Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
Crosstalk ID
M6ACROT03395
[1], [2]
Histone modification H3K4me1 Epigenetic Regulator MIR570HG Indirect Inhibition m6A modification MET MET METTL3 Methylation : m6A sites
m6A Modification:
m6A Regulator Methyltransferase-like 3 (METTL3) WRITER
m6A Target Hepatocyte growth factor receptor (c-Met/MET)
Epigenetic Regulation that have Cross-talk with This m6A Modification:
Epigenetic Regulation Type Histone modification (HistMod)
Regulated Target Histone H3 lysine 4 monomethylation (H3K4me1) View Details
Downstream Gene MIR570HG View Details
Crosstalk Relationship Histone modification  →  m6A Inhibition
Crosstalk Mechanism Histone modification indirectly regulates m6A modification through downstream signaling pathways
Crosstalk Summary Gain of Histone H3 lysine 4 monomethylation (H3K4me1) and H3K27ac led to the activation of MIR570HG expression. LINC00969 interacts with EZH2 and METTL3, transcriptionally regulates the level of H3K27me3 in the NLRP3 promoter region, and posttranscriptionally modifies the m6A level of NLRP3 in an m6A-YTHDF2-dependent manner METTL3 combines with Hepatocyte growth factor receptor (c-Met/MET) and causes the PI3K/AKT signalling pathway to be manipulated, which affects the sensitivity of lung cancer cells to gefitinib. METTL3 knockdown promotes apoptosis and inhibits proliferation of lung cancer cells.
Responsed Disease Lung cancer ICD-11: 2C25
Responsed Drug Gefitinib
Cell Process Pyroptosis
In-vitro Model
PC-9 Lung adenocarcinoma Homo sapiens CVCL_B260
NCI-H3255 Lung adenocarcinoma Homo sapiens CVCL_6831
Full List of Potential Compound(s) Related to This m6A-centered Crosstalk
Hepatocyte growth factor receptor (c-Met/MET) 76 Compound(s) Regulating the Target Click to Show/Hide the Full List
 Compound Name Capmatinib Approved [3]
Synonyms
1029712-80-8; INCB28060; INC-280; INC280; UNII-TY34L4F9OZ; 2-fluoro-N-methyl-4-(7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl)benzamide; INC28060; INCB-28060; INCB28060(Capmatinib); NVP-INC280; TY34L4F9OZ; Capmatinib (INCB28060); INCB 28060; 2-Fluoro-N-methyl-4-[7-[(quinolin-6-yl)methyl]imidazo[1,2-b]-[1,2,4]triazin-2-yl]benzamide; BenzaMide, 2-fluoro-N-Methyl-4-[7-(6-quinolinylMethyl)iMidazo[1,2-b][1,2,4]triazin-2-yl]-; C23H17FN6O
    Click to Show/Hide
MOA Modulator
Activity IC50 = 0.13 nM
External Link
 Compound Name Tepotinib Approved [4]
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
MOA Modulator
Activity IC50 < 1 nM
External Link
 Compound Name Cabozantinib Approved [5]
Synonyms
Cabometyx; Cometriq
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1.3 nM
External Link
 Compound Name Amivantamab Approved [6]
MOA Inhibitor
External Link
 Compound Name Crizotinib Approved [7]
Synonyms
Xalkori (TN); novel ALK inhibitors
    Click to Show/Hide
MOA Modulator
Activity IC50 = 0.51 nM
External Link
 Compound Name RG3638 Phase 3 [8]
Synonyms
Onartuzumab
    Click to Show/Hide
MOA Modulator
External Link
 Compound Name Savolitinib Phase 3 [9]
Synonyms
1313725-88-0; AZD-6094; AZD6094; UNII-2A2DA6857R; CHEMBL3334567; 2A2DA6857R; Savolitinib [INN]; Volitinib(Savolitinib); Savolitinib [USAN:INN]; GTPL9918; SCHEMBL12489208; EX-A845; BDBM50023342; ZINC149738712; AKOS030526403; DB12048; compound 28 [PMID: 25148209]; HY-15959; AS-35250; 1H-1,2,3-Triazolo(4,5-b)pyrazine, 1-((1S)-1-imidazo(1,2-a)pyridin-6-ylethyl)-6-(1-methyl-1H-pyrazol-4-yl)-; KB-333895; FT-0700162; J-690125; 4-{1-[(1S)-1-{imidazo[1,2-a]pyri
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1.995 nM
External Link
 Compound Name Beperminogene perplasmid Phase 3 [10]
MOA Modulator
External Link
 Compound Name Tivantinib Phase 3 [11]
Synonyms
905854-02-6; ARQ-197; ARQ197; ARQ 197; Tivantinib (ARQ 197); (3R,4R)-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione; UNII-PJ4H73IL17; PJ4H73IL17; 1000873-98-2; (3R,4R)-3-(5,6-Dihydro-4H-pyrrolo(3,2,1-ij)quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione; Tivantinib [USAN:INN]; 1228508-24-4; ARQ 197, Tivantinib; Tivantinib (ARQ-197); ARQ 197 (Tivantinib); cc-86; SCHEMBL44944; Tivantinib (JAN/USAN/INN); GTPL7948; CHEMBL2103882; CHEBI:91398; QCR-102
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 355 nM
External Link
 Compound Name MGCD516 Phase 2/3 [8]
Synonyms
Sitravatinib
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name LY-2875358 Phase 2 [12]
Synonyms
C-Met mAb (cancer), Eli Lilly; Anti-c-Met antibody (cancer), Lilly
    Click to Show/Hide
External Link
 Compound Name SAR-125844 Phase 2 [13]
Synonyms
Met inhibitor (iv, cancer), sanofi-aventis
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 4 nM
External Link
 Compound Name Emibetuzumab Phase 2 [14]
MOA Inhibitor
External Link
 Compound Name AMG 337 Phase 2 [15]
MOA Modulator
Activity IC50 = 1 nM
External Link
 Compound Name AMG 208 Phase 2 [16]
Synonyms
AMG-208; 1002304-34-8; AMG208; UNII-Y2SR66P7VM; 7-methoxy-4-((6-phenyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methoxy)quinoline; Y2SR66P7VM; CHEBI:90626; 7-methoxy-4-[(6-phenyl[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methoxy]quinoline; 7-Methoxy-4-[(6-phenyl-1,2,4-triazolo[4,3-b]pyridazin-3-yl)methoxy]quinoline; C22H17N5O2; 7-methoxy-4-[(6-phenyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methoxy]quinoline; 7-methoxy-4-({6-phenyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl}methoxy)quinoline; Triazolopyridazine, 4; 3cd8
    Click to Show/Hide
MOA Modulator
Activity IC50 = 9 nM
External Link
 Compound Name HM-5016504 Phase 2 [8]
Synonyms
C-Met inhibitor (cancer), Hutchison
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Telisotuzumab vedotin Phase 2 [17]
Synonyms
ABBV-399
    Click to Show/Hide
External Link
 Compound Name APL-101 Phase 2 [18]
Synonyms
Bozitinib; PLB-1001; 1440964-89-5; Vebreltinib; Vebreltinib [USAN]; UNII-2WZP8A9VFN; 2WZP8A9VFN; Bozitinib (PLB-1001); SCHEMBL15594471; BDBM107096; CBI-3103; s6762; WHO 11677; HY-125017; CS-0088607; US9695175, 44; 1,2,4-Triazolo(4,3-b)pyridazine, 6-(1-cyclopropyl-1H-pyrazol-4-yl)-3-(difluoro(6- fluoro-2-methyl-2H-indazol-5-yl)methyl)-; 6-(1-Cyclopropyl-1H-pyrazol-4-yl)-3-(difluoro(6-fluoro-2-methyl-2H-indazol-5- yl)methyl)-1,2,4-triazolo(4,3-b)pyridazine
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name CMX-2043 Phase 2 [19]
MOA Modulator
External Link
 Compound Name LY2801653 Phase 2 [20]
Synonyms
Merestinib; 1206799-15-6; LY-2801653; UNII-5OGS5K699E; N-(3-fluoro-4-((1-methyl-6-(1H-pyrazol-4-yl)-1H-indazol-5-yl)oxy)phenyl)-1-(4-fluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridine-3-carboxamide; 5OGS5K699E; N-(3-Fluoro-4-{[1-Methyl-6-(1h-Pyrazol-4-Yl)-1h-Indazol-5-Yl]oxy}phenyl)-1-(4-Fluorophenyl)-6-Methyl-2-Oxo-1,2-Dihydropyridine-3-Carboxamide; C30H22F2N6O3; Merestinib [USAN]; SCHEMBL679002; LY2801653 (Merestinib); GTPL9841; CHEMBL3545307; QCR-139; DTXSID20659635; SYN1222; QHADVLVFMKEIIP-UHFFFAOYSA-N
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MOA Modulator
Activity IC50 = 4.7 nM
External Link
 Compound Name XL880 Phase 2 [21]
Synonyms
GSK 089; GSK 1363089; GSK1363089; XL 880; GSK1363089, GSK089, foretinib, EXEL-2880, XL880; 88Z; MET inhibitors
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MOA Modulator
Activity IC50 = 0.4 nM
External Link
 Compound Name ChronSeal Phase 1/2 [22]
Synonyms
Antibiotic-free recombinant HGF, Linkoping; Recombinant HGF, Kringle/ChronTech; Recombinant HGF, Kringle/Tripep
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Anti-C-met CAR-T cells Phase 1/2 [23]
MOA CAR-T-Cell-Therapy
External Link
 Compound Name BMS-777607 Phase 1/2 [24]
Synonyms
1025720-94-8; BMS 777607; 1196681-44-3; BMS777607; ASLAN-002; UNII-A3MMS6HDO1; N-(4-(2-Amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide; A3MMS6HDO1; N-[4-[(2-Amino-3-chloropyridin-4-yl)oxy]-3-fluorophenyl]-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide; N-(4-((2-amino-3-chloropyridin-4-yl)oxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide
    Click to Show/Hide
MOA Inhibitor
Activity IC50 < 2.512 nM
External Link
 Compound Name Sym015 Phase 1/2 [9]
MOA Inhibitor
External Link
 Compound Name MK-2461 Phase 1/2 [25]
Synonyms
MK 2461
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 0.4 nM
External Link
 Compound Name REGN5093 Phase 1 [26]
MOA Inhibitor
External Link
 Compound Name PF-4217903 Phase 1 [27]
Synonyms
2-(4-(1-(Quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-yl)ethanol; PF-04217903; 956905-27-4; PF04217903; PF 04217903; UNII-CYJ9ATV1IJ; CYJ9ATV1IJ; CHEMBL2001019; 1159490-85-3; aka PF-04217903; C19H16N8O; 2-[4-(3-Quinolin-6-ylmethyl-3H-[1,2,3]triazolo[4,5-b]pyrazin-5-yl)-pyrazol-1-yl]-ethanol; 2-(4-(1-(Quinolin-6-ylmethyl)-1H-(1,2,3)triazolo(4,5-b)pyrazin-6-yl)-1H-pyrazol-1-yl)ethanol; 3zxz; PDMUGYOXRHVNMO-UHFFFAOYSA-N
    Click to Show/Hide
MOA Inhibitor
Activity EC50 = 0.3 nM
External Link
 Compound Name ABBV-399 Phase 1 [14]
MOA Inhibitor
External Link
 Compound Name CBT-101 Phase 1 [9]
Synonyms
L-Asparaginyl-L-leucyl-glycyl-L-valyl-L-[S-(acetamidomethyl)]cysteinamide hydrochloride
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name MK-8033 Phase 1 [28]
Synonyms
1001917-37-8; UNII-350H6PBQ5Q; 3-(1-Methyl-1H-pyrazol-4-yl)-5-oxo-N-(2-pyridinylmethyl)-5H-benzo[4,5]cyclohepta[1,2-b]pyridine-7-methanesulfonamide; 350H6PBQ5Q; CHEMBL2323775; MK8033; 1-(3-(1-Methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo(4,5)cyclohepta(1,2-b)pyridin-7-yl)-N-(pyridin-2-ylmethyl)methanesulfonamide; 1-[2-(1-methylpyrazol-4-yl)-11-oxobenzo[1,2]cyclohepta[2,4-b]pyridin-9-yl]-N-(pyridin-2-ylmethyl)methanesulfonamide
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 0.6 nM
External Link
 Compound Name Autologous T Cells Expressing MET scFv CAR Phase 1 [29]
MOA CAR-T-Cell-Therapy
External Link
 Compound Name ABT-700 Phase 1 [30]
MOA Modulator
External Link
 Compound Name Hepapoietin Phase 1 [31]
Synonyms
APS-1010; Hepapoietin, SnowBrand; Hepapoietin (liver/kidney disease); Hepapoietin (liver/kidney disease), Atlas Pharmaceuticals
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name EMD-1204831 Phase 1 [32]
MOA Inhibitor
External Link
 Compound Name JNJ-38877605 Phase 1 [33]
Synonyms
C-met inhibitor, Ortho Biotech Oncology Research & Development; C-met inhibitor (solid tumors), ORD/J&J PRD
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 0.95 nM
External Link
 Compound Name SGX523 Phase 1 [34]
Synonyms
SGX-523; SGX523, SGX-523
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 3.1 nM
External Link
 Compound Name TR1801-ADC Phase 1 [35]
External Link
 Compound Name LY3164530 Phase 1 [36]
MOA Modulator
External Link
 Compound Name C-Met/PD-L1 CAR-T Cell Phase 1 [37]
MOA CAR-T-Cell-Therapy(Dual specific)
External Link
 Compound Name E-7050 Phase 1 [38]
Synonyms
C-Met and VEGF-2 tyrosine kinase inhibitor (oral, cancer), Eisai
    Click to Show/Hide
MOA Modulator
Activity IC50 = 14 nM
External Link
 Compound Name XL092 Phase 1 [39]
Synonyms
SCHEMBL21200856; NSC828252; XL-092; NSC-828252; 2367004-54-2
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name BPI-9016 M Phase 1 [40]
MOA Inhibitor
External Link
 Compound Name AZD9592 Phase 1 [41]
External Link
 Compound Name TPX-0022 Phase 1 [42]
Synonyms
CSF1R-IN-2; SCHEMBL20694441; TPX0022; NSC820832; NSC-820832; HY-111787; CS-0091874; 2271119-26-5
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MOA Inhibitor
External Link
 Compound Name RXDX-106 Phase 1 [43]
Synonyms
CEP-40783; 1437321-24-8; CEP40783; UNII-1969ZJE05Q; 1969ZJE05Q; N-(4-((6,7-dimethoxyquinolin-4-yl)oxy)-3-fluorophenyl)-3-(4-fluorophenyl)-1-isopropyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide; N-[4-(6,7-dimethoxyquinolin-4-yl)oxy-3-fluorophenyl]-3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide; RXDX-106 (CEP-40783); SCHEMBL16089863; BCP25839; EX-A2540; MFCD28502441; NSC797770; s8570; AKOS032960472; ZINC205893112; CCG-270157; CS-6371; NSC-797770; SB18930; AC-31425; AS-35141; HY-100946; N-(4-((6,7-Dimethoxy-4-quinolinyl)oxy)-3-fluorophenyl)-3-(4-fluorophenyl)-1,2,3,4-tetrahydro-1-(1-methylethyl)-2,4-dioxo-5-pyrimidinecarboxamide
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Altiratinib Phase 1 [44]
MOA Inhibitor
Activity IC50 = 2.7 nM
External Link
 Compound Name Mteron-F1 Preclinical [45]
MOA Stimulator
External Link
 Compound Name NPS-1034 Preclinical [46]
Synonyms
1221713-92-3; CHEMBL3810063; 1-(4-fluorophenyl)-N-[3-fluoro-4-[(3-phenyl-1H-pyrrolo[2,3-b]pyridin-4-yl)oxy]phenyl]-2,3-dimethyl-5-oxopyrazole-4-carboxamide; N-(3-fluoro-4-((3-phenyl-1H-pyrrolo[2,3-b]pyridin-4-yl)oxy)phenyl)-2-(4-fluorophenyl)-1,5-dimethyl-3-oxo-2,3-dihydro-1H-pyrazole-4-carboxamide.; SCHEMBL1963111; BCP15998; NPS1034;NPS 1034; BDBM50172077; s7669; ZINC68204845; CCG-270007; NCGC00481564-01; AC-31427; AK685795; BS-14709; HY-100509; CS-0019643; N-(3-fluoro-4-((3-phenyl-1H-pyrrolo[2,3-b]pyridin-4-yl)oxy)phenyl)-2-(4-fluorophenyl)-1,5-dimethyl-3-oxo-2,3-dihydro-1H-pyrazole-4-carboxamide; S4K
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name ALD-805 Investigative [8]
External Link
 Compound Name PHA-665752 Investigative [8]
Synonyms
477575-56-7; PHA 665752; PHA665752; TCMDC-125885; UNII-0VXU5T5R3J; (2R)-1-[[5-[(Z)-[5-[[(2,6-DICHLOROPHENYL)METHYL]SULFONYL]-1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDENE]METHYL]-2,4-DIMETHYL-1H-PYRROL-3-YL]CARBONYL]-2-(1-PYRROLIDINYLMETHYL)PYRROLIDINE; 0VXU5T5R3J; CHEMBL450786; CHEBI:90197; (R,Z)-5-(2,6-dichlorobenzylsulfonyl)-3-((3,5-dimethyl-4-(2-(pyrrolidin-1-ylmethyl)pyrrolidine-1-carbonyl)-1H-pyrrol-2-yl)methylene)indolin-2-one; PHA-665752 hydrate
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MOA Inhibitor
Activity IC50 = 9 nM
External Link
 Compound Name APS-3010 Investigative [8]
Synonyms
Hepatic growth factor inhibitor (cancer), Atlas Pharmaceuticals
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MOA Inhibitor
External Link
 Compound Name LA-480 Investigative [8]
Synonyms
Bispecific c-Met monoclonal antibody (cancer), Lilly
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External Link
 Compound Name Anti-cMET mab Investigative [8]
Synonyms
Anti-cMET mAb (undisclosed indication); Anti-cMET mAb (undisclosed indication), PharmAbcine; CMET inhibitor (mAb, undisclosed indication), PharmAbcine
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name AM7 Investigative [47]
Synonyms
pyrimidone, 22; AM 7; AM-7
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 8.9 nM
External Link
 Compound Name mab 224G11 Investigative [8]
Synonyms
C-Met antagonist monoclonal antibody (cancer); C-Met antagonist monoclonal antibody (cancer), Pierre Fabre/Abbott
    Click to Show/Hide
External Link
 Compound Name TP-801 Investigative [8]
Synonyms
C-Met tyrosine kinase inhibitor (oral, cancer), Tiger Pharmatech
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name SU11274 Investigative [48]
Synonyms
Met kinase Inhibitor; SU-11274
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 10 nM
External Link
 Compound Name PF-00614435 Investigative [8]
Synonyms
PF-00658968; PF-00851623; PF-02311803; PF-4254644; PF-851623; PF-899555; C-Met (HGFR) inhibitors (cancer), Pfizer
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name CMET Avimer polypeptides Investigative [8]
Synonyms
CMET Avimer polypeptides (cancer); MEDI-555; CMET Avimer polypeptides (cancer), MedImmmue; CMET-targeting anticancer avimers, MedImmune; CMET-targeting avimers (cancer), Avidia/MedImmune
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MOA Inhibitor
External Link
 Compound Name PRS-110 Investigative [8]
Synonyms
C-Met inhibitor (cancer), Pieris; C-mesenchymal-epithelial transition factor (lipoprotein/protein recombinant, cancer), Pieris AG
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 1-benzyl-1H-pyrrolo[3,2-b]pyridine Investigative [49]
Synonyms
CHEMBL561256; 1-benzyl-4-azaindole; 1h-pyrrolo[3,2-b]pyridine,1-(phenylmethyl)-; SCHEMBL4716978; LOGFFHFLSCMKJF-UHFFFAOYSA-N; BDBM50295764; ZINC43079815; 50426-35-2
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 19 nM
External Link
 Compound Name RP-1040 Investigative [8]
Synonyms
RP-1086; RP-1087; RP-1088; RP-1101; RP-1103; RP-1105; RP-1109; RP-1110; RP-1111; RP-1112; C-Met kinase inhibitors (oral,cancer); C-Met kinase inhibitors (oral, cancer), Incozen Therapeutics/Rhizen Pharmaceuticals
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name BAY-85-3474 Investigative [8]
Synonyms
Met inhibitor (cancer), Bayer Schering
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name GE-137 Investigative [50]
MOA Modulator
External Link
 Compound Name 3-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridine Investigative [49]
Synonyms
CHEMBL538932; 633303-90-9; SCHEMBL3889418; CTK2A9458; DTXSID00621754; XIVJYIWQYBHEBJ-UHFFFAOYSA-N; BDBM50295740; 3-(Benzenesulfonyl)-1H-pyrrolo[2,3-b]pyridine; 1H-Pyrrolo[2,3-b]pyridine, 3-(phenylsulfonyl)-
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1175 nM
External Link
 Compound Name 1-(2-nitrophenethyl)-1H-pyrrolo[3,2-b]pyridine Investigative [49]
Synonyms
CHEMBL540744
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MOA Inhibitor
Activity IC50 = 250 nM
External Link
 Compound Name ALD-806 Investigative [8]
Synonyms
Anti-HGF mAb (cancer), Alder Biopharmaceuticals
    Click to Show/Hide
External Link
 Compound Name 1-(phenylsulfonyl)-1H-pyrrolo[3,2-b]pyridine Investigative [49]
Synonyms
1-(Phenylsulfonyl)-4-azaindole; 677302-44-2; CHEMBL556118; SCHEMBL3705420; HGOGRVVSSAWHTO-UHFFFAOYSA-N; BDBM50295729; ZINC42923799; AKOS032961360; KB-3354225
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 3500 nM
External Link
 Compound Name DP-3590 Investigative [8]
Synonyms
DP-4157; DP-4693; DP-4756; C-Met kinase inhibitors (solid tumor/metastatic cancer); C-Met kinase inhibitors (solid tumor/metastatic cancer), Deciphera
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MOA Inhibitor
External Link
 Compound Name HuMax-cMet Investigative [8]
Synonyms
CMet-targeting human IgG1 antibody (cancer), Genmab
    Click to Show/Hide
External Link
 Compound Name YH013 Investigative [51]
External Link
 Compound Name PMID24210504C1o Investigative [52]
Synonyms
GTPL8143; BDBM50444090
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MOA Inhibitor
Activity IC50 = 8 nM
External Link
 Compound Name PMID21123062C27 Investigative [53]
Synonyms
GTPL8210; BDBM50334085
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MOA Inhibitor
Activity IC50 = 44 nM
External Link
 Compound Name PMID21967808CR-16 Investigative [54]
Synonyms
GTPL8213; BDBM50361564
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 26 nM
External Link
 Compound Name BMS-536924 Investigative [55]
MOA Inhibitor
Activity IC50 = 4870 nM
External Link
2C25: Lung cancer 52 Compound(s) Regulating the Disease Click to Show/Hide the Full List
 Compound Name Adagrasib Approved [56]
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)-
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 Compound Name Amivantamab Approved [57]
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 Compound Name Mobocertinib Approved [58]
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
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 Compound Name Sugemalimab Approved in China [59]
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 Compound Name Sacituzumab govitecan Approved [60]
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
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 Compound Name Atezolizumab Approved [61]
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 Compound Name Tepotinib Approved [4]
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
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 Compound Name Sotorasib Approved [62]
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)-
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 Compound Name Entrectinib Approved [63]
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
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 Compound Name Repotrectinib Approved [64]
Synonyms
FIKPXCOQUIZNHB-RRKGBCIJSA-N; SCHEMBL20438940; TPX 0005; BCP19778
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 Compound Name MYL-1402O Phase 3 [65]
Synonyms
bevacizumab biosimilar
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 Compound Name AB154 Phase 3 [66]
Synonyms
Domvanalimab
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 Compound Name Datopotamab deruxtecan Phase 3 [67]
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 Compound Name CS1001 Phase 3 [68]
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 Compound Name JDQ443 Phase 3 [69]
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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 Compound Name TRS003 Phase 3 [70]
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 Compound Name Tusamitamab ravtansine Phase 3 [71]
Synonyms
SAR408701
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 Compound Name RG6058 Phase 3 [72]
Synonyms
Tiragolumab
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 Compound Name GSK4069889 Phase 2 [73]
Synonyms
TSR-022
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 Compound Name APL-101 Phase 2 [74]
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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 Compound Name SGN-LIV1A Phase 2 [75]
Synonyms
Ladiratuzumab Vedotin
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 Compound Name BNT116 Phase 2 [76]
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 Compound Name AZD7789 Phase 2 [77]
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 Compound Name L-DOS47 Phase 1/2 [78]
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 Compound Name NC318 Phase 2 [79]
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 Compound Name Vorolanib Phase 2 [80]
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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 Compound Name Xofigo Phase 2 [81]
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 Compound Name Bintrafusp alfa Phase 2 [82]
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 Compound Name Voyager-V1 Phase 2 [83]
Synonyms
VSV-IFNBeta-NIS
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 Compound Name AB-106 Phase 2 [84]
Synonyms
DS6051b; GTPL11198; AB106
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 Compound Name RO-5126766 Phase 2 [85]
Synonyms
VS-6766; CH-5126766; Dual Raf/MEK protein kinase inhibitor (cancer), Roche
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 Compound Name TC-210 Phase 1/2 [86]
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 Compound Name EMB-01 Phase 1/2 [87]
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 Compound Name NM21-1480 Phase 1/2 [88]
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 Compound Name MRx0518 Phase 1/2 [89]
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 Compound Name DZD9008 Phase 1/2 [90]
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 Compound Name BGB-A425 Phase 1/2 [91]
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 Compound Name Rilvegostomig Phase 1/2 [92]
Synonyms
AZD2936
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 Compound Name IK-007 Phase 1/2 [93]
Synonyms
grapiprant
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 Compound Name IBI318 Phase 1 [94]
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 Compound Name GEN-011 Phase 1 [95]
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 Compound Name ENV-105 Phase 1 [96]
Synonyms
Carotuximab
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 Compound Name AMG 160 Phase 1 [97]
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 Compound Name ADP-A2M10 Phase 1 [98]
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 Compound Name MEDI5752 Phase 1 [99]
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 Compound Name PF-07104091 Phase 1 [100]
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 Compound Name PF-06936308 Phase 1 [101]
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 Compound Name GEM3PSCA Phase 1 [102]
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 Compound Name PF-07257876 Phase 1 [103]
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 Compound Name Cosibelimab Phase 1 [104]
Synonyms
CK-301/TG-1501
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 Compound Name Gemcitabine Approved [7]
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 Compound Name SMI-4a Investigative [105]
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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References
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