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Assay Detail

CHEMBL3792084

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 after 60 mins by ELISA
22
Total Activities
22
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 and synthesis of novel benzo[d]oxazol-2(3H)-one derivatives bearing 7-substituted-4-enthoxyquinoline moieties as c-Met kinase inhibitors.
Lu D, Shen A, Liu Y, Peng X, Xing W, Ai J, Geng M, Hu Y.
Eur J Med Chem (2016) 115 : 191 -200
PubMed 27017548 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 8.00 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL601719 CRIZOTINIB 4.0 1 9.05
CHEMBL3786898 1 9.00
CHEMBL3787612 1 8.47
CHEMBL3786136 1 8.46
CHEMBL3787354 1 8.42
CHEMBL3786610 1 8.42
CHEMBL3785650 1 8.29
CHEMBL3787278 1 8.25
CHEMBL3786574 1 8.23
CHEMBL3786217 1 8.22
CHEMBL3786924 1 8.12
CHEMBL3785213 1 8.01
CHEMBL3785800 1 7.96
CHEMBL3787308 1 7.80
CHEMBL3786658 1 7.72
CHEMBL3786588 1 7.71
CHEMBL3417482 1 7.70
CHEMBL3785106 1 7.47
CHEMBL3786146 1 7.37
CHEMBL3787185 1 7.32
CHEMBL3786753 1 7.03
CHEMBL3787205 1 6.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL601719 CRIZOTINIB IC50 = 0.9 nM 9.05
CHEMBL3786898 IC50 = 1.0 nM 9.00
CHEMBL3787612 IC50 = 3.4 nM 8.47
CHEMBL3786136 IC50 = 3.5 nM 8.46
CHEMBL3787354 IC50 = 3.8 nM 8.42
CHEMBL3786610 IC50 = 3.8 nM 8.42
CHEMBL3785650 IC50 = 5.1 nM 8.29
CHEMBL3787278 IC50 = 5.6 nM 8.25
CHEMBL3786574 IC50 = 5.9 nM 8.23
CHEMBL3786217 IC50 = 6.0 nM 8.22
CHEMBL3786924 IC50 = 7.6 nM 8.12
CHEMBL3785213 IC50 = 9.8 nM 8.01
CHEMBL3785800 IC50 = 11.0 nM 7.96
CHEMBL3787308 IC50 = 15.7 nM 7.80
CHEMBL3786658 IC50 = 18.9 nM 7.72
CHEMBL3786588 IC50 = 19.5 nM 7.71
CHEMBL3417482 IC50 = 20.0 nM 7.70
CHEMBL3785106 IC50 = 33.5 nM 7.47
CHEMBL3786146 IC50 = 42.3 nM 7.37
CHEMBL3787185 IC50 = 47.8 nM 7.32
CHEMBL3786753 IC50 = 93.6 nM 7.03
CHEMBL3787205 IC50 = 105.1 nM 6.98