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Assay Detail

CHEMBL3801041

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of recombinant c-Met (unknown origin) using poly (Glu, Tyr) 4:1 as substrate incubated for 60 mins by ELISA
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Hepatocyte growth factor receptor (CHEMBL3717)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 6-(difluoro(6-(4-fluorophenyl)-[1,2,4]triazolo[4,3-b][1,2,4]triazin-3-yl)methyl)quinoline as a highly potent and selective c-Met inhibitor.
Zhan Z, Peng X, Liu Q, Chen F, Ji Y, Yao S, Xi Y, Lin Y, Chen T, Xu Y, Ai J, Geng M, Duan W.
Eur J Med Chem (2016) 116 : 239 -251
PubMed 27061987 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 8.63 9.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3797911 1 9.72
CHEMBL3797579 1 9.62
CHEMBL3800471 1 9.38
CHEMBL3797914 1 9.34
CHEMBL3799192 1 9.31
CHEMBL3798905 1 9.30
CHEMBL3800420 1 9.30
CHEMBL3800559 1 9.23
CHEMBL3799263 1 9.05
CHEMBL2133806 JNJ-38877605 1.0 1 9.02
CHEMBL3800427 1 8.92
CHEMBL3800295 1 8.92
CHEMBL3797871 1 8.85
CHEMBL3798623 1 8.70
CHEMBL3797547 1 8.64
CHEMBL3798174 1 8.64
CHEMBL3797307 1 8.60
CHEMBL3800061 1 8.55
CHEMBL3798660 1 8.49
CHEMBL3799924 1 8.39
CHEMBL3798130 1 8.38
CHEMBL3798590 1 8.28
CHEMBL3798542 1 8.16
CHEMBL3798746 1 7.98
CHEMBL3798974 1 6.90
CHEMBL3799231 1 6.89
CHEMBL3798619 1 6.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3797911 IC50 = 0.19 nM 9.72
CHEMBL3797579 IC50 = 0.24 nM 9.62
CHEMBL3800471 IC50 = 0.42 nM 9.38
CHEMBL3797914 IC50 = 0.46 nM 9.34
CHEMBL3799192 IC50 = 0.49 nM 9.31
CHEMBL3798905 IC50 = 0.5 nM 9.30
CHEMBL3800420 IC50 = 0.5 nM 9.30
CHEMBL3800559 IC50 = 0.59 nM 9.23
CHEMBL3799263 IC50 = 0.9 nM 9.05
CHEMBL2133806 JNJ-38877605 IC50 = 0.95 nM 9.02
CHEMBL3800427 IC50 = 1.2 nM 8.92
CHEMBL3800295 IC50 = 1.2 nM 8.92
CHEMBL3797871 IC50 = 1.4 nM 8.85
CHEMBL3798623 IC50 = 2.0 nM 8.70
CHEMBL3797547 IC50 = 2.3 nM 8.64
CHEMBL3798174 IC50 = 2.3 nM 8.64
CHEMBL3797307 IC50 = 2.5 nM 8.60
CHEMBL3800061 IC50 = 2.8 nM 8.55
CHEMBL3798660 IC50 = 3.2 nM 8.49
CHEMBL3799924 IC50 = 4.1 nM 8.39
CHEMBL3798130 IC50 = 4.2 nM 8.38
CHEMBL3798590 IC50 = 5.3 nM 8.28
CHEMBL3798542 IC50 = 6.9 nM 8.16
CHEMBL3798746 IC50 = 10.5 nM 7.98
CHEMBL3798974 IC50 = 126.6 nM 6.90
CHEMBL3799231 IC50 = 129.2 nM 6.89
CHEMBL3798619 IC50 = 413.2 nM 6.38