; CS-0114256; TAK-788;TAK 788; AP 32788; 5-Pyrimidinecarboxylic acid, 2-((4-((2-(dimethylamino)ethyl)methylamino)-2-methoxy-5-((1-oxo-2-propen-1-yl)amino)phenyl)amino)-4-(1-methyl-1H-indol-3-yl)-, 1-methylethyl ester; C(C=C)(=O)NC=1C(=CC(=C(C=1)NC1=NC=C(C(=N1)C1=CN(C2=CC=CC=C12)C)C(=O)OC(C)C)OC)N(C)CCN(C)C; Isopropyl 2-((5-acrylamido-4-((2-(dimethylamino)ethyl)(methyl)amino)-2-methoxyphenyl)amino)-4-(1-methyl-1H-indol-3-yl)pyrimidine-5-carboxylate; Isopropyl 2-(5-acrylamido-4-((2-(dimethylamino)ethyl)(methyl)amino)-2-methoxyphenylamino)-4-(1-methyl-1H-indol-3-yl)pyrimidine-5-carboxylate; Propan-2-yl 2-(5-(acryloylamino)-4-((2-(dimethylamino)ethyl)(methyl)amino)-2-methoxyanilino)-4-(1-methyl-1H-indol-3-yl)pyrimidine-5-carboxylate; propan-2-yl 2-[4-[2-(dimethylamino)ethyl-methylamino]-2-methoxy-5-(prop-2-enoylamino)anilino]-4-(1-methylindol-3-yl)pyrimidine-5-carboxylate
    Click to Show/Hide
External Link
 Compound Name Sugemalimab Approved in China [33]
External Link
 Compound Name Sacituzumab govitecan Approved [34]
Synonyms
1491917-83-9; 1535963-91-7; 1796566-95-4; CYSTEINYL CL2A-SN-38; DA64T2C2IO; DTXSID401335985; EX-A4354; F82944; GOVITECAN CYSTEINYL CONJUGATE; hRS 7SN38; hRS7-SN38; IMMU 132; IMMU-132; M9BYU8XDQ6; Sacituzumab govitecan; Sacituzumab govitecan [USAN]; sacituzumab-govitecan; Satralizumab linker; SN-38 CYSTEINYL CONJUGATE; UNII-M9BYU8XDQ6
    Click to Show/Hide
External Link
 Compound Name Atezolizumab Approved [35]
External Link
 Compound Name Tepotinib Approved [36]
Synonyms
1100598-32-0; EMD 1214063; UNII-1IJV77EI07; Tepotinib (EMD 1214063); EMD1214063; 1IJV77EI07; MSC-2156119J; Benzonitrile, 3-[1,6-dihydro-1-[[3-[5-[(1-methyl-4-piperidinyl)methoxy]-2-pyrimidinyl]phenyl]methyl]-6-oxo-3-pyridazinyl]-; C29H28N6O2; Tepotinib [INN]; Benzonitrile, 3-[1,6-Dihydro-1-[[3-[5-[(1-Methyl-4-Piperidinyl)Methoxy]-2-PyriMidinyl]Phenyl]Methyl]-6-Oxo-3-Pyridazinyl]; Benzonitrile, 3-(1,6-dihydro-1-((3-(5-((1-methyl-4-piperidinyl)methoxy)-2-pyrimidinyl)phenyl)methyl)-6-oxo
    Click to Show/Hide
External Link
 Compound Name Sotorasib Approved [37]
Synonyms
AMG-510; AMG510; AMG-510 racemate; 2252403-56-6; AMG 510; Kras G12C inhibitor 9; 2296729-00-3; UNII-2B2VM6UC8G; 2B2VM6UC8G; CHEMBL4535757; 2296729-00-3 (racemate); 4-((S)-4-Acryloyl-2-methylpiperazin-1-yl)-6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(2-isopropyl-4-methylpyridin-3-yl)pyrido[2,3-d]pyrimidin-2(1H)-one; 6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-propan-2-ylpyridin-3-yl)-4-[(2S)-2-methyl-4-prop-2-enoylpiperazin-1-yl]pyrido[2,3-d]pyrimidin-2-one; Sotorasib [INN]; 6-Fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-propan-2-ylpyridin-3-yl)-4-((2S)-2-methyl-4-prop-2-enoylpiperazin-1-yl)pyrido(2,3-d)pyrimidin-2-one; AMG510 racemate; Sotorasib [USAN]; AMG-510(racemate); Kras mutant-targeting AMG 510; SCHEMBL20560375; GTPL10678; AMG 510 pound>>AMG-510; AMY16918; BCP30452; BCP33368; EX-A3538; BDBM50514402; NSC818433; s8830; WHO 11370; DB15569; NSC-818433; BS-16684; HY-114277; CS-0081316; compound (R)-38 [PMID: 31820981]; (1m)-6-Fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-(propan-2-yl)pyridin-3-yl)-4-((2S)-2-methyl-4-(prop-2-enoyl)piperazin-1-yl)pyrido(2,3-d)pyrimidin-2(1H)-one; (1S)-4-((S)-4-Acryloyl-2-methylpiperazin-1-yl)-6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(2-isopropyl-4-methylpyridin-3-yl)pyrido[2,3-d]pyrimidin-2(1H)-one; 2296729-66-1; Pyrido(2,3-d)pyrimidin-2(1H)-one, 6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-(1-methylethyl)-3-pyridinyl)-4-((2S)-2-methyl-4-(1-oxo-2-propen-1-yl)-1-piperazinyl)-
    Click to Show/Hide
External Link
 Compound Name Entrectinib Approved [38]
Synonyms
1108743-60-7; RXDX-101; UNII-L5ORF0AN1I; Entrectinib (RXDX-101); L5ORF0AN1I; Benzamide, N-[5-[(3,5-difluorophenyl)methyl]-1H-indazol-3-yl]-4-(4-methyl-1-piperazinyl)-2-[(tetrahydro-2H-pyran-4-yl)amino]-; Benzamide, N-(5-((3,5-difluorophenyl)methyl)-1H-indazol-3-yl)-4-(4-methyl-1-piperazinyl)-2-((tetrahydro-2H-pyran-4-yl)amino)-; Entrectinib [USAN:INN]; YMX; Kinome_2659; Entrectinib(rxdx-101); Entrectinib (USAN/INN); SCHEMBL3512601; GTPL8290; CHEMBL1983268; KS-00000TSK
    Click to Show/Hide
External Link
 Compound Name Repotrectinib Approved [39]
Synonyms
FIKPXCOQUIZNHB-RRKGBCIJSA-N; SCHEMBL20438940; TPX 0005; BCP19778
    Click to Show/Hide
External Link
 Compound Name MYL-1402O Phase 3 [40]
Synonyms
bevacizumab biosimilar
    Click to Show/Hide
External Link
 Compound Name AB154 Phase 3 [41]
Synonyms
Domvanalimab
    Click to Show/Hide
External Link
 Compound Name Datopotamab deruxtecan Phase 3 [42]
External Link
 Compound Name CS1001 Phase 3 [43]
External Link
 Compound Name JDQ443 Phase 3 [44]
Synonyms
(S)-JDQ-443; 1-(6-((4S)-4-(5-Chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methyl-1H-indazol-5-yl)-1H-pyrazol-1-yl)-2-azaspiro[3.3]heptan-2-yl)prop-2-en-1-one; 1-[6-[(4R)-4-(5-chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methyl-1H-inda zol-5-yl)-1H-pyrazol-1-yl]-2-azaspiro[3.3]hept-2-yl]- 2-Propen-1-one; 1-[6-[(4R)-4-(5-Chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methyl-1H-indazol-5-yl)-1H-pyrazol-1-yl]-2-azaspiro[3.3]hept-2-yl]-2-propen-1-one; 1-[6-[4-(5-chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methylindazol-5-yl)pyrazol-1-yl]-2-azaspiro[3.3]heptan-2-yl]prop-2-en-1-one; 1-{6-[(4M)-4-(5-chloro-6-methyl-1H-indazol-4-yl)-5- methyl-3-(1-methyl-1H-indazol-5-yl)-1H-pyrazol-1-yl]-2- azaspiro[3.3]heptan-2-yl}prop-2-en-1-one; 1-{6-[(4M)-4-(5-Chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methyl-1H-indazol-5-yl)-1H-pyrazol-1-yl]-2-azaspiro[3.3]heptan-2-yl}prop-2-en-1-one; 2653994-08-0; 2653994-10-4; 2-Propen-1-one, 1-[6-[(4R)-4-(5-chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methyl-1H-indazol-5-yl)-1H-pyrazol-1-yl]-2-azaspiro[3.3]hept-2-yl]-; AKOS040757949; AT36708; BDBM50579985; CHEMBL5077861; compound 5 [PMID: 35404998]; CS-0226220; CS-0311034; EX-A5693; example 1a [WO2021120890A1]; GLXC-25533; GTPL11715; HY-139612A; JDQ 443; JDQ 443 [WHO-DD]; JDQ443; JDQ-443; MS-29737; NSC846146; NSC-846146; NVP-JDQ443; NVP-JDQ-443; Opnurasib; opnurasib [INN]; -PROPEN-1-ONE, 1-(6-((4R)-4-(5-CHLORO-6-METHYL-1H-INDAZOL-4-YL)-5-METHYL-3-(1-METHYL-1H-INDAZOL-5-YL)-1H-PYRAZOL-1-YL)-2-AZASPIRO(3.3)HEPT-2-YL)-; Q3W0H3V1LQ; SCHEMBL23533580
    Click to Show/Hide
External Link
 Compound Name TRS003 Phase 3 [45]
External Link
 Compound Name Tusamitamab ravtansine Phase 3 [46]
Synonyms
SAR408701
    Click to Show/Hide
External Link
 Compound Name RG6058 Phase 3 [47]
Synonyms
Tiragolumab
    Click to Show/Hide
External Link
 Compound Name GSK4069889 Phase 2 [48]
Synonyms
TSR-022
    Click to Show/Hide
External Link
 Compound Name APL-101 Phase 2 [49]
Synonyms
Bozitinib; PLB-1001; 1440964-89-5; Vebreltinib; Vebreltinib [USAN]; UNII-2WZP8A9VFN; 2WZP8A9VFN; Bozitinib (PLB-1001); SCHEMBL15594471; BDBM107096; CBI-3103; s6762; WHO 11677; HY-125017; CS-0088607; US9695175, 44; 1,2,4-Triazolo(4,3-b)pyridazine, 6-(1-cyclopropyl-1H-pyrazol-4-yl)-3-(difluoro(6- fluoro-2-methyl-2H-indazol-5-yl)methyl)-; 6-(1-Cyclopropyl-1H-pyrazol-4-yl)-3-(difluoro(6-fluoro-2-methyl-2H-indazol-5- yl)methyl)-1,2,4-triazolo(4,3-b)pyridazine
    Click to Show/Hide
External Link
 Compound Name SGN-LIV1A Phase 2 [50]
Synonyms
Ladiratuzumab Vedotin
    Click to Show/Hide
External Link
 Compound Name BNT116 Phase 2 [51]
External Link
 Compound Name AZD7789 Phase 2 [52]
External Link
 Compound Name L-DOS47 Phase 1/2 [53]
External Link
 Compound Name NC318 Phase 2 [54]
External Link
 Compound Name Vorolanib Phase 2 [55]
Synonyms
UNII-YP8G3I74EL; YP8G3I74EL; 1013920-15-4; (S,Z)-N-(1-(Dimethylcarbamoyl)pyrrolidin-3-yl)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide; Vorolanib [INN]; SCHEMBL2439528; CHEMBL4297587; N-((3S)-1-(dimethylcarbamoyl)pyrrolidin-3-yl)-5-((Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide; s6843; DB15247; HY-109019; CS-0030517; Q27294638; 1H-Pyrrole-3-carboxamide, N-((3S)-1-((dimethylamino)carbonyl)-3-pyrrolidinyl)-5-((Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl)-2,4-dimethyl-
    Click to Show/Hide
External Link
 Compound Name Xofigo Phase 2 [56]
External Link
 Compound Name Bintrafusp alfa Phase 2 [57]
External Link
 Compound Name Voyager-V1 Phase 2 [58]
Synonyms
VSV-IFNBeta-NIS
    Click to Show/Hide
External Link
 Compound Name AB-106 Phase 2 [59]
Synonyms
DS6051b; GTPL11198; AB106
    Click to Show/Hide
External Link
 Compound Name RO-5126766 Phase 2 [60]
Synonyms
VS-6766; CH-5126766; Dual Raf/MEK protein kinase inhibitor (cancer), Roche
    Click to Show/Hide
External Link
 Compound Name TC-210 Phase 1/2 [61]
External Link
 Compound Name EMB-01 Phase 1/2 [62]
External Link
 Compound Name NM21-1480 Phase 1/2 [63]
External Link
 Compound Name MRx0518 Phase 1/2 [64]
External Link
 Compound Name DZD9008 Phase 1/2 [65]
External Link
 Compound Name BGB-A425 Phase 1/2 [66]
External Link
 Compound Name Rilvegostomig Phase 1/2 [67]
Synonyms
AZD2936
    Click to Show/Hide
External Link
 Compound Name IK-007 Phase 1/2 [68]
Synonyms
grapiprant
    Click to Show/Hide
External Link
 Compound Name IBI318 Phase 1 [69]
External Link
 Compound Name GEN-011 Phase 1 [70]
External Link
 Compound Name ENV-105 Phase 1 [71]
Synonyms
Carotuximab
    Click to Show/Hide
External Link
 Compound Name AMG 160 Phase 1 [72]
External Link
 Compound Name ADP-A2M10 Phase 1 [73]
External Link
 Compound Name MEDI5752 Phase 1 [74]
External Link
 Compound Name PF-07104091 Phase 1 [75]
External Link
 Compound Name PF-06936308 Phase 1 [76]
External Link
 Compound Name GEM3PSCA Phase 1 [77]
External Link
 Compound Name PF-07257876 Phase 1 [78]
External Link
 Compound Name Cosibelimab Phase 1 [79]
Synonyms
CK-301/TG-1501
    Click to Show/Hide
External Link
 Compound Name Gemcitabine Approved [80]
External Link
 Compound Name SMI-4a Investigative [81]
Synonyms
438190-29-5; SMI 4a; TCS PIM-1 4a; (Z)-SMI-4a; (Z)-5-(3-(trifluoromethyl)benzylidene)thiazolidine-2,4-dione; (5Z)-5-[3-(trifluoromethyl)benzylidene]-1,3-thiazolidine-2,4-dione; CHEMBL183906; (5Z)-5-[[3-(TRIFLUOROMETHYL)PHENYL]METHYLENE]-2,4-THIAZOLIDINEDIONE; (5Z)-5-[[3-(trifluoromethyl)phenyl]methylidene]-1,3-thiazolidine-2,4-dione; 327033-36-3; C11H6F3NO2S; (Z)-5-(3-(Trifluoromethyl)benzylidene)-thiazolidine-2,4-dione; (5Z)-5-{[3-(trifluoromethyl)phenyl]methylidene}-1,3-thiazolidine-2,4-dione; Pim inhibitor 4a; 3vc4; SMI-4q; TCS PIM-1-4a; 5-(3-(Trifluoromethyl)benzylidene)thiazolidine-2,4-dione; 5-[3-(Trifluoromethyl)benzylidene]thiazolidine-2,4-dione; cc-717; thiazolidine-2,4-dione, 4a; SCHEMBL2541382; SCHEMBL2541388; BDBM26626; AOB6260; EX-A111; SYN1113; BDBM138364; HMS3229J21; 2720AH; HY-16576A; MFCD01152003; s8005; ZINC12576047; AKOS001314163; SMI-4a, >=98% (HPLC); CCG-265027; NCGC00345836-02; NCGC00345836-14; AC-32861; HY-15474; AB0165836; EC-000.2291; J3.561.866J; A11945; W-5256; US8877795, 12; Q27451064; 5-[[3-(trifluoromethyl)phenyl]methylene]-2,4-thiazolidinedione
    Click to Show/Hide
External Link
References
Ref 1 Stimulation of Let-7 Maturation by Metformin Improved the Response to Tyrosine Kinase Inhibitor Therapy in an m6A Dependent Manner. Front Oncol. 2022 Jan 6;11:731561. doi: 10.3389/fonc.2021.731561. eCollection 2021.
Ref 2 Methyltransferase-like 3 promotes the progression of lung cancer via activating PI3K/AKT/mTOR pathway. Clin Exp Pharmacol Physiol. 2022 Jul;49(7):748-758. doi: 10.1111/1440-1681.13647. Epub 2022 May 23.
Ref 3 Novel and selective DNA methyltransferase inhibitors: Docking-based virtual screening and experimental evaluation. Bioorg Med Chem. 2010 Jan 15;18(2):822-9. doi: 10.1016/j.bmc.2009.11.050. Epub 2009 Nov 27.
Ref 4 DNA methyltransferase inhibitors: an updated patent review (2012-2015). Expert Opin Ther Pat. 2016 Sep;26(9):1017-30. doi: 10.1080/13543776.2016.1209488. Epub 2016 Jul 18.
Ref 5 SAR around (l)-S-adenosyl-l-homocysteine, an inhibitor of human DNA methyltransferase (DNMT) enzymes. Bioorg Med Chem Lett. 2009 May 15;19(10):2747-51. doi: 10.1016/j.bmcl.2009.03.113. Epub 2009 Mar 28.
Ref 6 Constrained (l-)-S-adenosyl-l-homocysteine (SAH) analogues as DNA methyltransferase inhibitors. Bioorg Med Chem Lett. 2009 May 15;19(10):2742-6.
Ref 7 FDA Approved Drug Products from FDA Official Website. 2023. Application Number: 218197
Ref 8 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 9 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: 1479).
Ref 10 CenterWatch. Drugs in Clinical Trials Database. CenterWatch. 2008.
Ref 11 Pre-clinical and Clinical Safety Studies of CMX-2043: a cytoprotective lipoic acid analogue for ischaemia-reperfusion injury. Basic Clin Pharmacol Toxicol. 2014 Nov;115(5):456-64. doi: 10.1111/bcpt.12254. Epub 2014 May 16.
Ref 12 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 13 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 14 Discovery of a 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitor (BMS-754807) of insulin-like growth factor receptor (IGF-1R) kinase in clinical development. J Med Chem. 2009 Dec 10;52(23):7360-3. doi: 10.1021/jm900786r.
Ref 15 Cancer stem cell (CSC) inhibitors: a review of recent patents (2012-2015). Expert Opin Ther Pat. 2017 Jul;27(7):753-761. doi: 10.1080/13543776.2017.1325465. Epub 2017 May 5.
Ref 16 Raft nanodomains contribute to Akt/PKB plasma membrane recruitment and activation. Nat Chem Biol. 2008 Sep;4(9):538-47. doi: 10.1038/nchembio.103. Epub 2008 Jul 20.
Ref 17 Comprehensive analysis of kinase inhibitor selectivity. Nat Biotechnol. 2011 Oct 30;29(11):1046-51. doi: 10.1038/nbt.1990.
Ref 18 The PI3K/Akt pathway as a target in the treatment of hematologic malignancies. Anticancer Agents Med Chem. 2009 Jun;9(5):550-9. doi: 10.2174/187152009788451851.
Ref 19 Syntheses of potent, selective, and orally bioavailable indazole-pyridine series of protein kinase B/Akt inhibitors with reduced hypotension. J Med Chem. 2007 Jun 28;50(13):2990-3003.
Ref 20 A phthalide with in vitro growth inhibitory activity from an oidiodendron strain. J Nat Prod. 2004 Dec;67(12):2086-9. doi: 10.1021/np040123n.
Ref 21 Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3814-8. doi: 10.1016/j.bmcl.2007.04.071. Epub 2007 Apr 27.
Ref 22 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
Ref 23 Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors. Bioorg Med Chem Lett. 2005 Feb 1;15(3):761-4.
Ref 24 Identification of 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a novel inhibitor of AKT kinase. J Med Chem. 2008 Sep 25;51(18):5663-79. doi: 10.1021/jm8004527.
Ref 25 2,3,5-Trisubstituted pyridines as selective AKT inhibitors. Part II: Improved drug-like properties and kinase selectivity from azaindazoles. Bioorg Med Chem Lett. 2010 Jan 15;20(2):679-83. doi: 10.1016/j.bmcl.2009.11.060. Epub 2009 Nov 20.
Ref 26 Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105. doi: 10.1042/0264-6021:3510095.
Ref 27 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 28 Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole. J Med Chem. 2004 Dec 2;47(25):6239-47. doi: 10.1021/jm049854a.
Ref 29 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 30 FDA Approved Drug Products from FDA Official Website. 2022. Application Number: 216340.
Ref 31 FDA Approved Drug Products from FDA Official Website. 2022. Application Number: 761210.
Ref 32 ClinicalTrials.gov (NCT04129502) TAK-788 as First-line Treatment Versus Platinum-Based Chemotherapy for Non-Small Cell Lung Cancer (NSCLC) With EGFR Exon 20 Insertion Mutations. U.S. National Institutes of Health.
Ref 33 Sugemalimab: First Approval. Drugs. 2022 Apr;82(5):593-599.
Ref 34 ClinicalTrials.gov (NCT05089734) Open-Label, Global, Multicenter, Randomized, Phase 3 Study of Sacituzumab Govitecan Versus Docetaxel in Patients With Advanced or Metastatic Non-Small Cell Lung Cancer (NSCLC) With Progression on or After Platinum-Based Chemotherapy and Anti-PD-1/PD-L1 Immunotherapy. U.S.National Institutes of Health.
Ref 35 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
Ref 36 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2021
Ref 37 FDA Approved Drug Products from FDA Official Website. 2023. Application Number: 214665.
Ref 38 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
Ref 39 FDA Approved Drug Products from FDA Official Website. 2023. Application Number: 218213
Ref 40 ClinicalTrials.gov (NCT04633564) Multicenter, Double-Blind, Randomized, Parallel-Group Study to Assess the Efficacy and Safety of MYL-1402O Compared With Avastin?, in the First-line Treatment of Patients With Stage IV Non-Squamous Non-Small Cell Lung Cancer. U.S.National Institutes of Health.
Ref 41 ClinicalTrials.gov (NCT04736173) Study to Evaluate Monotherapy Compared to Combination Immunotherapies in Participants With PD-L1 Positive Non-small Cell Lung Cancer. U.S. National Institutes of Health.
Ref 42 ClinicalTrials.gov (NCT05555732) A Randomized Phase 3 Study of Datopotamab Deruxtecan (Dato-DXd) and Pembrolizumab With or Without Platinum Chemotherapy in Subjects With No Prior Therapy for Advanced or Metastatic PD-L1 TPS <50% Non-squamous Non-small Cell Lung Cancer Without Actionable Genomic Alterations (TROPION-Lung07). U.S.National Institutes of Health.
Ref 43 ClinicalTrials.gov (NCT03728556) A Study of CS1001 in Subjects With Stage III Non-Small Cell Lung Cancer. U.S. National Institutes of Health.
Ref 44 ClinicalTrials.gov (NCT05132075) A Randomized, Controlled, Open Label, Phase III Study Evaluating the Efficacy and Safety of JDQ443 Versus Docetaxel in Previously Treated Subjects With Locally Advanced or Metastatic KRAS G12C Mutant Non-small Cell Lung Cancer. U.S.National Institutes of Health.
Ref 45 ClinicalTrials.gov (NCT04416035) A Phase 3, Multicenter, Randomized and Double-Blind Study to Assess the Similarity in Efficacy and Safety Between TRS003 and China-approved Bevacizumab in Subjects With Advanced Nonsquamous NSCLC. U.S.National Institutes of Health.
Ref 46 ClinicalTrials.gov (NCT05245071) Open-label, Phase 2 Study, Evaluating the Efficacy and Safety of Tusamitamab Ravtansine in Non-squamous Non-small-cell Lung Cancer (NSQ NSCLC) Participants With Negative or Moderate CEACAM5 Expression Tumors and High Circulating CEA. U.S.National Institutes of Health.
Ref 47 ClinicalTrials.gov (NCT04294810) A Study of Tiragolumab in Combination With Atezolizumab Compared With Placebo in Combination With Atezolizumab in Patients With Previously Untreated Locally Advanced Unresectable or Metastatic PD-L1-Selected Non-Small Cell Lung Cancer (SKYSCRAPER-01). U.S. National Institutes of Health.
Ref 48 ClinicalTrials.gov (NCT04655976) Study of Cobolimab in Combination With Dostarlimab and Docetaxel in Advanced NSCLC Participants (COSTAR Lung). U.S. National Institutes of Health.
Ref 49 ClinicalTrials.gov (NCT04258033) A Study of PLB1001 in Non-small Cell Lung Cancer With c-Met Dysregulation. U.S. National Institutes of Health.
Ref 50 ClinicalTrials.gov (NCT04032704) A Study of Ladiratuzumab Vedotin in Advanced Solid Tumors. U.S. National Institutes of Health.
Ref 51 ClinicalTrials.gov (NCT05557591) A Phase 2 Study of Cemiplimab (Anti-PD-1 Antibody) in Combination With BNT116 (FixVac Lung) Versus Cemiplimab Monotherapy in First-Line Treatment of Patients With Advanced Non-Small Cell Lung Cancer (NSCLC) With Tumors Expressing PD-L1 >=50%. U.S.National Institutes of Health.
Ref 52 ClinicalTrials.gov (NCT04931654) A Phase I/IIa Open-label Dose Escalation and Expansion Study to Evaluate the Safety, Pharmacokinetics, Pharmacodynamics, and Efficacy of AZD7789, an Anti-PD-1 and Anti-TIM-3 Bispecific Antibody, in Participants With Advanced or Metastatic Solid Tumors. U.S.National Institutes of Health.
Ref 53 ClinicalTrials.gov (NCT02340208) A Phase I/II Open-Label, Non-Randomized Dose Escalation Study of Immunoconjugate L-DOS47. U.S. National Institutes of Health.
Ref 54 ClinicalTrials.gov (NCT04699123) The Study of NC318 Alone or in Combination With Pembrolizumab in Patients With Advanced Non-small Cell Lung Cancer. U.S. National Institutes of Health.
Ref 55 ClinicalTrials.gov (NCT03848611) CM082 and JS001 in Patients With Advanced Non-Small Cell Lung Cancer (NSCLC).. U.S. National Institutes of Health.
Ref 56 ClinicalTrials.gov (NCT02283749) BrUOG L301: Xofigo Following Frontline-Line Chemotherapy For Patients With Non-Small Cell Lung Cancer and Bone Metastases. U.S.National Institutes of Health.
Ref 57 ClinicalTrials.gov (NCT04560686) Bintrafusp Alfa Before Surgery for the Treatment of Untreated Resectable Non-small Cell Lung Cancer. U.S. National Institutes of Health.
Ref 58 ClinicalTrials.gov (NCT04291105) Phase 2 Trial of Voyager V1 in Combination With Cemiplimab in Cancer Patients. U.S. National Institutes of Health.
Ref 59 ClinicalTrials.gov (NCT04395677) A Study of AB-106 in Subjects With Advanced NSCLC Harboring ROS1 Fusion Gene. U.S. National Institutes of Health.
Ref 60 ClinicalTrials.gov (NCT04625270) A Study of VS-6766 v. VS-6766 + Defactinib in Recurrent Low-Grade Serous Ovarian Cancer With and Without a KRAS Mutation. U.S. National Institutes of Health.
Ref 61 ClinicalTrials.gov (NCT03907852) Phase 1/2 Trial of Gavo-cel (TC-210) in Patients With Advanced Mesothelin-Expressing Cancer. U.S. National Institutes of Health.
Ref 62 ClinicalTrials.gov (NCT03797391) A Dose Escalation Study of EMB-01 in Participants With Advanced/Metastatic Solid Tumors. U.S. National Institutes of Health.
Ref 63 ClinicalTrials.gov (NCT04442126) A Study of NM21-1480 in Adult Patients With Advanced Solid Tumors. U.S. National Institutes of Health.
Ref 64 ClinicalTrials.gov (NCT03637803) Live Biotherapeutic Product MRx0518 and Pembrolizumab Combination Study in Solid Tumors. U.S. National Institutes of Health.
Ref 65 ClinicalTrials.gov (NCT03974022) Assessing an Oral EGFR Inhibitor, DZD9008 in Patients Who Have Advanced Non-small Cell Lung Cancer With EGFR or HER2 Mutation (WU-KONG1). U.S. National Institutes of Health.
Ref 66 ClinicalTrials.gov (NCT03744468) Study of BGB-A425 in Combination With Tislelizumab in Advanced Solid Tumors. U.S. National Institutes of Health.
Ref 67 ClinicalTrials.gov (NCT04995523) Phase I/II, Open-label, Dose Escalation and Dose Expansion Study to Evaluate Safety, Pharmacokinetics, Pharmacodynamics and Efficacy of AZD2936 Anti-TIGIT/Anti-PD-1 Bispecific Antibody in Participants With Advanced or Metastatic NSCLC. U.S.National Institutes of Health.
Ref 68 ClinicalTrials.gov (NCT03696212) Open Label, Single Arm, Phase 1b/2 Study to Evaluate the Safety and Efficacy of Grapiprant (ARY-007) in Combination With Pembrolizumab in Patients With Advanced or Metastatic Post-PD-1/L1 Non-Small Cell Lung Cancer (NSCLC) Adenocarcinoma. U.S.National Institutes of Health.
Ref 69 ClinicalTrials.gov (NCT04777084) The Efficacy and Safety of the Bispecific Anti-PD-1/PD-L1 Antibody IBI318 Combined With Lenvatinib in NSCLC.. U.S. National Institutes of Health.
Ref 70 ClinicalTrials.gov (NCT04596033) TiTAN-1: Safety, Proliferation and Persistence of GEN-011 Autologous Cell Therapy. U.S. National Institutes of Health.
Ref 71 ClinicalTrials.gov (NCT05401110) IIT2021-12-Reckamp-Osi105: Phase I Study of Osimertinib With Carotuximab in Advanced, EGFR-mutated Non-Small Cell Lung Cancer. U.S.National Institutes of Health.
Ref 72 ClinicalTrials.gov (NCT04822298) Study of AMG 160 in Subjects With Non-Small Cell Lung Cancer. U.S. National Institutes of Health.
Ref 73 Phase I clinical trial evaluating the safety and efficacy of ADP-A2M10 SPEAR T cells in patients with MAGE-A10(+) advanced non-small cell lung cancer. J Immunother Cancer. 2022 Jan;10(1):e003581.
Ref 74 ClinicalTrials.gov (NCT03819465) A Study of Novel Anti-cancer Agents in Patients With Previously Untreated NSCLC (MAGELLAN). U.S. National Institutes of Health.
Ref 75 ClinicalTrials.gov (NCT04553133) PF-07104091 as a Single Agent and in Combination Therapy. U.S. National Institutes of Health.
Ref 76 ClinicalTrials.gov (NCT03674827) Vaccine-Based Immunotherapy Regimen For NSCLC and TNBC. U.S. National Institutes of Health.
Ref 77 ClinicalTrials.gov (NCT03927573) Study With Bispecific Antibody Engaging T-cells, in Patients With Progressive Cancer Diseases With Positive PSCA Marker. U.S. National Institutes of Health.
Ref 78 ClinicalTrials.gov (NCT04881045) A PHASE 1 DOSE ESCALATION AND EXPANSION STUDY EVALUATING THE SAFETY, TOLERABILITY, PHARMACOKINETICS, PHARMACODYNAMICS, AND ANTITUMOR ACTIVITY OF PF-07257876 IN PATIENTS WITH ADVANCED OR METASTATIC TUMORS. U.S.National Institutes of Health.
Ref 79 ClinicalTrials.gov (NCT04786964) Study of Pemetrexed+Platinum Chemotherapy With or Without Cosibelimab (CK-301) in First Line Metastatic Non-squamous Non-Small Cell Lung Cancer (CONTERNO). U.S. National Institutes of Health.
Ref 80 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 81 Pim-1 inhibitor SMI-4a suppresses tumor growth in non-small cell lung cancer via PI3K/AKT/mTOR pathway. Onco Targets Ther. 2019 Apr 23;12:3043-3050.