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Assay Detail

CHEMBL4193718

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

Binding
Inhibition of recombinant human His-tagged c-Met cytoplasmic domain (956 to 1390 residues) expressed in baculovirus expression system using poly (Glu,Tyr)4:1 as substrate after 60 mins by spectrophotometric analysis
19
Total Activities
19
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 the First c-Met/HDAC Inhibitors Based on Pyridazinone Derivatives.
Lu D, Yan J, Wang L, Liu H, Zeng L, Zhang M, Duan W, Ji Y, Cao J, Geng M, Shen A, Hu Y.
ACS Med Chem Lett (2017) 8 : 830 -834
PubMed 28835797 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 8.88 9.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4214018 1 9.36
CHEMBL4209174 1 9.27
CHEMBL4207111 1 9.20
CHEMBL4204833 1 9.15
CHEMBL4204308 1 9.14
CHEMBL3417489 1 9.08
CHEMBL4205747 1 9.02
CHEMBL4209005 1 9.02
CHEMBL4209562 1 9.00
CHEMBL4208236 1 9.00
CHEMBL4207710 1 8.96
CHEMBL4203363 1 8.92
CHEMBL4209189 1 8.89
CHEMBL4218410 1 8.82
CHEMBL4204322 1 8.43
CHEMBL4210834 1 8.29
CHEMBL4216512 1 7.43
CHEMBL98 VORINOSTAT 4.0 1 -
CHEMBL3621988 TUCIDINOSTAT 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4214018 IC50 = 0.44 nM 9.36
CHEMBL4209174 IC50 = 0.54 nM 9.27
CHEMBL4207111 IC50 = 0.63 nM 9.20
CHEMBL4204833 IC50 = 0.71 nM 9.15
CHEMBL4204308 IC50 = 0.73 nM 9.14
CHEMBL3417489 IC50 = 0.84 nM 9.08
CHEMBL4205747 IC50 = 0.96 nM 9.02
CHEMBL4209005 IC50 = 0.96 nM 9.02
CHEMBL4209562 IC50 = 1.0 nM 9.00
CHEMBL4208236 IC50 = 1.0 nM 9.00
CHEMBL4207710 IC50 = 1.1 nM 8.96
CHEMBL4203363 IC50 = 1.2 nM 8.92
CHEMBL4209189 IC50 = 1.3 nM 8.89
CHEMBL4218410 IC50 = 1.5 nM 8.82
CHEMBL4204322 IC50 = 3.7 nM 8.43
CHEMBL4210834 IC50 = 5.1 nM 8.29
CHEMBL4216512 IC50 = 37.0 nM 7.43
CHEMBL98 VORINOSTAT IC50 - -
CHEMBL3621988 TUCIDINOSTAT IC50 - -