m6A-centered Crosstalk Information

Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
Crosstalk ID
M6ACROT03342
 [1], [2]
Histone modification H3K18la EP300 YTHDF2 Direct Enhancement m6A modification MTOR MTOR YTHDF2 : m6A sites
m6A Modification:
m6A Regulator YTH domain-containing family protein 2 (YTHDF2) READER
 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 Histone modification (HistMod)
Epigenetic Regulator Histone acetyltransferase p300 (P300) WRITER View Details
Regulated Target Histone H3 lysine 18 lactylation (H3K18la) View Details
Downstream Gene YTHDF2 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 lactylation activates the transcription of YTHDF2 through p300-mediated Histone H3 lysine 18 lactylation (H3K18la) modification. In colorectal cancer, Glutaminolysis inhibition upregulated ATF4 expression in an m6A-dependent manner to activate pro-survival autophagy through transcriptional activation of the mTOR inhibitor DDIT4. Determined the relationship between FTO alpha-ketoglutarate dependent dioxygenase (FTO), YTH N6-methyladenosine RNA binding protein 2 (YTHDF2), and ATF4. ATF4 transcriptionally upregulated DDIT4 to suppress Serine/threonine-protein kinase mTOR (MTOR), which induced pro-survival autophagy during glutaminolysis inhibition.
Responsed Disease Colorectal cancer ICD-11: 2B91
 Disease Info 
Responsed Drug CB-839
 Drug Info 
Pathway Response mTOR signaling pathway hsa04150
Cell Process RNA decay
Cell growth and death
Cell autophagy
In-vitro Model
 SW480 Colon adenocarcinoma Homo sapiens CVCL_0546
HCT 116 Colon carcinoma Homo sapiens CVCL_0291
Full List of Potential Compound(s) Related to This m6A-centered Crosstalk
Histone acetyltransferase p300 (P300) 2 Compound(s) Regulating the Target Click to Show/Hide the Full List
 Compound Name CCS1477 Phase 1/2 [3]
Synonyms
CCS-1477; CBP-IN-1; 2222941-37-7; (S)-1-(3,4-Difluorophenyl)-6-(5-(3,5-dimethylisoxazol-4-yl)-1-((1r,4S)-4-methoxycyclohexyl)-1H-benzo[d]imidazol-2-yl)piperidin-2-one; SCHEMBL20094038; SCHEMBL21515367; SCHEMBL22134021; EX-A3687; NSC818619; NSC-818619; HY-111784; CS-0091862; (S)-1-(3,4-Difluorophenyl)-6-(5-(3,5-dimethylisoxazol-4-yl)-1-(trans-4-methoxycyclohexyl)-1H-benzo[d]imidazol-2-yl)piperidin-2-one
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 134457551
TTD: DIY4C2
 Compound Name FT-7051 Phase 1 [4]
MOA Inhibitor
External Link
TTD: DT8IL6
Serine/threonine-protein kinase mTOR (MTOR) 72 Compound(s) Regulating the Target Click to Show/Hide the Full List
 Compound Name Novolimus Approved [5]
MOA Inhibitor
External Link
CID: 9854320
TTD: D03FCF
 Compound Name Temsirolimus Approved [6]
Synonyms
Torisel
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1760 nM
External Link
CID: 6918289
TTD: D0ES1Q
 Compound Name Everolimus Approved [7]
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
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 6442177
TTD: D0K3QS
DrugBank: DB01590
 Compound Name Zotarolimus Approved [8]
Synonyms
Abt-578; Zotarolimus (TN)
    Click to Show/Hide
MOA Modulator
Activity IC50 = 3.3 nM
External Link
CID: 9876378
TTD: D0V7WS
 Compound Name Sirolimus Approved [9]
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)
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 5284616
TTD: D03LJR
DrugBank: DB00877
 Compound Name PF-04449913 Approved [10]
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
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 25166913
TTD: D0S5LO
DrugBank: DB11978
 Compound Name Ridaforolimus Phase 3 [11]
Synonyms
Deforolimus; AP 23573; MK 8669; AP-23573; MK-8669; AP23573, MK-8669, Ridaforolimus, Deforolimus
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 11520894
TTD: D0O3CV
DrugBank: DB06233
 Compound Name INK128 Phase 2 [12]
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)
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 1 nM
External Link
CID: 45375953
TTD: D03DPZ
DrugBank: DB11836
 Compound Name OSI-027 Phase 2 [13]
MOA Inhibitor
External Link
CID: 135398516
TTD: D0H7XL
DrugBank: DB12387
 Compound Name ABI-009 Phase 2 [14]
MOA Inhibitor
External Link
TTD: D0W3UV
 Compound Name Salirasib Discontinued in Phase 1/2 [5]
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
    Click to Show/Hide
MOA Modulator
External Link
CID: 5469318
TTD: D00KTV
DrugBank: DB12681
 Compound Name SAR245409 Phase 2 [5]
MOA Inhibitor
Activity IC50 = 157 nM
External Link
CID: 16123056
TTD: D01PGR
DrugBank: DB12400
 Compound Name SF1126 Phase 2 [14]
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
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 66577114
TTD: D03NJY
 Compound Name PF-05212384 Phase 2 [15]
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)-
    Click to Show/Hide
MOA Modulator
Activity IC50 = 0.4 nM
External Link
CID: 44516953
TTD: D0D8JB
DrugBank: DB11896
 Compound Name LY3023414 Phase 2 [16]
MOA Modulator
External Link
CID: 57519748
TTD: D0H1WC
DrugBank: DB12167
 Compound Name PF-04691502 Phase 2 [17]
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
    Click to Show/Hide
MOA Modulator
Activity IC50 = 7.9 nM
External Link
CID: 25033539
TTD: D0N5JZ
DrugBank: DB11974
 Compound Name GDC-0980/RG7422 Phase 2 [5]
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
    Click to Show/Hide
MOA Modulator
Activity Ki = 17 nM
External Link
CID: 25254071
TTD: D0O6VZ
DrugBank: DB12180
 Compound Name BEZ235 Phase 2 [18]
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
    Click to Show/Hide
MOA Modulator
Activity IC50 = 5 nM
External Link
CID: 11977753
TTD: D0VG0D
DrugBank: DB11651
 Compound Name MM-141 Phase 2 [14]
MOA Inhibitor
External Link
TTD: D00BUO
 Compound Name PQR309 Phase 2 [5]
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)
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 62 nM
External Link
CID: 58507717
TTD: D0TU7B
DrugBank: DB14846
 Compound Name AZD2014 Phase 2 [19]
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)
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 2.8 nM
External Link
CID: 25262792
TTD: D0Z2UQ
DrugBank: DB11925
 Compound Name CC-223 Phase 1/2 [20]
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
    Click to Show/Hide
MOA Modulator
Activity IC50 = 10 nM
External Link
CID: 58298316
TTD: D05EXN
DrugBank: DB12570
 Compound Name BGT226 Phase 1/2 [21]
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
    Click to Show/Hide
MOA Modulator
External Link
CID: 11978790
TTD: D0X7IN
 Compound Name ME-344 Phase 1/2 [22]
Synonyms
NV-128; NV-344; MTOR inhibitor (cancer), Novogen; MTOR inhibitors (cancer), Marshall Edwards
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 68026984
TTD: D03IXK
DrugBank: DB13062
 Compound Name BI 860585 Phase 1 [23]
MOA Inhibitor
External Link
TTD: D08PSC
 Compound Name LAM-001 Phase 1 [24]
MOA Inhibitor
External Link
TTD: D0QN5M
 Compound Name DS-3078 Phase 1 [25]
MOA Modulator
External Link
TTD: D0R9VX
 Compound Name GDC-0349 Phase 1 [26]
Synonyms
MTORC1/2 inhibitors
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 3.8 nM
External Link
CID: 59239165
TTD: D0U8QH
DrugBank: DB13072
 Compound Name CERC 006 Phase 1 [27]
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
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 135398516
TTD: D1RLY2
DrugBank: DB12387
 Compound Name DS-7423 Phase 1 [28]
MOA Modulator
External Link
TTD: D0X4RT
 Compound Name PWT-33597 Phase 1 [29]
Synonyms
PI3 kinase alpha/mTOR dual inhibitor (cancer), Pathway Therapeutics
    Click to Show/Hide
MOA Modulator
External Link
CID: 46917355
TTD: D0Y0FE
 Compound Name VS-5584 Phase 1 [5]
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
    Click to Show/Hide
MOA Modulator
External Link
CID: 46912230
TTD: D0U3DP
DrugBank: DB12986
 Compound Name PMID25726713-Compound-49 Patented [30]
MOA Inhibitor
Activity IC50 < 1 nM
External Link
TTD: D07TVO
 Compound Name PMID25726713-Compound-51 Patented [30]
MOA Inhibitor
Activity IC50 < 1 nM
External Link
TTD: D0KH7Q
 Compound Name PMID25726713-Compound-48 Patented [30]
MOA Inhibitor
Activity IC50 < 1 nM
External Link
TTD: D0WJ3W
 Compound Name PMID25726713-Compound-47 Patented [30]
MOA Inhibitor
Activity IC50 < 1 nM
External Link
TTD: D0X5VI
 Compound Name PMID25726713-Compound-50 Patented [30]
MOA Inhibitor
Activity IC50 < 1 nM
External Link
TTD: D0Y8JF
 Compound Name AZD8055 Discontinued in Phase 1/2 [31]
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 [32]
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 [33]
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 [34]
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 [35]
MOA Inhibitor
External Link
TTD: D01AQN
 Compound Name C-16-(S)-3-methylindolerapamycin Investigative [36]
Synonyms
CHEMBL503885
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 5 nM
External Link
CID: 44576240
TTD: D02TCF
 Compound Name PF-05094037 Investigative [5]
Synonyms
PF-05171310; PF-05181059; MTOR inhibitors (cancer), Pfizer
    Click to Show/Hide
MOA Inhibitor
External Link
TTD: D03XRZ
 Compound Name SX-MTR1 Investigative [5]
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 [34]
MOA Inhibitor
Activity IC50 = 2500 nM
External Link
CID: 135955185
TTD: D07JKB
 Compound Name P-2281 Investigative [5]
Synonyms
MTOR inhibitor (ulcerative colitis), Piramal
    Click to Show/Hide
MOA Inhibitor
External Link
TTD: D07NFT
 Compound Name X-387 Investigative [5]
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 [34]
MOA Inhibitor
Activity IC50 = 450 nM
External Link
CID: 135955186
TTD: D09FBN
 Compound Name EM-101 Investigative [5]
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 [5]
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 [34]
Synonyms
CHEMBL604876; SCHEMBL4439490
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 2800 nM
External Link
CID: 25074311
TTD: D0AH8Q
 Compound Name SB-2280 Investigative [5]
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 [34]
Synonyms
CHEMBL608095; SCHEMBL4438208
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 3900 nM
External Link
CID: 25074312
TTD: D0F1SI
 Compound Name torin 1 Investigative [37]
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 [5]
Synonyms
Folate-everolimus conjugate (inflammation), Endocyte
    Click to Show/Hide
MOA Inhibitor
External Link
TTD: D0H4KF
 Compound Name OXA-01 Investigative [5]
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 [5]
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 [38]
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 [34]
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 [36]
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 [34]
Synonyms
CHEMBL611630
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 150 nM
External Link
CID: 46225260
TTD: D0Y1DR
 Compound Name Torin2 Investigative [39]
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 [5]
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 [40]
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 [41]
Synonyms
PP242; TORKinib
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 8 nM
External Link
CID: 135565635
TTD: D0H2CM
 Compound Name CU-906 Investigative [5]
MOA Inhibitor
External Link
TTD: D0JD4S
 Compound Name P-6915 Investigative [5]
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 [42]
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 [42]
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 [42]
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 [41]
Synonyms
PP-121; PP 121
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 10 nM
External Link
CID: 24905142
TTD: D03EHM
DrugBank: DB08052
2B91: Colorectal cancer 25 Compound(s) Regulating the Disease Click to Show/Hide the Full List
 Compound Name Retifanlimab Approved [43]
Synonyms
INCMGA0012; Retifanlimab
    Click to Show/Hide
External Link
TTD: D0PG5O
 Compound Name Aflibercept Approved [44]
Synonyms
Ziv-Aflibercept; Zaltrap (TN); VEGF Trap; VEGF Trap-Eye
    Click to Show/Hide
External Link
TTD: D0C9ET
 Compound Name Regorafenib Approved [45]
Synonyms
755037-03-7; BAY 73-4506; Regorafenibum; Stivarga; 4-(4-(3-(4-Chloro-3-(trifluoromethyl)phenyl)ureido)-3-fluorophenoxy)-N-methylpicolinamide; BAY73-4506; Regorafenib (BAY 73-4506); UNII-24T2A1DOYB; 4-[4-({[4-Chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide; BAY-73-4506; 24T2A1DOYB; CHEMBL1946170; CHEBI:68647; Stivarga (TN); BAY73-4506 hydrochloride; Regorafenib [USAN:INN]
    Click to Show/Hide
External Link
CID: 11167602
TTD: D09GDD
DrugBank: DB08896
 Compound Name Bevacizumab Approved [14]
Synonyms
Bevacizumab (ophthalmic slow-release tissue tablet)
    Click to Show/Hide
External Link
TTD: D04KBL
 Compound Name SYM-004 Phase 3 [14]
Synonyms
Chimeric IgG1 antibody 1024 (cancer), Symphogen; Chimeric IgG1 antibody 992 (cancer), Symphogen; Chimeric IgG1 antibodies992 + 1024 (cancer), Symphogen
    Click to Show/Hide
External Link
TTD: D0CR8H
 Compound Name Bevacizumab + Erlotinib Phase 3 [46]
External Link
TTD: D09BKY
 Compound Name CPI-613 Phase 3 [14]
Synonyms
95809-78-2; 6,8-bis(benzylthio)octanoic acid; CPI 613; MLS006010202; SCHEMBL1062218; 6,8-Bis(benzylsulfanyl)octanoic acid; Octanoic acid, 6,8-bis((phenylmethyl)thio)-; Octanoic acid, 6,8-bis[(phenylMethyl)thio]-; 6,8-Bis[(phenylmethyl)thio]octanoic acid; CPI613; CHEMBL3186849; QCR-193; AOB1058; MolPort-023-219-128; HMS3656L06; C22H28O2S2; BCP04663; EX-A2043; s2776; AKOS025142095; BCP9000552; DB12109; RL06062; CS-0961; NCGC00344764-01; SMR004701300; AS-16613; BC261916; AK174899; HY-15453; BCP0726000030; KB-293127; AB0035874
    Click to Show/Hide
External Link
CID: 24770514
TTD: D07NVI
DrugBank: DB12109
 Compound Name Bevacizumab Approved [44]
External Link
TTD: D0FX3U
 Compound Name AlloStim Phase 2/3 [47]
Synonyms
AlloStim (TN)
    Click to Show/Hide
External Link
TTD: D0B3CC
 Compound Name Sibrotuzumab Phase 2 [48]
External Link
TTD: DVX3H0
 Compound Name CV301 Phase 2 [49]
External Link
TTD: D9LT5G
 Compound Name Efatutazone Phase 2 [50]
Synonyms
Inolitazone; 223132-37-4; 5-[[4-[[6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1H-benzimidazol-2-yl]methoxy]phenyl]methyl]-2,4-Thiazolidinedione; Efatutazone [INN]; RS5444; CS-7017; SCHEMBL3246054; CHEMBL3545280; JCYNMRJCUYVDBC-UHFFFAOYSA-N; Efatutazone;CS-7017;RS5444; BCP07478; AKOS030526729; DB11894; CS-0778; KB-77905; DA-07988; HY-14792; QC-10456; 4CA-1384; FT-0737589; 5-[4-[6-(4-amino-3 ,5-dimethylphenoxy)-1-methyl-1H-benzimidazol-2-ylmethoxy]benzyl]thiazolidine-2,4-dione
    Click to Show/Hide
External Link
CID: 9832447
TTD: D0Y8NZ
DrugBank: DB11894
 Compound Name LOR-2040 Phase 2 [51]
External Link
TTD: D0I7NG
 Compound Name RG7221 Phase 2 [52]
External Link
TTD: D06FTM
 Compound Name PEG-SN38 Phase 2 [53]
Synonyms
EZN-2208
    Click to Show/Hide
External Link
CID: 59443782
TTD: D05UFP
 Compound Name MEGF0444A Phase 2 [54]
External Link
TTD: D01LES
 Compound Name Encapsulated cell therapy Phase 1/2 [55]
External Link
TTD: D0XY8C
 Compound Name AB928 Phase 1/2 [56]
External Link
CID: 135242184
TTD: D04UBI
 Compound Name MGD007 Phase 1 [52]
External Link
TTD: D00PEN
 Compound Name BNC-101 Phase 1 [57]
External Link
TTD: DD6AZ5
 Compound Name Navicixizumab Phase 1 [14]
External Link
TTD: D00IVN
 Compound Name RG7160 Discontinued in Phase 2 [58]
External Link
TTD: D0E2CQ
 Compound Name Nimesulide Terminated [59]
Synonyms
51803-78-2; N-(4-Nitro-2-phenoxyphenyl)methanesulfonamide; Mesulid; Flogovital; Sulidene; Nimed; R-805; 4-NITRO-2-PHENOXYMETHANESULFONANILIDE; Nisulid; Nimesulidum [INN-Latin]; Nimesulida [INN-Spanish]; R 805; UNII-V4TKW1454M; 4-Nitro-2-phenoxy-methanesulfonanilide; 4'-Nitro-2'-phenoxymethanesulfonanilide; Methanesulfonamide, N-(4-nitro-2-phenoxyphenyl)-; EINECS 257-431-4; 4'-Nitro-2'-phenoxymethansulfonanilid; BRN 2421175; CHEMBL56367; MLS000069680; V4TKW1454M; Methanesulfonanilide, 4'-nitro-2'-phenoxy-; CHEBI:44445; Dulanermin
    Click to Show/Hide
External Link
CID: 4495
TTD: D0C0JT
DrugBank: DB04743
 Compound Name Saracatinib Phase 2 [60]
External Link
CID: 10302451
TTD: D05YTN
DrugBank: DB11805
 Compound Name G3139 + Irinotecan Investigative [61]
External Link
CID: 91865905
TTD: D05IAN
References
Ref 1 The m6A methyltransferase METTL3 modifies Kcnk6 promoting on inflammation associated carcinogenesis is essential for colon homeostasis and defense system through histone lactylation dependent YTHDF2 binding. Int Rev Immunol. 2025;44(1):1-16. doi: 10.1080/08830185.2024.2401358. Epub 2024 Sep 13.
Ref 2 Targeting ATF4-dependent pro-survival autophagy to synergize glutaminolysis inhibition. Theranostics. 2021 Jul 25;11(17):8464-8479. doi: 10.7150/thno.60028. eCollection 2021.
Ref 3 Targeting the p300/CBP Axis in Lethal Prostate Cancer. Cancer Discov. 2021 May;11(5):1118-1137. doi: 10.1158/2159-8290.CD-20-0751. Epub 2021 Jan 11.
Ref 4 Clinical pipeline report, company report or official report of FORMA Therapeutics.
Ref 5 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: 2109).
Ref 6 Advances in kinase targeting: current clinical use and clinical trials. Trends Pharmacol Sci. 2014 Nov;35(11):604-20. doi: 10.1016/j.tips.2014.09.007. Epub 2014 Oct 10.
Ref 7 [Mammalian target of rapamycin, its mode of action and clinical response in metastatic clear cell carcinoma]. Gan To Kagaku Ryoho. 2009 Jul;36(7):1076-9.
Ref 8 Natural products to drugs: natural product-derived compounds in clinical trials. Nat Prod Rep. 2008 Jun;25(3):475-516.
Ref 9 Knockouts model the 100 best-selling drugs--will they model the next 100 Nat Rev Drug Discov. 2003 Jan;2(1):38-51.
Ref 10 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 11 A novel c-Met inhibitor, MK8033, synergizes with carboplatin plus paclitaxel to inhibit ovarian cancer cell growth. Oncol Rep. 2013 May;29(5):2011-8. doi: 10.3892/or.2013.2329. Epub 2013 Mar 5.
Ref 12 2011 Pipeline of Intellikine.
Ref 13 Targeting the phosphoinositide 3-kinase pathway in cancer. Nat Rev Drug Discov. 2009 Aug;8(8):627-44. doi: 10.1038/nrd2926.
Ref 14 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 15 First-in-Human Study of PF-05212384 (PKI-587), a Small-Molecule, Intravenous, Dual Inhibitor of PI3K and mTOR in Patients with Advanced Cancer. Clin Cancer Res. 2015 Apr 15;21(8):1888-95. doi: 10.1158/1078-0432.CCR-14-1306. Epub 2015 Feb 4.
Ref 16 Company report (Lilly)
Ref 17 PF-04691502, a potent and selective oral inhibitor of PI3K and mTOR kinases with antitumor activity. Mol Cancer Ther. 2011 Nov;10(11):2189-99. doi: 10.1158/1535-7163.MCT-11-0185. Epub 2011 Jul 12.
Ref 18 The dual PI3K/mTOR inhibitor NVP-BEZ235 is a potent inhibitor of ATM- and DNA-PKCs-mediated DNA damage responses. Neoplasia. 2012 Jan;14(1):34-43.
Ref 19 Dramatic suppression of colorectal cancer cell growth by the dual mTORC1 and mTORC2 inhibitor AZD-2014. Biochem Biophys Res Commun. 2014 Jan 10;443(2):406-12. doi: 10.1016/j.bbrc.2013.11.099. Epub 2013 Dec 2.
Ref 20 CC-223, a Potent and Selective Inhibitor of mTOR Kinase: In Vitro and In Vivo Characterization. Mol Cancer Ther. 2015 Jun;14(6):1295-305. doi: 10.1158/1535-7163.MCT-14-1052. Epub 2015 Apr 8.
Ref 21 Simultaneous targeting of PI3K and mTOR with NVP-BGT226 is highly effective in multiple myeloma. Anticancer Drugs. 2012 Jan;23(1):131-8. doi: 10.1097/CAD.0b013e32834c8683.
Ref 22 National Cancer Institute Drug Dictionary (drug id 728650).
Ref 23 Clinical pipeline report, company report or official report of tatcongress.
Ref 24 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 25 A first-in-human Phase I study of DS-3078a, an oral TORC1/2 inhibitor, in patients with advanced solid tumors: Preliminary results, Mol Cancer Ther November,2013, 12, C173.
Ref 26 Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349. ACS Med Chem Lett. 2012 Nov 29;4(1):103-7. doi: 10.1021/ml3003132. eCollection 2013 Jan 10.
Ref 27 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2023. Adis Insight
Ref 28 Antitumor activity and induction of TP53-dependent apoptosis toward ovarian clear cell adenocarcinoma by the dual PI3K/mTOR inhibitor DS-7423. PLoS One. 2014 Feb 4;9(2):e87220. doi: 10.1371/journal.pone.0087220. eCollection 2014.
Ref 29 PIK3CA mutation H1047R is associated with response to PI3K/AKT/mTOR signaling pathway inhibitors in early phase clinical trials
Ref 30 Hedgehog inhibitors: a patent review (2013 - present). Expert Opin Ther Pat. 2015 May;25(5):549-65. doi: 10.1517/13543776.2015.1019864. Epub 2015 Mar 1.
Ref 31 Clinical pipeline report, company report or official report of AstraZeneca (2009).
Ref 32 EP patent application no. 2275103, Mtor inhibitors in the treatment of endocrine tumors.
Ref 33 Early detection of response to experimental chemotherapeutic Top216 with [18F]FLT and [18F]FDG PET in human ovary cancer xenografts in mice. PLoS One. 2010 Sep 24;5(9):e12965. doi: 10.1371/journal.pone.0012965.
Ref 34 Novel purine and pyrazolo[3,4-d]pyrimidine inhibitors of PI3 kinase-alpha: Hit to lead studies. Bioorg Med Chem Lett. 2010 Jan 15;20(2):636-9. doi: 10.1016/j.bmcl.2009.11.051. Epub 2009 Dec 5.
Ref 35 Selected novel anticancer treatments targeting cell signaling proteins. Oncologist. 2001;6(6):517-37. doi: 10.1634/theoncologist.6-6-517.
Ref 36 The rapamycin-binding domain of the protein kinase mammalian target of rapamycin is a destabilizing domain. J Biol Chem. 2007 May 4;282(18):13395-401. doi: 10.1074/jbc.M700498200. Epub 2007 Mar 9.
Ref 37 Discovery of 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a highly potent, selective mammalian target of rapamycin (mTOR) inhibitor for the treatment of cancer. J Med Chem. 2010 Oct 14;53(19):7146-55. doi: 10.1021/jm101144f.
Ref 38 Synthesis and therapeutic evaluation of pyridyl based novel mTOR inhibitors. Bioorg Med Chem Lett. 2009 Jun 1;19(11):2949-52. doi: 10.1016/j.bmcl.2009.04.055. Epub 2009 Apr 18.
Ref 39 Torin2 Potentiates Anticancer Effects on Adult T-Cell Leukemia/Lymphoma by Inhibiting Mammalian Target of Rapamycin. Anticancer Res. 2016 Jan;36(1):95-102.
Ref 40 Discovery of the Highly Potent PI3K/mTOR Dual Inhibitor PF-04979064 through Structure-Based Drug Design. ACS Med Chem Lett. 2012 Nov 7;4(1):91-7. doi: 10.1021/ml300309h. eCollection 2013 Jan 10.
Ref 41 Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol. 2008 Nov;4(11):691-9. doi: 10.1038/nchembio.117. Epub 2008 Oct 12.
Ref 42 Selective benzopyranone and pyrimido[2,1-a]isoquinolin-4-one inhibitors of DNA-dependent protein kinase: synthesis, structure-activity studies, and radiosensitization of a human tumor cell line in vitro. J Med Chem. 2005 Jan 27;48(2):569-85. doi: 10.1021/jm049526a.
Ref 43 Development of Inhibitors of the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Signaling Pathway.J Med Chem. 2019 Feb 28;62(4):1715-1730.
Ref 44 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 45 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5891).
Ref 46 ClinicalTrials.gov (NCT00130728) A Study to Evaluate the Efficacy of Bevacizumab in Combination With Tarceva for Advanced Non-Small Cell Lung Cancer
Ref 47 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 48 ClinicalTrials.gov (NCT02198274) Intravenous BIBH 1 in Patients With Metastatic Colorectal Cancer. U.S. National Institutes of Health.
Ref 49 ClinicalTrials.gov (NCT03547999) A Trial of Perioperative CV301 Vaccination in Combination With Nivolumab and Systemic Chemotherapy for Metastatic CRC. U.S. National Institutes of Health.
Ref 50 ClinicalTrials.gov (NCT02152137) Efatutazone With Paclitaxel Versus Paclitaxel Alone in Treating Patients With Advanced Anaplastic Thyroid Cancer. U.S. National Institutes of Health.
Ref 51 ClinicalTrials.gov (NCT00087165) GTI-2040, Docetaxel, and Prednisone in Treating Patients With Prostate Cancer. U.S. National Institutes of Health.
Ref 52 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 53 ClinicalTrials.gov (NCT01036113) A Phase 2 Study of EZN-2208 in Patients With Metastatic Breast Cancer. U.S. National Institutes of Health.
Ref 54 ClinicalTrials.gov (NCT00909740) A Study of the Safety and Pharmacokinetics of MEGF0444A Administered to Patients With Advanced Solid Tumors. U.S. National Institutes of Health.
Ref 55 VC-01's Path to the Clinic. Viacyte. 2015.
Ref 56 ClinicalTrials.gov (NCT04660812) An Open Label Study Evaluating the Efficacy and Safety of AB928 Based Treatment Combinations in Patients With Metastatic Colorectal Cancer.. U.S. National Institutes of Health.
Ref 57 ClinicalTrials.gov (NCT02726334) A Phase I, Dose Escalation Study of BNC101 in Patients With Metastatic Colorectal Cancer.. U.S. National Institutes of Health.
Ref 58 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029052)
Ref 59 Clinical pipeline report, company report or official report of Genentech (2011).
Ref 60 Phase II Study of Saracatinib (AZD0530) in Patients With Previously Treated Metastatic Colorectal Cancer. Invest New Drugs. 2015 Aug;33(4):977-84.
Ref 61 Design and development of antisense drugs. Expert Opin. Drug Discov. 2008 3(10):1189-1207.