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Assay Detail

CHEMBL2032485

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

Binding
Inhibition of recombinant c-met-mediated gastrin phosphorylation by HTRF assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Structure-based design of novel class II c-Met inhibitors: 1. Identification of pyrazolone-based derivatives.
Norman MH, Liu L, Lee M, Xi N, Fellows I, D'Angelo ND, Dominguez C, Rex K, Bellon SF, Kim TS, Dussault I.
J Med Chem (2012) 55 : 1858 -1867
PubMed 22320343 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.89 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2031893 1 9.00
CHEMBL573761 1 8.77
CHEMBL404881 1 8.40
CHEMBL2032039 1 8.32
CHEMBL2032033 1 7.86
CHEMBL518208 1 7.85
CHEMBL2032037 1 7.42
CHEMBL2032034 1 7.25
CHEMBL2032036 1 7.22
CHEMBL2032035 1 6.85
CHEMBL2032038 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2031893 Ki = 1.0 nM 9.00
CHEMBL573761 Ki = 1.7 nM 8.77
CHEMBL404881 Ki = 4.0 nM 8.40
CHEMBL2032039 Ki = 4.8 nM 8.32
CHEMBL2032033 Ki = 13.7 nM 7.86
CHEMBL518208 Ki = 14.0 nM 7.85
CHEMBL2032037 Ki = 37.8 nM 7.42
CHEMBL2032034 Ki = 56.7 nM 7.25
CHEMBL2032036 Ki = 60.2 nM 7.22
CHEMBL2032035 Ki = 140.0 nM 6.85
CHEMBL2032038 Ki > 20000.0 nM -