m6A-centered Crosstalk Information

Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
Crosstalk ID
M6ACROT02151
 [1], [2]
DNA methylation DNMT3A METTL3 Direct Inhibition m6A modification MTOR MTOR METTL3 Methylation : m6A sites
m6A Modification:
m6A Regulator Methyltransferase-like 3 (METTL3) WRITER
 Regulator Info 
m6A Target Serine/threonine-protein kinase mTOR (MTOR)
 Targert Gene 
Epigenetic Regulation that have Cross-talk with This m6A Modification:
Epigenetic Regulation Type DNA methylation (DNAMeth)
Epigenetic Regulator Cysteine methyltransferase DNMT3A (DNMT3A) 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/AKT/Serine/threonine-protein kinase mTOR (MTOR) pathway.
Responsed Disease Lung cancer ICD-11: 2C25
 Disease Info 
Responsed Drug Metformin
 Drug Info 
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
Cysteine methyltransferase DNMT3A (DNMT3A) 8 Compound(s) Regulating the Target Click to Show/Hide the Full List
 Compound Name PMID27376512-Compound-Figure3CN Patented [3]
MOA Inhibitor
Activity EC50 = 1100 nM
External Link
CID: 117968550
TTD: D02VTV
 Compound Name PMID27376512-Compound-Figure3CG Patented [3]
MOA Inhibitor
Activity EC50 = 2400 nM
External Link
CID: 117967861
TTD: D03LZO
 Compound Name PMID27376512-Compound-Figure3CM Patented [3]
MOA Inhibitor
Activity EC50 = 1100 nM
External Link
CID: 117976053
TTD: D0F8AB
 Compound Name PMID27376512-Compound-Figure2aExample1 Patented [3]
MOA Inhibitor
Activity IC50 = 3000 nM
External Link
CID: 71521835
TTD: D01LUJ
 Compound Name PMID27376512-Compound-MTC-424 Patented [3]
MOA Inhibitor
Activity IC50 = 1940 nM
External Link
TTD: D02WRM
 Compound Name PMID27376512-Compound-MTC-427 Patented [3]
MOA Inhibitor
Activity IC50 = 295 nM
External Link
TTD: D0HA0J
 Compound Name PMID27376512-Compound-MTC-422 Patented [3]
MOA Inhibitor
Activity IC50 = 1430 nM
External Link
TTD: D0QY0N
 Compound Name PMID27376512-Compound-MTC-423 Patented [3]
MOA Inhibitor
Activity IC50 = 363 nM
External Link
TTD: D0W9VZ
Serine/threonine-protein kinase mTOR (MTOR) 72 Compound(s) Regulating the Target Click to Show/Hide the Full List
 Compound Name Novolimus Approved [4]
MOA Inhibitor
External Link
CID: 9854320
TTD: D03FCF
 Compound Name Temsirolimus Approved [5]
Synonyms
Torisel
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MOA Inhibitor
Activity IC50 = 1760 nM
External Link
CID: 6918289
TTD: D0ES1Q
 Compound Name Everolimus Approved [6]
Synonyms
Afinitor; Afinitor (TN); CERTICAN(R); Certican; Certican (TN); Everolimus (JAN/USAN/INN); Everolimus [USAN]; MTOR kinase inhibitors; NVP-RAD-001; RAD 001; RAD-001; RAD-001C; RAD001; RAD001, SDZ-RAD, Certican, Zortress, Afinitor, Everolimus; SDZ-RAD; Zortress
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MOA Inhibitor
External Link
CID: 6442177
TTD: D0K3QS
DrugBank: DB01590
 Compound Name Zotarolimus Approved [7]
Synonyms
Abt-578; Zotarolimus (TN)
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MOA Modulator
Activity IC50 = 3.3 nM
External Link
CID: 9876378
TTD: D0V7WS
 Compound Name Sirolimus Approved [8]
Synonyms
53123-88-9; Rapamune; Rapamycin (Sirolimus); AY-22989; Rapammune; sirolimusum; WY-090217; RAPA; Antibiotic AY 22989; AY 22989; UNII-W36ZG6FT64; CCRIS 9024; CHEBI:9168; SILA 9268A; W36ZG6FT64; HSDB 7284; C51H79NO13; NSC 226080; DE-109; NCGC00021305-05; DSSTox_CID_3582; DSSTox_RID_77091; DSSTox_GSID_23582; Cypher; Supralimus; Wy 090217; Perceiva; RAP; RPM; Rapamycin from Streptomyces hygroscopicus; SIIA 9268A; LCP-Siro; MS-R001; Rapamune (TN); Rapamycin (TN); Sirolimus (RAPAMUNE); Rapamycin C-7, analog 4; Sirolimus (USAN/INN); Sirolimus [USAN:BAN:INN]; Sirolimus, Rapamune,Rapamycin; Heptadecahydro-9,27-dihydroxy-3-[(1R)-2-[(1S,3R,4R)-4-hydroxy; 23,27-Epoxy-3H-pyrido(2,1-c)(1,4)oxaazacyclohentriacontine; 23,27-Epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclohentriacontine; 23,27-epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclohentriacontine-1,5,11,28,29; 3H-pyrido(2,1-c)(1,4)oxaazacyclohentriacontine-1,5,11,28,29(4H,6H,31H)-pentone; Sirolimus (MTOR inhibitor)
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MOA Inhibitor
External Link
CID: 5284616
TTD: D03LJR
DrugBank: DB00877
 Compound Name PF-04449913 Approved [9]
Synonyms
Glasdegib; 1095173-27-5; PF 04449913; UNII-K673DMO5H9; K673DMO5H9; CHEMBL2043437; Glasdegib (PF-04449913); Glasdegib [USAN:INN]; Glasdegib (USAN/INN); PF-04449913;Glasdegib; GTPL8201; Glasdegib(PF-04449913); EX-A858; MolPort-035-789-706; SFNSLLSYNZWZQG-VQIMIIECSA-N; ZINC68251434; PF-913; BDBM50385635; 2640AH; AKOS027324121; CS-2
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MOA Inhibitor
External Link
CID: 25166913
TTD: D0S5LO
DrugBank: DB11978
 Compound Name Ridaforolimus Phase 3 [10]
Synonyms
Deforolimus; AP 23573; MK 8669; AP-23573; MK-8669; AP23573, MK-8669, Ridaforolimus, Deforolimus
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MOA Inhibitor
External Link
CID: 11520894
TTD: D0O3CV
DrugBank: DB06233
 Compound Name INK128 Phase 2 [11]
Synonyms
1224844-38-5; Sapanisertib; INK-128; INK 128; INK 128 (MLN0128); TAK-228; UNII-JGH0DF1U03; JGH0DF1U03; 5-(4-amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)benzo[d]oxazol-2-amine; INK-0128; 3-(2-Amino-5-benzoxazolyl)-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine; C15H15N7O; 5-(4-amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)-1,3-benzoxazol-2-amine; 5-(4-Amino-1-isopropyl-1H-pyrazolo[3,4-d]-pyrimidin-3-yl)benzo[d]oxazol-2-amine; Sapanisertib (USAN/INN)
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MOA Inhibitor
Activity Ki = 1 nM
External Link
CID: 45375953
TTD: D03DPZ
DrugBank: DB11836
 Compound Name OSI-027 Phase 2 [12]
MOA Inhibitor
External Link
CID: 135398516
TTD: D0H7XL
DrugBank: DB12387
 Compound Name ABI-009 Phase 2 [13]
MOA Inhibitor
External Link
TTD: D0W3UV
 Compound Name Salirasib Discontinued in Phase 1/2 [4]
Synonyms
162520-00-5; Farnesylthiosalicylic acid; S-Farnesylthiosalicylic acid; UNII-MZH0OM550M; MZH0OM550M; CHEMBL23293; AK186909; Farnesyl Thiosalicylic Acid; 2-[[(2E,6E)-3,7,11-Trimethyl-2,6,10-dodecatrien-1-yl]thio]benzoic Acid; 2-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trienyl]sulfanylbenzoic acid; 2-((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trienylthio)benzoic acid; 2-(((2E,6E)-3,7,11-Trimethyl-2,6,10-dodecatrienyl)sulfanyl)benzoic acid; Benzoic acid, 2-(((2E,6E)-3,7,11-trimethyl-2,6,10-dodecatrienyl)thio)-; FTS; Farnesylthiosalicyclic acid; FTS, Thyreos; Ras antagonists, Thyreos; S-trans; Th-101; Trans-farnesylthiosalicylicacid; FTS (oral, cancer), Concordia; Farnesylthiosalicyclic acid (oral, cancer), Concordia; Ras-inhibitors (cancer), Concordia; FTS (oral, cancer), Concordia/Ono; KD032
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MOA Modulator
External Link
CID: 5469318
TTD: D00KTV
DrugBank: DB12681
 Compound Name SAR245409 Phase 2 [4]
MOA Inhibitor
Activity IC50 = 157 nM
External Link
CID: 16123056
TTD: D01PGR
DrugBank: DB12400
 Compound Name SF1126 Phase 2 [13]
Synonyms
CC-1126; SF-1126; L-Serine, N2-(1,4-dioxo-4-((4-(4-oxo-8-phenyl-4H-1-benzopyran-2-yl)morpholinium-4-yl)methoxy)butyl)-L-arginylglycyl-L-alpha-aspartyl-, inner salt
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MOA Inhibitor
External Link
CID: 66577114
TTD: D03NJY
 Compound Name PF-05212384 Phase 2 [14]
Synonyms
PKI-587; 1197160-78-3; Gedatolisib; PKI587; PKI 587; 1-(4-(4-(Dimethylamino)piperidine-1-carbonyl)phenyl)-3-(4-(4,6-dimorpholino-1,3,5-triazin-2-yl)phenyl)urea; PF 05212384; UNII-96265TNH2R; PF-05212384 (PKI-587); CHEMBL592445; 96265TNH2R; N-[4-[[4-(Dimethylamino)-1-piperidinyl]carbonyl]phenyl]-N'-[4-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]phenyl]urea; Gedatolisib (PF-05212384, PKI-587); Urea, N-(4-((4-(dimethylamino)-1-piperidinyl)carbonyl)phenyl)-N'-(4-(4,6-di-4-morpholinyl-1,3,5-triazin-2-yl)phenyl)-
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MOA Modulator
Activity IC50 = 0.4 nM
External Link
CID: 44516953
TTD: D0D8JB
DrugBank: DB11896
 Compound Name LY3023414 Phase 2 [15]
MOA Modulator
External Link
CID: 57519748
TTD: D0H1WC
DrugBank: DB12167
 Compound Name PF-04691502 Phase 2 [16]
Synonyms
1013101-36-4; PF 04691502; UNII-4W39NS61KI; 4W39NS61KI; 2-amino-8-((1r,4r)-4-(2-hydroxyethoxy)cyclohexyl)-6-(6-methoxypyridin-3-yl)-4-methylpyrido[2,3-d]pyrimidin-7(8H)-one; CHEMBL1234354; PF04691502; 2-Amino-8-[trans-4-(2-Hydroxyethoxy)cyclohexyl]-6-(6-Methoxypyridin-3-Yl)-4-Methylpyrido[2,3-D]pyrimidin-7(8h)-One; 2-Amino-8-[4-(2-hydroxyethoxy)cyclohexyl]-6-(6-methoxypyridin-3-yl)-4-methylpyrido[2,3-d]pyrimidin-7-one
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MOA Modulator
Activity IC50 = 7.9 nM
External Link
CID: 25033539
TTD: D0N5JZ
DrugBank: DB11974
 Compound Name GDC-0980/RG7422 Phase 2 [4]
Synonyms
Apitolisib; 1032754-93-0; GDC-0980; GDC0980; RG7422; (S)-1-(4-((2-(2-aminopyrimidin-5-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)piperazin-1-yl)-2-hydroxypropan-1-one; UNII-1C854K1MIJ; GDC-0980 (RG7422); Apitolisib (GDC-0980, RG7422); 1C854K1MIJ; CHEMBL1922094; RG-7422; (2s)-1-(4-{[2-(2-Aminopyrimidin-5-Yl)-7-Methyl-4-(Morpholin-4-Yl)thieno[3,2-D]pyrimidin-6-Yl]methyl}piperazin-1-Yl)-2-Hydroxypropan-1-One; J-502360; C23H30N8O3S
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MOA Modulator
Activity Ki = 17 nM
External Link
CID: 25254071
TTD: D0O6VZ
DrugBank: DB12180
 Compound Name BEZ235 Phase 2 [17]
Synonyms
BEZ-235; S14-0511; NVP-BEZ-235; NVP-BEZ235, BEZ235; 2-(4-(2,3-dihydro-3-methyl-2-oxo-8-(quinolin-3-yl)imidazo[4,5-c]quinolin-1-yl)phenyl)-2-methylpropanenitrile
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MOA Modulator
Activity IC50 = 5 nM
External Link
CID: 11977753
TTD: D0VG0D
DrugBank: DB11651
 Compound Name MM-141 Phase 2 [13]
MOA Inhibitor
External Link
TTD: D00BUO
 Compound Name PQR309 Phase 2 [4]
Synonyms
Bimiralisib; 1225037-39-7; PI3K-IN-2; PQR-309; UNII-6Z3QHB00LB; 6Z3QHB00LB; 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine; 5-[bis(morpholin-4-yl)-1,3,5-triazin-2-yl]-4-(trifluoromethyl)pyridin-2-amine; 5-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine; Bimiralisib [INN]; Bimiralisib [USAN]; Bimiralisib [WHO-DD]; NCB5; SCHEMBL1309049; GTPL8383; Bimiralisib free base; ADGGYDAFIHSYFI-UHFFFAOYSA-N; EX-A2018; BCP15887; PQR-309(PI3K-IN-2)
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MOA Inhibitor
Activity Ki = 62 nM
External Link
CID: 58507717
TTD: D0TU7B
DrugBank: DB14846
 Compound Name AZD2014 Phase 2 [18]
Synonyms
1009298-59-2; Vistusertib; AZD-2014; AZD 2014; UNII-0BSC3P4H5X; 0BSC3P4H5X; cc-551; 3-[2,4-Bis((3S)-3-methylmorpholin-4-yl)pyrido[5,6-e]pyrimidin-7-yl]-N-methylbenzamide; CHEMBL2336325; 3-[2,4-Bis((3S)-3-methyLmorpholin-4-yl)pyrido-[5,6-e]pyrimidin-7-yl]-N-methylbenzamide; C25H30N6O3; 3-(2,4-bis((S)-3-methylmorpholino)pyrido[2,3-d]pyrimidin-7-yl)-N-methylbenzamide; 3-[2,4-bis[(3S)-3-methylmorpholin-4-yl]pyrido[2,3-d]pyrimidin-7-yl]-N-methylbenzamide; Vistusertib [INN]; Vistusertib [USAN]; Vistusertib (JAN/INN)
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MOA Inhibitor
Activity IC50 = 2.8 nM
External Link
CID: 25262792
TTD: D0Z2UQ
DrugBank: DB11925
 Compound Name CC-223 Phase 1/2 [19]
Synonyms
GW 791343 HYDROCHLORIDE; GW791343 trihydrochloride; 309712-55-8; 1019779-04-4; GW791343 HCl; GW791343 (trihydrochloride); GW791343; GW-791343; 2-[(3,4-Difluorophenyl)amino]-N-[2-methyl-5-(1-piperazinylmethyl)phenyl]-acetamide trihydrochloride; GW791343 (HCL); GW-791343 hydrochloride; C20H27Cl3F2N4O; GW 791343 Trihydrochloride; C20H24F2N4O.3ClH; CTK8F0044; EX-A438; GW 791343 HCl; WSBRAHWNJBXXJM-UHFFFAOYSA-N; MolPort-023-219-209; BCP23425; AKOS024457596; CS-1030; BCP9000749; API0008007; HY-15470; BCP0726000290; RT-017402; KB-272661
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MOA Modulator
Activity IC50 = 10 nM
External Link
CID: 58298316
TTD: D05EXN
DrugBank: DB12570
 Compound Name BGT226 Phase 1/2 [20]
Synonyms
BGT-226 free base; 915020-55-2; UNII-ZXE7F2GMJJ; BGT226 free base; ZXE7F2GMJJ; BGT-226; 8-(6-Methoxypyridin-3-yl)-3-methyl-1-[4-(piperazin-1-yl)-3-trifluoromethylphenyl]-1,3-dihydroimidazo[4,5-c]quinolin-2-one; CHEBI:71967; BGT 226; NVPBGT226; 8-(6-methoxypyridin-3-yl)-3-methyl-1-[4-(piperazin-1-yl)-3-(trifluoromethyl)phenyl]-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one; 8-(6-Methoxy-pyridin-3-yl)-3-methyl-1-(4-piperazin-1-yl-3-trifluoromethyl-phenyl)-1,3-dihydro-imidazo[4,5-c]quinolin-2-one; NPV-BGT226; SCHEMBL146939
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MOA Modulator
External Link
CID: 11978790
TTD: D0X7IN
 Compound Name ME-344 Phase 1/2 [21]
Synonyms
NV-128; NV-344; MTOR inhibitor (cancer), Novogen; MTOR inhibitors (cancer), Marshall Edwards
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MOA Inhibitor
External Link
CID: 68026984
TTD: D03IXK
DrugBank: DB13062
 Compound Name BI 860585 Phase 1 [22]
MOA Inhibitor
External Link
TTD: D08PSC
 Compound Name LAM-001 Phase 1 [23]
MOA Inhibitor
External Link
TTD: D0QN5M
 Compound Name DS-3078 Phase 1 [24]
MOA Modulator
External Link
TTD: D0R9VX
 Compound Name GDC-0349 Phase 1 [25]
Synonyms
MTORC1/2 inhibitors
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MOA Inhibitor
Activity Ki = 3.8 nM
External Link
CID: 59239165
TTD: D0U8QH
DrugBank: DB13072
 Compound Name CERC 006 Phase 1 [26]
Synonyms
(+/-)-Cyclohexanecarboxylic acid, 4-(4-amino-5-(7-methoxy-1H-indol-2-yl)imidazo(5,1-f)(1,2,4)triazin-7-yl)-, trans-; (1r,4r)-4-(4-Amino-5-(7-methoxy-1H-indol-2-yl)imidazo[5,1-f][1,2,4]triazin-7-yl)cyclohexane-1-carboxylic acid; (1r,4r)-4-(4-amino-5-(7-methoxy-1H-indol-2-yl)imidazo[5,1-f][1,2,4]triazin-7-yl)cyclohexanecarboxylic acid; (1r,4r)-4-(4-Amino-5-(7-methoxy-1H-indol-2-yl)imidazo-[5,1-f][1,2,4]triazin-7-yl)cyclohexanecarboxylic acid; 1187559-66-5; 25MKH1SZ0M; 4-(4-Amino-5-(7-methoxy-1H-indol-2-yl)imidazo[5,1-f] [1,2,4]Triazin-7-yl)cyclohexanecarboxylic Acid; 4-[(5Z)-4-amino-5-(7-methoxyindol-2-ylidene)-1H-imidazo[5,1-f][1,2,4]triazin-7-yl]cyclohexane-1-carboxylic acid; 4-[4-amino-5-(7-methoxy-1H-indol-2-yl)imidazo[5,1-f][1,2,4]triazin-7-yl]cyclohexane-1-carboxylic acid; 4-[4-amino-5-(7-methoxy-2-indolylidene)-1H-imidazo[5,1-f][1,2,4]triazin-7-yl]-1-cyclohexanecarboxylic acid; 936890-98-1; 936890-98-1 (free acid); A-1065; AC-31517; AEVI-006; AKOS030238938; AKOS037643584; AM81260; AS-17003; ASP 7486; ASP4786; ASP7486; ASP-7486; BCP02613; BCP9001034; BDBM185151; BRD-K94294671-003-01-3; CCG-268721; CERC 006; CERC006; CERC-006; CHEBI:91363; CHEMBL2132692; CHEMBL3120215; CS-0257; Cyclohexanecarboxylic acid, 4-(4-amino-5-(7-methoxy-1H-indol-2-yl)imidazo(5,1-f)(1,2,4)triazin-7-yl)-, trans-; Cyclohexanecarboxylic acid, 4-[4-amino-5-(7-methoxy-1h-indol-2-yl)imidazo[5,1-f][1,2,4]triazin-7-yl]-, trans-; DB12387; DTXSID901025951; EX-A143; F17371; HMS3656H05; HMS3748I11; HY-10423; J-523839; JROFGZPOBKIAEW-HAQNSBGRSA-N; LS-14875; MLS006011006; NCGC00250395-01; NCGC00386179-01; NCGC00386179-04; NCGC00387858-03; NSC800810; NSC-800810; OSI 027; OSI027; OSI-027; Q27163231; Q27253978; s2624; SB19259; SCHEMBL20482333; SCHEMBL22594988; SCHEMBL22787096; SCHEMBL976795; SCHEMBL976796; SMR004702804; SW220246-1; trans-4-(4-Amino-5-(7-methoxy-1H-indol-2-yl)imidazo[5,1-f][1,2,4]triazin-7-yl)cyclohexanecarboxylic acid; TRANS-4-[4-AMINO-5-(7-METHOXY-1H-INDOL-2-YL)IMIDAZO[5,1-F][1,2,4]TRIAZIN-7-YL]CYCLOHEXANECARBOXYLIC ACID; trans-4-[4-amino-5-(7-methoxy-1H-indol-2-yl)imidazo[5,1-f][1,2,4]triazin-7-yl]-cyclohexanecarboxylic acid; trans-4-[4-amino-5-(7-methoxy-1H-indol-2-yl)-imidazo[5,1-f][1,2,4]triazin-7-yl]-cyclohexanecarboxylic acid; UNII-25MKH1SZ0M
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MOA Inhibitor
External Link
CID: 135398516
TTD: D1RLY2
DrugBank: DB12387
 Compound Name DS-7423 Phase 1 [27]
MOA Modulator
External Link
TTD: D0X4RT
 Compound Name PWT-33597 Phase 1 [28]
Synonyms
PI3 kinase alpha/mTOR dual inhibitor (cancer), Pathway Therapeutics
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MOA Modulator
External Link
CID: 46917355
TTD: D0Y0FE
 Compound Name VS-5584 Phase 1 [4]
Synonyms
5-(9-Isopropyl-8-methyl-2-morpholino-9H-purin-6-yl)pyrimidin-2-amine; 1246560-33-7; VS-5584 (SB2343); UNII-W71J4X250V; SB-2343; SB2343; CHEMBL3393066; W71J4X250V; 5-(8-methyl-2-morpholin-4-yl-9-propan-2-ylpurin-6-yl)pyrimidin-2-amine; C17H22N8O; QYBGBLQCOOISAR-UHFFFAOYSA-N; SCHEMBL539098; GTPL8382; EX-A288; DTXSID10677328; MolPort-035-757-944; HMS3652B16; BCP08247; 2797AH; ZINC95644685; s7016; VS5584; BDBM50059635; AKOS024465057; 5-(9-isopropyl-8-methyl-2-morpholin-4-yl-9H-purin-6-yl)-pyrimidin-2-ylamine; SB16877
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MOA Modulator
External Link
CID: 46912230
TTD: D0U3DP
DrugBank: DB12986
 Compound Name PMID25726713-Compound-49 Patented [29]
MOA Inhibitor
Activity IC50 < 1 nM
External Link
TTD: D07TVO
 Compound Name PMID25726713-Compound-51 Patented [29]
MOA Inhibitor
Activity IC50 < 1 nM
External Link
TTD: D0KH7Q
 Compound Name PMID25726713-Compound-48 Patented [29]
MOA Inhibitor
Activity IC50 < 1 nM
External Link
TTD: D0WJ3W
 Compound Name PMID25726713-Compound-47 Patented [29]
MOA Inhibitor
Activity IC50 < 1 nM
External Link
TTD: D0X5VI
 Compound Name PMID25726713-Compound-50 Patented [29]
MOA Inhibitor
Activity IC50 < 1 nM
External Link
TTD: D0Y8JF
 Compound Name AZD8055 Discontinued in Phase 1/2 [30]
Synonyms
1009298-09-2; AZD-8055; AZD 8055; [5-[2,4-Bis((3S)-3-methylmorpholin-4-yl)pyrido[2,3-d]pyrimidin-7-yl]-2-methoxyphenyl]methanol; (5-(2,4-bis((S)-3-methylmorpholino)pyrido[2,3-d]pyrimidin-7-yl)-2-methoxyphenyl)methanol; UNII-970JJ37FPW; 970JJ37FPW; CHEMBL1801204; AK109550; (5-(2,4-Bis((S)-3-methylmorpholino)pyrido-[2,3-d]pyrimidin-7-yl)-2-methoxyphenyl)methanol; (5-(2,4-bis((3S)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanol
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 4 nM
External Link
CID: 25262965
TTD: D0K1VK
DrugBank: DB12774
 Compound Name TAFA-93 Discontinued in Phase 1 [31]
Synonyms
MTOR inhibitor, Isotechnika; Rapamycin prodrug, Isotechnika; Transplant rejection therapy, Isotechnika
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 54601137
TTD: D0H5MX
 Compound Name SCR-44001 Terminated [32]
Synonyms
MTOR pathway inhibitors (cancer); PI3K modulators, BioImage; SCR-0044001; SCR-0334654; SCR-0335319; TOP-216; MTOR pathway inhibitors (cancer), TopoTarget; MTOR pathway inhibitors (cancer), BioImage/TopoTarget
    Click to Show/Hide
MOA Inhibitor
External Link
TTD: D05SXC
 Compound Name (4-(6-morpholino-9H-purin-2-yl)phenyl)methanol Investigative [33]
Synonyms
CHEMBL594669; SCHEMBL4442909
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 4500 nM
External Link
CID: 25069592
TTD: D00GQM
 Compound Name Rapamycin complexed with immunophilin FKBP12 Investigative [34]
MOA Inhibitor
External Link
TTD: D01AQN
 Compound Name C-16-(S)-3-methylindolerapamycin Investigative [35]
Synonyms
CHEMBL503885
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 5 nM
External Link
CID: 44576240
TTD: D02TCF
 Compound Name PF-05094037 Investigative [4]
Synonyms
PF-05171310; PF-05181059; MTOR inhibitors (cancer), Pfizer
    Click to Show/Hide
MOA Inhibitor
External Link
TTD: D03XRZ
 Compound Name SX-MTR1 Investigative [4]
Synonyms
MTOR modulators (small peptide mimetics, bladder cancer), Serometrix
    Click to Show/Hide
MOA Modulator
External Link
TTD: D05SOW
 Compound Name 2-(6-morpholino-9H-purin-2-yl)phenol Investigative [33]
MOA Inhibitor
Activity IC50 = 2500 nM
External Link
CID: 135955185
TTD: D07JKB
 Compound Name P-2281 Investigative [4]
Synonyms
MTOR inhibitor (ulcerative colitis), Piramal
    Click to Show/Hide
MOA Inhibitor
External Link
TTD: D07NFT
 Compound Name X-387 Investigative [4]
Synonyms
MTOR inhibitors (cancer), Shanghai Institute of Materia Medica
    Click to Show/Hide
MOA Inhibitor
External Link
TTD: D08BTX
 Compound Name 4-(6-morpholino-9H-purin-2-yl)phenol Investigative [33]
MOA Inhibitor
Activity IC50 = 450 nM
External Link
CID: 135955186
TTD: D09FBN
 Compound Name EM-101 Investigative [4]
Synonyms
EM-100 series; LY-3; LY-303511; MTOR pathway inhibitors (cancer), Emiliem; MTOR pathway inhibitors (cancer), NIH
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 3971
TTD: D09VHS
 Compound Name EC-0845 Investigative [4]
Synonyms
MTOR modulator (inflammatory disease), Endocyte
    Click to Show/Hide
MOA Modulator
External Link
TTD: D0A8ES
 Compound Name 4-(2-(thiophen-2-yl)-9H-purin-6-yl)morpholine Investigative [33]
Synonyms
CHEMBL604876; SCHEMBL4439490
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 2800 nM
External Link
CID: 25074311
TTD: D0AH8Q
 Compound Name SB-2280 Investigative [4]
Synonyms
SB-2602; Selective mTOR inhibitors (cancer); Selective mTOR inhibitors (cancer), S*BIO
    Click to Show/Hide
MOA Inhibitor
External Link
TTD: D0E1YN
 Compound Name 4-(2-(thiophen-3-yl)-9H-purin-6-yl)morpholine Investigative [33]
Synonyms
CHEMBL608095; SCHEMBL4438208
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 3900 nM
External Link
CID: 25074312
TTD: D0F1SI
 Compound Name torin 1 Investigative [36]
Synonyms
Torin-1
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 4.32 nM
External Link
CID: 49836027
TTD: D0H0HR
 Compound Name EC-0565 Investigative [4]
Synonyms
Folate-everolimus conjugate (inflammation), Endocyte
    Click to Show/Hide
MOA Inhibitor
External Link
TTD: D0H4KF
 Compound Name OXA-01 Investigative [4]
Synonyms
MTORC1/mTORC2 inhibitor (cancer) OSI Pharmaceuticals
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 45276387
TTD: D0J9PK
 Compound Name AR-mTOR-26 Investigative [4]
Synonyms
AR-mTOR-1; MTORC1/2 inhibitors (cancer); MTORC1/2 inhibitors (cancer), Array BioPharma
    Click to Show/Hide
MOA Inhibitor
External Link
TTD: D0N9TK
 Compound Name 2-chloro-N-(6-cyanopyridin-3-yl)propanamide Investigative [37]
Synonyms
1112994-35-0; SCHEMBL1483919; CHEMBL446834; VFOLQYOVUCHHET-UHFFFAOYSA-N
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 25141337
TTD: D0P0UV
 Compound Name 3-(6-morpholino-9H-purin-2-yl)phenol Investigative [33]
Synonyms
CHEMBL593515; SCHEMBL4443377; FUDQNOGEMXSUSQ-UHFFFAOYSA-N
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1650 nM
External Link
CID: 16049458
TTD: D0TC5H
 Compound Name AP-21967 Investigative [35]
Synonyms
CHEMBL525042; SCHEMBL18176922; C-16-(S)-7-methylindolerapamycin
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 10 nM
External Link
CID: 44576241
TTD: D0U8GR
 Compound Name 4-(2-(1H-indol-6-yl)-9H-purin-6-yl)morpholine Investigative [33]
Synonyms
CHEMBL611630
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 150 nM
External Link
CID: 46225260
TTD: D0Y1DR
 Compound Name Torin2 Investigative [38]
Synonyms
Torin 2; 1223001-51-1; Torin-2; 9-(6-aminopyridin-3-yl)-1-[3-(trifluoromethyl)phenyl]benzo[h][1,6]naphthyridin-2-one; 9-(6-AMINO-3-PYRIDINYL)-1-[3-(TRIFLUOROMETHYL)PHENYL]-BENZO[H]-1,6-NAPHTHYRIDIN-2(1H)-ONE; CHEMBL1765602; C24H15F3N4O; CHEBI:90682; 9-(6-Aminopyridin-3-Yl)-1-[3-(Trifluoromethyl)phenyl]benzo[h][1,6]naphthyridin-2(1h)-One; 9-(6-AMINOPYRIDIN-3-YL)-1-(3-(TRIFLUOROMETHYL)PHENYL)BENZO[H][1,6]NAPHTHYRIDIN-2(1H)-ONE; 9-(6-Aminopyridin-3-yl)-1-(3-(trifluoromethyl)-phenyl)benzo[h][1,6]naphthyridin-2(1H)-one; BENZO[H]-1,6-NAPHTHYRIDIN-2(1H)-ONE, 9-(6-AMINO-3-PYRIDINYL)-1-[3-(TRIFLUOROMETHYL)PHENYL]-; 9-(6-Amino-3-pyridinyl)-1-[3-(trifluoromethyl)phenyl]benzo[h]-1,6-naphthyridin-2(1H)-one; cc-275; MLS006011167; GTPL8839; SCHEMBL6876328; AOB3537; DTXSID00679917; EX-A431; HMS3265O05; HMS3265O06; HMS3265P05; HMS3265P06; HMS3651N13; BCP02612; ABP000908; BDBM50341209; MFCD18782652; NSC775727; s2817; ZINC71318831; AKOS024458055; CCG-265003; CS-0236; NSC-775727; PB34957; NCGC00263216-01; NCGC00263216-02; NCGC00263216-09; NCGC00263216-13; 9-(6-AMINO-PYRIDIN-3-YL)-1-(3-TRIFLUOROMETHYL-PHENYL)-1H-BENZO[H][1,6]NAPHTHYRIDIN-2-ONE; AC-31520; AK171126; AS-74405; HY-13002; SMR004702936; AB0035864; DB-084736; FT-0700124; SW218309-2; Y0293; Q-4148; J-519481; BRD-K68174511-001-01-7; Q27089008; 9-(6-amino-3-pyridyl)-1-[3-(trifluoromethyl)phenyl]benzo[h][1,6]naphthyridin-2-one; 17G; 9-(6-Amino-3-pyridinyl)-1-[3-(trifl uoromethyl)phenyl]-benzo[h]-1,6-naphthyridin-2(1H) -one; 9-(6-AMINOPYRIDIN-3-YL)-1-[3-(TRIFLUOROMETHYL)PHENYL]-1H,2H-BENZO[H]1,6-NAPHTHYRIDIN-2-ONE
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 51358113
TTD: D2B7WM
 Compound Name HM-5016699 Investigative [4]
Synonyms
Dual PI3K/mTOR inhibitor (cancer); Dual PI3K/mTOR inhibitor (cancer), Hutchison
    Click to Show/Hide
MOA Inhibitor
External Link
TTD: D02ELN
 Compound Name PF-03772304 Investigative [39]
Synonyms
MTOR inhibitors, Biotica; MTOR inhibitors, Wyeth; PF-04979064; PF-05017255; PF-05168899; WYE-125132; WYE-132; WYE-178; WYE-354; WYE-600; WYE-687; Imidazolo and pyrazolopyrimidine derivatives (cancer), Pfizer; Imidazolopyrimidine derivatives (cancer), Pfizer; Imidazolopyrimidine derivatives (cancer), Wyeth; Non-rapamycin mTOR/PI3K inhibitors (cancer); PI3K/mTOR signalling inhibitors (cancer), Wyeth; Non-rapamycin mTOR/PI3K inhibitors (cancer), Pfizer; 5H-pyrrolo[3,2-d]pyridimine analogs (cancer), Wyeth
    Click to Show/Hide
MOA Inhibitor
External Link
TTD: D05RSS
 Compound Name PP-242 Investigative [40]
Synonyms
PP242; TORKinib
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 8 nM
External Link
CID: 135565635
TTD: D0H2CM
 Compound Name CU-906 Investigative [4]
MOA Inhibitor
External Link
TTD: D0JD4S
 Compound Name P-6915 Investigative [4]
Synonyms
PI3K/mTOR inhibitors (cancer), Piramal
    Click to Show/Hide
MOA Inhibitor
External Link
TTD: D0QE9F
 Compound Name 2-Morpholin-4-yl-pyrimido[2,1-a]isoquinolin-4-one Investigative [41]
Synonyms
Compound 401; 168425-64-7; 2-morpholino-4H-pyrimido[2,1-a]isoquinolin-4-one; 2-(morpholin-4-yl)pyrimido[2,1-a]isoquinolin-4-one; CHEMBL179242; 2-(4-MORPHOLINYL)-4H-PYRIMIDO[2,1-A]ISOQUINOLIN-4-ONE; Compound401; SCHEMBL10092321; KS-00001DEG; CTK4D2994; DTXSID20434626; MolPort-023-276-726; HMS3229D15; EX-A1016; BCP04303; BDBM50159620; ZINC13608047; AKOS016369524; CS-5624; NCGC00378805-02; HY-19341; KB-224235; M2537; B7337; S-7713; J-010456
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 5300 nM
External Link
CID: 10039361
TTD: D0T0BY
 Compound Name 2-(2-Methyl-morpholin-4-yl)-benzo[h]chromen-4-one Investigative [41]
Synonyms
CHEMBL435507; SCHEMBL3545107
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 4800 nM
External Link
CID: 10017389
TTD: D0X7TB
 Compound Name Ethyl 1-[(1H-benzimidazol-2(3H)one-5-yl)sulfonyl]-1H-pyrrole-2-carboxylate Investigative [41]
Synonyms
2-(Morpholin-4-yl)-benzo[h]chromen-4-one; 154447-35-5; NU7026; NU 7026; DNA-PK Inhibitor II; NU-7026; 2-morpholino-4H-benzo[h]chromen-4-one; LY293646; LY-293646; 2-(4-Morpholinyl)-4H-naphthol[1,2-b]pyran-4-one; 2-(4-morpholinyl)-4H-naphtho[1,2-b]pyran-4-one; CHEMBL104468; AK186905; DNA-Dependent Protein Kinase Inhibitor II; 2-morpholin-4-ylbenzo[h]chromen-4-one; SCHEMBL610237; ZINC9230; GTPL5959; KS-00000XHI; CTK0E7833; CHEBI:92165; DTXSID10432010; AOB2835; MolPort-009-019-548; HMS3229C11; EX-A1100; BCP04736; IN1364; s2893
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 6400 nM
External Link
CID: 9860529
TTD: D0W1ST
 Compound Name PP121 Investigative [40]
Synonyms
PP-121; PP 121
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 10 nM
External Link
CID: 24905142
TTD: D03EHM
DrugBank: DB08052
2C25: Lung cancer 52 Compound(s) Regulating the Disease Click to Show/Hide the Full List
 Compound Name Adagrasib Approved [42]
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
CID: 138611145
TTD: DUQV41
 Compound Name Amivantamab Approved [43]
External Link
TTD: DQ5X1Z
 Compound Name Mobocertinib Approved [44]
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
CID: 118607832
TTD: DI4HA7
 Compound Name Sugemalimab Approved in China [45]
External Link
TTD: DDZ48Y
 Compound Name Sacituzumab govitecan Approved [46]
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
CID: 91668186
TTD: D8LAE2
 Compound Name Atezolizumab Approved [47]
External Link
TTD: D0YM2K
 Compound Name Tepotinib Approved [48]
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
CID: 25171648
TTD: D0R8QG
DrugBank: DB15133
 Compound Name Sotorasib Approved [49]
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
CID: 137278711
TTD: D0R7LD
DrugBank: DB15569
 Compound Name Entrectinib Approved [50]
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
CID: 25141092
TTD: D0O0LS
DrugBank: DB11986
 Compound Name Repotrectinib Approved [51]
Synonyms
FIKPXCOQUIZNHB-RRKGBCIJSA-N; SCHEMBL20438940; TPX 0005; BCP19778
    Click to Show/Hide
External Link
CID: 135565923
TTD: D05NFR
 Compound Name MYL-1402O Phase 3 [52]
Synonyms
bevacizumab biosimilar
    Click to Show/Hide
External Link
TTD: DYH3Q6
 Compound Name AB154 Phase 3 [53]
Synonyms
Domvanalimab
    Click to Show/Hide
External Link
TTD: DT1FS0
 Compound Name Datopotamab deruxtecan Phase 3 [54]
External Link
TTD: DP41HV
 Compound Name CS1001 Phase 3 [55]
External Link
TTD: D3MP1S
 Compound Name JDQ443 Phase 3 [56]
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
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External Link
CID: 156501355
TTD: D37IQM
 Compound Name TRS003 Phase 3 [57]
External Link
TTD: D2KVG4
 Compound Name Tusamitamab ravtansine Phase 3 [58]
Synonyms
SAR408701
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External Link
TTD: D2D6NJ
 Compound Name RG6058 Phase 3 [59]
Synonyms
Tiragolumab
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External Link
TTD: D0L4VD
 Compound Name GSK4069889 Phase 2 [60]
Synonyms
TSR-022
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External Link
TTD: DZW53X
 Compound Name APL-101 Phase 2 [61]
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
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External Link
CID: 72202701
TTD: DV3Y7F
 Compound Name SGN-LIV1A Phase 2 [62]
Synonyms
Ladiratuzumab Vedotin
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TTD: DS6B1L
 Compound Name BNT116 Phase 2 [63]
External Link
TTD: DR39GZ
 Compound Name AZD7789 Phase 2 [64]
External Link
TTD: DNI7E3
 Compound Name L-DOS47 Phase 1/2 [65]
External Link
TTD: DN3Z5D
 Compound Name NC318 Phase 2 [66]
External Link
TTD: D9UZ5Q
 Compound Name Vorolanib Phase 2 [67]
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-
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CID: 59215954
TTD: D8AG3S
DrugBank: DB15247
 Compound Name Xofigo Phase 2 [68]
External Link
TTD: D6B7FP
 Compound Name Bintrafusp alfa Phase 2 [69]
External Link
TTD: D5J3BL
 Compound Name Voyager-V1 Phase 2 [70]
Synonyms
VSV-IFNBeta-NIS
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External Link
TTD: D4AGB6
 Compound Name AB-106 Phase 2 [71]
Synonyms
DS6051b; GTPL11198; AB106
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External Link
CID: 154699459
TTD: D2KV8B
 Compound Name RO-5126766 Phase 2 [72]
Synonyms
VS-6766; CH-5126766; Dual Raf/MEK protein kinase inhibitor (cancer), Roche
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External Link
CID: 16719221
TTD: D0M6BD
DrugBank: DB15254
 Compound Name TC-210 Phase 1/2 [73]
External Link
TTD: DX6O9V
 Compound Name EMB-01 Phase 1/2 [74]
External Link
TTD: DWQ6J1
 Compound Name NM21-1480 Phase 1/2 [75]
External Link
TTD: DUVH60
 Compound Name MRx0518 Phase 1/2 [76]
External Link
TTD: DP4J2K
 Compound Name DZD9008 Phase 1/2 [77]
External Link
TTD: DM8Y2N
 Compound Name BGB-A425 Phase 1/2 [78]
External Link
TTD: D7UIZ1
 Compound Name Rilvegostomig Phase 1/2 [79]
Synonyms
AZD2936
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External Link
TTD: D4RMC9
 Compound Name IK-007 Phase 1/2 [80]
Synonyms
grapiprant
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External Link
TTD: D1KES8
 Compound Name IBI318 Phase 1 [81]
External Link
TTD: DX30BA
 Compound Name GEN-011 Phase 1 [82]
External Link
TTD: DR1YQ7
 Compound Name ENV-105 Phase 1 [83]
Synonyms
Carotuximab
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External Link
TTD: DQ8K3R
 Compound Name AMG 160 Phase 1 [84]
External Link
TTD: DOY4E6
 Compound Name ADP-A2M10 Phase 1 [85]
External Link
TTD: DM38KC
 Compound Name MEDI5752 Phase 1 [86]
External Link
TTD: D7L1MP
 Compound Name PF-07104091 Phase 1 [87]
External Link
TTD: D5TH2B
 Compound Name PF-06936308 Phase 1 [88]
External Link
TTD: D2LUK7
 Compound Name GEM3PSCA Phase 1 [89]
External Link
TTD: D1L7DE
 Compound Name PF-07257876 Phase 1 [90]
External Link
TTD: D1A7OP
 Compound Name Cosibelimab Phase 1 [91]
Synonyms
CK-301/TG-1501
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External Link
TTD: D17URP
 Compound Name Gemcitabine Approved [92]
External Link
CID: 60750
TTD: D0AJ3K
DrugBank: DB00441
 Compound Name SMI-4a Investigative [93]
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
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CID: 1361334
TTD: DAJ3D2
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