m6A-centered Crosstalk Information
Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
| Crosstalk ID |
M6ACROT03500
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[1], [2] | |||
Histone modification
H3K18la
Epigenetic Regulator
METTL14
Direct
Enhancement
m6A modification
MTOR
MTOR
METTL14
Methylation
: m6A sites
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| m6A Modification: | |||||
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| m6A Regulator | Methyltransferase-like 14 (METTL14) | WRITER | |||
| m6A Target | Serine/threonine-protein kinase mTOR (MTOR) | ||||
| Epigenetic Regulation that have Cross-talk with This m6A Modification: | |||||
| Epigenetic Regulation Type | Histone modification (HistMod) | ||||
| Regulated Target | Histone H3 lysine 18 lactylation (H3K18la) | View Details | |||
| Downstream Gene | METTL14 | View Details | |||
| Crosstalk Relationship | Histone modification → m6A | Enhancement | |||
| Crosstalk Mechanism | Histone modification directly impacts m6A modification through modulating the level of m6A regulator | ||||
| Crosstalk Summary | Histone H3 lysine 18 lactylation (H3K18la) was found to upregulate METTL14 expression. In conclusion, METTL14 knockdown promotes stemness in GC by mediating m6A modification of ATF5 mRNA, which activates the WDR74/beta-catenin axis, making METTL14 a potential therapeutic target for gastric cancer treatment. The m6A modification level was decreased in GC and METTL14 was a key regulator resulting in m6A disorder in GC. METTL14 overexpression suppressed GC cell proliferation and aggression by deactivating the PI3K/AKT/Serine/threonine-protein kinase mTOR (MTOR) pathway and the EMT pathway, respectively. | ||||
| Responsed Disease | Gastric cancer | ICD-11: 2B72 | |||
In-vitro Model |
GES-1 | Normal | Homo sapiens | CVCL_EQ22 | |
| SGC-7901 | Gastric carcinoma | Homo sapiens | CVCL_0520 | ||
| MGC-803 | Gastric mucinous adenocarcinoma | Homo sapiens | CVCL_5334 | ||
Full List of Potential Compound(s) Related to This m6A-centered Crosstalk
| Serine/threonine-protein kinase mTOR (MTOR) | 72 Compound(s) Regulating the Target | Click to Show/Hide the Full List | ||
| Novolimus | Approved | [3] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| Temsirolimus | Approved | [4] | ||
| Synonyms |
Torisel
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| MOA | Inhibitor | |||
| Activity | IC50 = 1760 nM | |||
| External Link | ||||
| Everolimus | Approved | [5] | ||
| 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 | ||||
| Zotarolimus | Approved | [6] | ||
| Synonyms |
Abt-578; Zotarolimus (TN)
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| MOA | Modulator | |||
| Activity | IC50 = 3.3 nM | |||
| External Link | ||||
| Sirolimus | Approved | [7] | ||
| 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 | ||||
| PF-04449913 | Approved | [8] | ||
| 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 | ||||
| Ridaforolimus | Phase 3 | [9] | ||
| Synonyms |
Deforolimus; AP 23573; MK 8669; AP-23573; MK-8669; AP23573, MK-8669, Ridaforolimus, Deforolimus
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| MOA | Inhibitor | |||
| External Link | ||||
| INK128 | Phase 2 | [10] | ||
| 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 | ||||
| OSI-027 | Phase 2 | [11] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| ABI-009 | Phase 2 | [12] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| Salirasib | Discontinued in Phase 1/2 | [3] | ||
| 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 | ||||
| SAR245409 | Phase 2 | [3] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 157 nM | |||
| External Link | ||||
| SF1126 | Phase 2 | [12] | ||
| 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 | ||||
| PF-05212384 | Phase 2 | [13] | ||
| 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 | ||||
| LY3023414 | Phase 2 | [14] | ||
| MOA | Modulator | |||
| External Link | ||||
| PF-04691502 | Phase 2 | [15] | ||
| 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 | ||||
| GDC-0980/RG7422 | Phase 2 | [3] | ||
| 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 | |||
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| BEZ235 | Phase 2 | [16] | ||
| 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 | |||
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| MM-141 | Phase 2 | [12] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PQR309 | Phase 2 | [3] | ||
| 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 | ||||
| AZD2014 | Phase 2 | [17] | ||
| 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 | |||
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| CC-223 | Phase 1/2 | [18] | ||
| 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 | |||
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| BGT226 | Phase 1/2 | [19] | ||
| 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 | |||
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| ME-344 | Phase 1/2 | [20] | ||
| Synonyms |
NV-128; NV-344; MTOR inhibitor (cancer), Novogen; MTOR inhibitors (cancer), Marshall Edwards
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| MOA | Inhibitor | |||
| External Link | ||||
| BI 860585 | Phase 1 | [21] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| LAM-001 | Phase 1 | [22] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| DS-3078 | Phase 1 | [23] | ||
| MOA | Modulator | |||
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| GDC-0349 | Phase 1 | [24] | ||
| Synonyms |
MTORC1/2 inhibitors
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| MOA | Inhibitor | |||
| Activity | Ki = 3.8 nM | |||
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| CERC 006 | Phase 1 | [25] | ||
| 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 | |||
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| DS-7423 | Phase 1 | [26] | ||
| MOA | Modulator | |||
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| PWT-33597 | Phase 1 | [27] | ||
| Synonyms |
PI3 kinase alpha/mTOR dual inhibitor (cancer), Pathway Therapeutics
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| MOA | Modulator | |||
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| VS-5584 | Phase 1 | [3] | ||
| 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 | |||
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| PMID25726713-Compound-49 | Patented | [28] | ||
| MOA | Inhibitor | |||
| Activity | IC50 < 1 nM | |||
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| PMID25726713-Compound-51 | Patented | [28] | ||
| MOA | Inhibitor | |||
| Activity | IC50 < 1 nM | |||
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| PMID25726713-Compound-48 | Patented | [28] | ||
| MOA | Inhibitor | |||
| Activity | IC50 < 1 nM | |||
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| PMID25726713-Compound-47 | Patented | [28] | ||
| MOA | Inhibitor | |||
| Activity | IC50 < 1 nM | |||
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| PMID25726713-Compound-50 | Patented | [28] | ||
| MOA | Inhibitor | |||
| Activity | IC50 < 1 nM | |||
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| AZD8055 | Discontinued in Phase 1/2 | [29] | ||
| 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
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| MOA | Inhibitor | |||
| Activity | IC50 = 4 nM | |||
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| TAFA-93 | Discontinued in Phase 1 | [30] | ||
| Synonyms |
MTOR inhibitor, Isotechnika; Rapamycin prodrug, Isotechnika; Transplant rejection therapy, Isotechnika
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| MOA | Inhibitor | |||
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| SCR-44001 | Terminated | [31] | ||
| 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
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| MOA | Inhibitor | |||
| External Link | ||||
| (4-(6-morpholino-9H-purin-2-yl)phenyl)methanol | Investigative | [32] | ||
| Synonyms |
CHEMBL594669; SCHEMBL4442909
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| MOA | Inhibitor | |||
| Activity | IC50 = 4500 nM | |||
| External Link | ||||
| Rapamycin complexed with immunophilin FKBP12 | Investigative | [33] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| C-16-(S)-3-methylindolerapamycin | Investigative | [34] | ||
| Synonyms |
CHEMBL503885
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| MOA | Inhibitor | |||
| Activity | IC50 = 5 nM | |||
| External Link | ||||
| PF-05094037 | Investigative | [3] | ||
| Synonyms |
PF-05171310; PF-05181059; MTOR inhibitors (cancer), Pfizer
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| MOA | Inhibitor | |||
| External Link | ||||
| SX-MTR1 | Investigative | [3] | ||
| Synonyms |
MTOR modulators (small peptide mimetics, bladder cancer), Serometrix
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| MOA | Modulator | |||
| External Link | ||||
| 2-(6-morpholino-9H-purin-2-yl)phenol | Investigative | [32] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 2500 nM | |||
| External Link | ||||
| P-2281 | Investigative | [3] | ||
| Synonyms |
MTOR inhibitor (ulcerative colitis), Piramal
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| MOA | Inhibitor | |||
| External Link | ||||
| X-387 | Investigative | [3] | ||
| Synonyms |
MTOR inhibitors (cancer), Shanghai Institute of Materia Medica
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| MOA | Inhibitor | |||
| External Link | ||||
| 4-(6-morpholino-9H-purin-2-yl)phenol | Investigative | [32] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 450 nM | |||
| External Link | ||||
| EM-101 | Investigative | [3] | ||
| Synonyms |
EM-100 series; LY-3; LY-303511; MTOR pathway inhibitors (cancer), Emiliem; MTOR pathway inhibitors (cancer), NIH
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| MOA | Inhibitor | |||
| External Link | ||||
| EC-0845 | Investigative | [3] | ||
| Synonyms |
MTOR modulator (inflammatory disease), Endocyte
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| MOA | Modulator | |||
| External Link | ||||
| 4-(2-(thiophen-2-yl)-9H-purin-6-yl)morpholine | Investigative | [32] | ||
| Synonyms |
CHEMBL604876; SCHEMBL4439490
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| MOA | Inhibitor | |||
| Activity | IC50 = 2800 nM | |||
| External Link | ||||
| SB-2280 | Investigative | [3] | ||
| Synonyms |
SB-2602; Selective mTOR inhibitors (cancer); Selective mTOR inhibitors (cancer), S*BIO
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| MOA | Inhibitor | |||
| External Link | ||||
| 4-(2-(thiophen-3-yl)-9H-purin-6-yl)morpholine | Investigative | [32] | ||
| Synonyms |
CHEMBL608095; SCHEMBL4438208
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| MOA | Inhibitor | |||
| Activity | IC50 = 3900 nM | |||
| External Link | ||||
| torin 1 | Investigative | [35] | ||
| Synonyms |
Torin-1
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| MOA | Inhibitor | |||
| Activity | IC50 = 4.32 nM | |||
| External Link | ||||
| EC-0565 | Investigative | [3] | ||
| Synonyms |
Folate-everolimus conjugate (inflammation), Endocyte
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| MOA | Inhibitor | |||
| External Link | ||||
| OXA-01 | Investigative | [3] | ||
| Synonyms |
MTORC1/mTORC2 inhibitor (cancer) OSI Pharmaceuticals
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| MOA | Inhibitor | |||
| External Link | ||||
| AR-mTOR-26 | Investigative | [3] | ||
| Synonyms |
AR-mTOR-1; MTORC1/2 inhibitors (cancer); MTORC1/2 inhibitors (cancer), Array BioPharma
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| MOA | Inhibitor | |||
| External Link | ||||
| 2-chloro-N-(6-cyanopyridin-3-yl)propanamide | Investigative | [36] | ||
| Synonyms |
1112994-35-0; SCHEMBL1483919; CHEMBL446834; VFOLQYOVUCHHET-UHFFFAOYSA-N
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| MOA | Inhibitor | |||
| External Link | ||||
| 3-(6-morpholino-9H-purin-2-yl)phenol | Investigative | [32] | ||
| Synonyms |
CHEMBL593515; SCHEMBL4443377; FUDQNOGEMXSUSQ-UHFFFAOYSA-N
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| MOA | Inhibitor | |||
| Activity | IC50 = 1650 nM | |||
| External Link | ||||
| AP-21967 | Investigative | [34] | ||
| Synonyms |
CHEMBL525042; SCHEMBL18176922; C-16-(S)-7-methylindolerapamycin
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| MOA | Inhibitor | |||
| Activity | IC50 = 10 nM | |||
| External Link | ||||
| 4-(2-(1H-indol-6-yl)-9H-purin-6-yl)morpholine | Investigative | [32] | ||
| Synonyms |
CHEMBL611630
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| MOA | Inhibitor | |||
| Activity | IC50 = 150 nM | |||
| External Link | ||||
| Torin2 | Investigative | [37] | ||
| 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
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| MOA | Inhibitor | |||
| External Link | ||||
| HM-5016699 | Investigative | [3] | ||
| Synonyms |
Dual PI3K/mTOR inhibitor (cancer); Dual PI3K/mTOR inhibitor (cancer), Hutchison
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| MOA | Inhibitor | |||
| External Link | ||||
| PF-03772304 | Investigative | [38] | ||
| 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
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| MOA | Inhibitor | |||
| External Link | ||||
| PP-242 | Investigative | [39] | ||
| Synonyms |
PP242; TORKinib
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| MOA | Inhibitor | |||
| Activity | IC50 = 8 nM | |||
| External Link | ||||
| CU-906 | Investigative | [3] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| P-6915 | Investigative | [3] | ||
| Synonyms |
PI3K/mTOR inhibitors (cancer), Piramal
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| MOA | Inhibitor | |||
| External Link | ||||
| 2-Morpholin-4-yl-pyrimido[2,1-a]isoquinolin-4-one | Investigative | [40] | ||
| 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
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| MOA | Inhibitor | |||
| Activity | IC50 = 5300 nM | |||
| External Link | ||||
| 2-(2-Methyl-morpholin-4-yl)-benzo[h]chromen-4-one | Investigative | [40] | ||
| Synonyms |
CHEMBL435507; SCHEMBL3545107
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| MOA | Inhibitor | |||
| Activity | IC50 = 4800 nM | |||
| External Link | ||||
| Ethyl 1-[(1H-benzimidazol-2(3H)one-5-yl)sulfonyl]-1H-pyrrole-2-carboxylate | Investigative | [40] | ||
| 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
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| MOA | Inhibitor | |||
| Activity | IC50 = 6400 nM | |||
| External Link | ||||
| PP121 | Investigative | [39] | ||
| Synonyms |
PP-121; PP 121
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| MOA | Inhibitor | |||
| Activity | IC50 = 10 nM | |||
| External Link | ||||
| 2B72: Gastric cancer | 81 Compound(s) Regulating the Disease | Click to Show/Hide the Full List | ||
| Leniolisib | Approved | [41] | ||
| Synonyms |
1354690-24-6; Leniolisib free base; UNII-L22772Z9CP; (S)-1-(3-((6-(6-methoxy-5-(trifluoromethyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yl)amino)pyrrolidin-1-yl)propan-1-one; L22772Z9CP; 1354690-24-6 (free base); leniolisib(CDZ 173); CDZ173; CDZ-173; 1-[(3S)-3-[[6-[6-methoxy-5-(trifluoromethyl)pyridin-3-yl]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-4-yl]amino]pyrrolidin-1-yl]propan-1-one; Leniolisib [INN]; Leniolisib (CDZ173); Leniolisib (USAN/INN); CDZ173-NX; SCHEMBL323054; GTPL9424; CHEMBL3643413; BDBM118299; EX-A2854; MFCD30470232; s8752; ZB1510; CS-7524; DC22326; SB18839; Example 67 [WO2012004299]; 1-{(S)-3-[6-(6-methoxy-5-trifluoromethyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-y; 1-{(S)-3-[6-(6-methoxy-5-trifluoromethyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-ylamino]-pyrrolidin-1-yl}-propan-1-one; AS-56217; HY-17635; A16796; D11158; US8653092, 67; Q27282602; 1-Propanone, 1-((3S)-3-((5,6,7,8-tetrahydro-6-(6-methoxy-5-(trifluoromethyl)-3-pyridinyl)pyrido(4,3-d)pyrimidin-4-yl)amino)-1-pyrrolidinyl)-; 9NQ
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| Atezolizumab | Approved | [12] | ||
| External Link | ||||
| Bavencio | Approved | [12] | ||
| External Link | ||||
| Tebentafusp | Approved | [42] | ||
| External Link | ||||
| Merimepodib | Approved | [43] | ||
| Synonyms |
Merimebodib; Merimepodib [USAN:INN]; Tyverb/Tykerb; MMPD; 198821-22-6; 2ZL2BA06FU; C23H24N4O6; CHEMBL304087; MERIMEPODIB, VI-21497, VX-497; UNII-2ZL2BA06FU; VI-21497; VX-497; VX497; Vx 497; carbamic acid
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| External Link | ||||
| Taxol | Approved | [22] | ||
| Synonyms |
C47H51NO14; weekly paclitaxel; Micellar Paclitaxel; Paclitaxel [USAN:INN:BAN]; SCHEMBL15000506; Benzenepropanoic acid, beta-(benzoylamino)-alpha-hydroxy-, 6,12b-bis(acetyloxy)-12-(benzoyloxy)-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-4,11-dihydroxy-4a,8,13,13-tetramethyl-5-oxo-7,11-methano-1H-cyclodeca(3,4)benz(1,2-b)oxet-9-yl ester, (2aR-(2aalpha,4beta,4abeta,6beta,9alpha(alphaR*,betaS*),11alpha,12alpha,12aalpha,12balpha))-
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| Ramucirumab | Approved | [44] | ||
| Synonyms |
LY3009806
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| Tucatinib | Approved | [45] | ||
| Synonyms |
Irbinitinib; 937263-43-9; ONT-380; UNII-234248D0HH; 234248D0HH; N6-(4,4-Dimethyl-4,5-dihydrooxazol-2-yl)-N4-(3-methyl-4-((1,2,4)triazolo(1,5-a)pyridin-7-yloxy)phenyl)quinazoline-4,6-diamine; 4,6-Quinazolinediamine, N6-(4,5-dihydro-4,4-dimethyl-2-oxazolyl)-N4-(3-methyl-4-((1,2,4)triazolo(1,5-a)pyridin-7-yloxy)phenyl)-; ONT 380; 4,6-QuinazolinediaMine, N6-(4,5-dihydro-4,4-diMethyl-2-oxazolyl)-N4-[3-Methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)phenyl]-; Tucatinib [USAN:INN]; 6-DIAMINE
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| Antacids | Approved | [46] | ||
| External Link | ||||
| Trastuzumab | Approved | [12] | ||
| Synonyms |
Herceptin; Herceptin (TN); Trastuzumab (INN); Trastuzumab (genetical recombination); Trastuzumab (genetical recombination) (JAN); Trastuzumab (ERBB2 mAb inhibitor)
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| Carbamazepine | Phase 3 | [47] | ||
| Synonyms |
Carbamazepine (iv, epilepsy); Carbamazepine (iv, epilepsy), Lundbeck; Carbamazepine (iv, epilepsy), Ovation Pharmaceuticals
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| Margetuximab | Approved | [12] | ||
| External Link | ||||
| Nivolumab | Approved | [12] | ||
| External Link | ||||
| GRANITE | Phase 3 | [48] | ||
| Synonyms |
Penoxsulam; 219714-96-2; 2-(2,2-difluoroethoxy)-N-(5,8-dimethoxy-[1,2,4]triazolo[1,5-c]pyrimidin-2-yl)-6-(trifluoromethyl)benzenesulfonamide; UNII-784ELC1SCZ; 784ELC1SCZ; CHEBI:81776; 2-(2,2-difluoroethoxy)-n-(5,8-dimethoxy[1,2,4]triazolo[1,5-c]pyrimidin-2-yl)-6-(trifluoromethyl)benzenesulfonamide; Penoxsulam [ISO]; PXD; DSSTox_CID_14803; DSSTox_RID_79204; DSSTox_GSID_34803; SCHEMBL116968; CHEMBL1895913; DTXSID0034803; HSDB 7887; AMY12535; BCP18718; EBD18529; Tox21_301010; MFCD07363876; ZINC13827750; AKOS025401685; NCGC00163715-01; NCGC00163715-02; NCGC00163715-03; NCGC00254912-01; AC-24494; Penoxsulam 100 microg/mL in Acetonitrile; CAS-219714-96-2; FT-0696708; Penoxsulam, PESTANAL(R), analytical standard; C18481; Q22808507; 2-(2,2-Difluoroethoxy)-6-trifluoromethyl-N-(5, 8-dimethoxy[1,2,4]triazolo[1,5-c]pyrimidin-2-yl)benzenesulfonamide; 2-(2,2-Difluoroethoxy)-N-(5,8-dimethoxy[1,2,4]-triazolo[1,5-c]pyrimidin-2-yl)-6-(trifluoromethyl)benzenesulfonamide; 2-(2,2-difluoroethoxy)-N-{5,8-dimethoxy-[1,2,4]triazolo[1,5-c]pyrimidin-2-yl}-6-(trifluoromethyl)benzene-1-sulfonamide; 2-(2,2-difluoroethyl)-N-(5,8-dimethoxy[1,2,4]triazolo[1,5-c]pyrimidin-2-yl)-6-(trifluoromethyl)benzenesulfonamide; Benzenesulfonamide, 2-(2,2-difluoroethoxy)-N-(5,8-dimethoxy(1,2,4)triazolo(1,5-c)pyrimidin-2-yl)-6-(trifluoromethyl)-
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| Zolbetuximab | Phase 3 | [49] | ||
| Synonyms |
IMAB362
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| Tusamitamab ravtansine | Phase 3 | [50] | ||
| Synonyms |
SAR408701
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| Andecaliximab | Phase 3 | [51] | ||
| External Link | ||||
| ABP 980 | Phase 3 | [52] | ||
| External Link | ||||
| GS-5745 | Phase 3 | [22] | ||
| External Link | ||||
| S-1 | Phase 3 | [53] | ||
| Synonyms |
Ciprofibrate-coa; Ciprofibrate-coenzyme A; Coenzyme A, ciprofibrate-; AC1L4TRG; AC1Q3T4H; 111900-25-5; s-{1-[(2r,3s,4r,5r)-5-(6-amino-9h-purin-9-yl)-4-hydroxy-3-(phosphonooxy)tetrahydrofuran-2-yl]-3,5,9-trihydroxy-8,8-dimethyl-3,5-dioxido-10,14-dioxo-2,4,6-trioxa-11,15-diaza-3; E5,5; E5-diphosphaheptadecan-17-yl} 2-[4-(2,2-dichlorocyclopropyl)phenoxy]-2-methylpropanethioate(non-preferred name); Coenzyme A, S-(2-(4-(2,2-dichlorocyclopropyl)phenoxy)-2-methylpropanoate)
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| Lonsurf | Phase 3 | [12] | ||
| External Link | ||||
| GDC-0068 | Phase 3 | [22] | ||
| Synonyms |
RG7440
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| Edotecarin | Phase 3 | [54] | ||
| Synonyms |
ED-749; Edotecarin < Prop INN; J-107088; PF-804950; 12-(beta-D-Glucopyranosyl)-2,10-dihydroxy-6-[2-hydroxy-1-(hydroxymethyl)ethylamino]-6,7,12,13-tetrahydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7-dione
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| RG3638 | Phase 3 | [55] | ||
| Synonyms |
Onartuzumab
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| G17DT | Phase 3 | [56] | ||
| Synonyms |
Gastrimmune; Insegia
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| DE-766 | Phase 3 | [57] | ||
| External Link | ||||
| Tesetaxel | Phase 2 | [58] | ||
| Synonyms |
DJ-927; 333754-36-2; UNII-UG97LO5M8Y; UG97LO5M8Y; Tesetaxel [INN]; DJ927; DJ 927; CHEMBL2107787; SCHEMBL12060837; DB12019; Z-3104; (2AS,2BR,3S,4S,6S,8AR,10R,11AS,11BR,13AR)-2A-ACETOXY-6-(((2R,3S)-3-((TERT-BUTOXYCARBONYL)AMINO)-3-(3-FLUOROPYRIDIN-2-YL)-2-HYDROXYPROPANOYL)OXY)-10-((DIMETHYLAMINO)METHYL)-4-HYDROXY-7,11B,14,14-TETRAMETHYL-2A,2B,3,4,5,6,8A,11A,11B,12,13,13A-DODECAHYDRO-2H-4,8-METHANOOXETO[3'',2'':3',4']BENZO[1',2':3,4]CYCLODECA[1,2-D][1,3]DIOXOL-3-YL BENZOATE
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| Nelipepimut S | Phase 3 | [59] | ||
| Synonyms |
E75
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| BMS-986205 | Phase 3 | [12] | ||
| Synonyms |
KRTIYQIPSAGSBP-KLAILNCOSA-N; 1923833-60-6; BMS986205; UNII-0A7729F42K; 0A7729F42K; GTPL9707; SCHEMBL18826792; SCHEMBL17740982; SCHEMBL19105151; EX-A2606; AKOS032954040; HY-101560; CS-0021719; Q29213697; (R)-N-(4-chlorophenyl)-2-((1s,4S)-4-(6-fluoroquinolin-4-yl)cyclohexyl)propanamide; (2R)-N-(4-chlorophenyl)-2-[4-(6-fluoroquinolin-4-yl)cyclohexyl]propanamide; (2R)-N-(4-Chlorophenyl)-2-(4-(6-fluoro-4-quinolyl)cyclohexyl)propanamide, cis; Cyclohexaneacetamide, N-(4-chlorophenyl)-4-(6-fluoro-4-quinolinyl)-alpha-methyl-, cis-(alphaR)-
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| Rivoceranib | Phase 3 | [12] | ||
| External Link | ||||
| Claudiximab | Phase 3 | [12] | ||
| Synonyms |
IMAB-362; Anti-GC182 mAbs (cancer), Ganymed; Anti-GC182 monoclonal antibodies (cancer), Ganymed; Anti-CLDN18-2 mAbs (cancer), Ganymed; Anti-CLDN18-2 monoclonal antibodies (cancer), Ganymed
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| OS-440 | Phase 3 | [60] | ||
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CNS modulator (spasticity), Osmotica
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| Oraxol | Phase 3 | [12] | ||
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| ICI 118,551 | Phase 3 | [22] | ||
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Ici 118551; (2R,3S)-1-[(7-methyl-2,3-dihydro-1H-inden-4-yl)oxy]-3-(propan-2-ylamino)butan-2-ol; CHEMBL198059; CHEBI:73289; ICI-118551; ICI118551; erythro-DL-1-(7-Methylindan-4-yloxy)-3-isopropylaminobutan-2-ol; (2R,3S)-3-(isopropylamino)-1-[(7-methyl-2,3-dihydro-1H-inden-4-yl)oxy]butan-2-ol; 2-Butanol, 1-((2,3-dihydro-7-methyl-1H-inden-4-yl)oxy)-3-((1-methylethyl)amino)-, (2R,3S)-rel-; 2-Butanol, 1-((2,3-dihydro-7-methyl-1H-inden-4-yl)oxy)-3-((1-methylethyl)amino)-, (R*,S*)-(+-)-; ICI-118,551; Ici 111,581; AC1NUNSO
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| Evorpacept | Phase 2/3 | [61] | ||
| Synonyms |
ALX148
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| BNT141 | Phase 2 | [62] | ||
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| Anti-LAG3 | Phase 2 | [52] | ||
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| GSK1292263 | Phase 2 | [63] | ||
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| MM-111 | Phase 2 | [64] | ||
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| Plevitrexed | Phase 2 | [65] | ||
| Synonyms |
ZD 9331; ZD9331; 153537-73-6; Plevitrexed [INN]; ZD-9331; NSC 696259; UNII-L9P2881C3H; CHEMBL126648; (2s)-2-[(2-fluoro-4-{[(4-hydroxy-2,7-dimethylquinazolin-6-yl)methyl](prop-2-yn-1-yl)amino}benzoyl)amino]-4-(2h-tetrazol-5-yl)butanoic acid; L9P2881C3H; Plevitrexed (INN); 172521-94-7; (2S)-2-[[4-[(2,7-dimethyl-4-oxo-1H-quinazolin-6-yl)methyl-prop-2-ynylamino]-2-fluorobenzoyl]amino]-4-(2H-tetrazol-5-yl)butanoic acid; 1H-Tetrazole-5-butanoic acid,
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| DS-8201 | Phase 1 | [52] | ||
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9-Aminofluorene; 9H-Fluoren-9-amine; 525-03-1; FLUOREN-9-AMINE; Fluoren-9-ylamine; UNII-4NHO2K4K5B; CCRIS 7000; BRN 2209545; 4NHO2K4K5B; OUGMRQJTULXVDC-UHFFFAOYSA-N; fluorene-9-ylamine; 9-Amino-fluoren; 9-amino-fluorene; 9H-9-fluorenamine; 9H-fluoren-9-yl-amine; AC1L1VP5; 4-12-00-03390 (Beilstein Handbook Reference); SCHEMBL353865; AC1Q53A2; AC1Q53A1; KS-00000JGC; CTK1H0380; DTXSID90200496; MolPort-001-794-448; HMS1780P20; 9H-fluoren-9-ylamine hydrochloride; ZINC1724407; ALBB-023296; CA-733; SBB005783; AKOS000264388; MCULE-8757055914; DS-
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| XL880 | Phase 2 | [66] | ||
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GSK 089; GSK 1363089; GSK1363089; XL 880; GSK1363089, GSK089, foretinib, EXEL-2880, XL880; 88Z; MET inhibitors
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| Matuzumab | Phase 2 | [67] | ||
| Synonyms |
EMD-62000; EMD-72000; Anti-EGF receptor humanized antibody (iv, cancer), Merck KGaA/ Takeda Pharmaceuticals; Anti-EGFR humanized mAb (iv, cancer), Merck KGaA/ Takeda Pharmaceuticals; Anti-epidermal growth factor receptor humanized antibody (iv, cancer), Merck KGaA/ Takeda Pharmaceuticals
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| BAY-57-9352 | Phase 2 | [22] | ||
| Synonyms |
Telatinib; Bay 57-9352
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| Bemarituzumab | Phase 2 | [68] | ||
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| PEGPH20 | Phase 2 | [12] | ||
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| Plevitrexed (R)-isomer | Phase 2 | [69] | ||
| Synonyms |
YW3548
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| APR-246 | Phase 2 | [70] | ||
| Synonyms |
Eprenetapopt
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| CRS-207 | Phase 2 | [59] | ||
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| Opdivo + Yervoy | Phase 3 | [12] | ||
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| CT-041 | Phase 1/2 | [71] | ||
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| BPX-601 | Phase 1/2 | [72] | ||
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| Anti-MUC1 CAR-T cells | Phase 1/2 | [73] | ||
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| Anti-Mesothelin CAR-T cells | Phase 1/2 | [74] | ||
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| Anti-HER2 CAR-T | Phase 1/2 | [75] | ||
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| CAR-T Cells targeting EpCAM | Phase 1/2 | [76] | ||
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| PAT-SC1 | Phase 1/2 | [77] | ||
| Synonyms |
SC-1; Adjuvant therapy (gastric cancer), University of Wurzburg; SC-1 (gastric cancer), CAT; SC-1 (gastric cancer), Debiopharm; SC-1 (gastric cancer), Patrys; SC-1 (stomach cancer), OncoMab
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| ASP2138 | Phase 1 | [78] | ||
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| SAR443216 | Phase 1 | [79] | ||
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| AMG 199 | Phase 1 | [80] | ||
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| AMG 910 | Phase 1 | [81] | ||
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| Alofanib | Phase 1 | [82] | ||
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1612888-66-0; 3-(N-(4-methyl-2-nitro-5-(pyridin-3-yl)phenyl)sulfamoyl)benzoic acid; RPT-835(alofanib); UNII-LQX7RFK8MZ; RPT-835; RPT835; LQX7RFK8MZ; ES000835; Alofanib [INN]; Alofanib(RPT835); Syn007154; CHEMBL4594436; SCHEMBL18660613; AMY16650; BCP31905; EX-A2731; MFCD30533418; NSC790182; s8754; Benzoic acid, 3-(((4-methyl-2-nitro-5-(3-pyridinyl)phenyl)amino)sulfonyl)-; NSC-790182; SB19665; AC-31695; AK668992; AS-56846; HY-17601; CS-0014684; RPT 835; Q27283135; 3-{[4-methyl-2-nitro-5-(pyridin-3-yl)phenyl]sulfamoyl}benzoic acid
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| HER2-specific CAR T cell | Phase 1 | [83] | ||
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| Anti-CEA-CAR T | Phase 1 | [84] | ||
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| XR-5944 | Phase 1 | [85] | ||
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MLN-944; XR-11576 analogs; XR-5000 analogs; XR-5942
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| A168 | Phase 1 | [86] | ||
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| EGFR806-specific CAR T cell | Phase 1 | [87] | ||
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| AbGn-107 | Phase 1 | [12] | ||
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| FPA144 | Phase 1 | [52] | ||
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| Minnelide 001 | Phase 1 | [22] | ||
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| CAR-T cells targeting EpCAM | Phase 1 | [88] | ||
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| Anti-CEA CAR-T cells | Phase 1 | [89] | ||
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| EPCAM-targeted CAR-T cells | Clinical trial | [90] | ||
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| PMID28460551-Compound-1 | Patented | [91] | ||
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| Conjugated 3-(indolyl)-and 3-(azaindolyl)-4-arylmaleimide compound 1 | Patented | [92] | ||
| Synonyms |
PMID28621580-Compound-WO2012084683c62
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| TOPIXANTRONE HYDROCHLORIDE | Discontinued in Phase 2 | [93] | ||
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SCHEMBL1418986; Topixantrone hydrochloride < Prop INNM; BBR-3409 (dimaleate); 5-[2-(Dimethylamino)ethylamino]-2-[2-(2-hydroxyethylamino)ethyl]indazolo[4,3-gh]isoquinolin-6(2H)-one dihydrochloride
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| MDL 101,731 | Discontinued in Phase 2 | [94] | ||
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Tezacitabine; Fmdc cpd; 130306-02-4; UNII-7607Y95N9S; Mdl 101731; (E)-2'-Deoxy-2'-(fluoromethylene) cytidine; MDL-101731; 2'-Deoxy-2'-(fluoromethylene)cytidine; 7607Y95N9S; Cytidine, 2'-deoxy-2'-(fluoromethylene)-, (2E)-; (E)-2'-Deoxy-2'-(fluoromethylene)cytidine; Tezacitabine [INN]; tezaciabine; Tezacitabine, anhydrous; AC1O5KIG; SCHEMBL18724; SCHEMBL18725; Tezacitabine, anhydrous [INN]; CHEMBL2105467; C10H12FN3O4; DTXSID10156446; GFFXZLZWLOBBLO-ASKVSEFXSA-N; ZINC3777826; KW-2331
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| BBR-3438 | Discontinued in Phase 2 | [95] | ||
| Synonyms |
Nortopixantrone; UNII-PH2639TAB4; PH2639TAB4; Nortopixantrone [INN:BAN]; AC1MI4ZO; CHEMBL150303; SCHEMBL7804438
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| IPI-493 | Discontinued in Phase 1 | [96] | ||
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[(3R,5R,6S,7R,8E,10R,11R,12Z,14E)-21-amino-6-hydroxy-5,11-dimethoxy-3,7,9,15-tetramethyl-16,20,22-trioxo-17-azabicyclo[16.3.1]docosa-1(21),8,12,14,18-pentaen-10-yl] carbamate; AC1NS08X; SCHEMBL16226496; SCHEMBL16225851
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| Kanjinti | Application submitted | [12] | ||
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| Anti-CD9 mab | Investigative | [97] | ||
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ALB-6; Anti-CD9 mAb (gastric cancer); Anti-CD9 mAb (gastric cancer), Osaka University
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References
: m6A sites