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Assay Detail

CHEMBL4432475

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
21
Total Activities
21
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

Design, synthesis and biological evaluation of c-Met kinase inhibitors bearing 2-oxo-1,2-dihydroquinoline scaffold.
Cui H, Peng X, Liu J, Ma C, Ji Y, Zhang W, Geng M, Li Y.
Bioorg Med Chem Lett (2016) 26 : 4483 -4486
PubMed 27524312 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 8.43 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4443952 1 9.22
CHEMBL4578460 1 9.15
CHEMBL4539641 1 9.00
CHEMBL4476854 1 8.77
CHEMBL4552325 1 8.77
CHEMBL4582423 1 8.74
CHEMBL4437901 1 8.68
CHEMBL4467949 1 8.64
CHEMBL4461741 1 8.62
CHEMBL4458142 1 8.62
CHEMBL4468577 1 8.60
CHEMBL460702 BMS-777607 2.0 1 8.59
CHEMBL4473908 1 8.41
CHEMBL4589258 1 8.38
CHEMBL4455924 1 8.33
CHEMBL4528003 1 8.33
CHEMBL4583172 1 8.19
CHEMBL4542515 1 8.03
CHEMBL4571149 1 8.01
CHEMBL4527370 1 6.98
CHEMBL4461009 1 6.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4443952 IC50 = 0.6 nM 9.22
CHEMBL4578460 IC50 = 0.7 nM 9.15
CHEMBL4539641 IC50 = 1.0 nM 9.00
CHEMBL4476854 IC50 = 1.7 nM 8.77
CHEMBL4552325 IC50 = 1.7 nM 8.77
CHEMBL4582423 IC50 = 1.8 nM 8.74
CHEMBL4437901 IC50 = 2.1 nM 8.68
CHEMBL4467949 IC50 = 2.3 nM 8.64
CHEMBL4461741 IC50 = 2.4 nM 8.62
CHEMBL4458142 IC50 = 2.4 nM 8.62
CHEMBL4468577 IC50 = 2.5 nM 8.60
CHEMBL460702 BMS-777607 IC50 = 2.6 nM 8.59
CHEMBL4473908 IC50 = 3.9 nM 8.41
CHEMBL4589258 IC50 = 4.2 nM 8.38
CHEMBL4455924 IC50 = 4.7 nM 8.33
CHEMBL4528003 IC50 = 4.7 nM 8.33
CHEMBL4583172 IC50 = 6.4 nM 8.19
CHEMBL4542515 IC50 = 9.4 nM 8.03
CHEMBL4571149 IC50 = 9.7 nM 8.01
CHEMBL4527370 IC50 = 104.9 nM 6.98
CHEMBL4461009 IC50 = 132.7 nM 6.88