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Assay Detail

CHEMBL971816

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

Binding
Inhibition of cMet by HTRF assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design, synthesis, and biological evaluation of potent c-Met inhibitors.
D'Angelo ND, Bellon SF, Booker SK, Cheng Y, Coxon A, Dominguez C, Fellows I, Hoffman D, Hungate R, Kaplan-Lefko P, Lee MR, Li C, Liu L, Rainbeau E, Reider PJ, Rex K, Siegmund A, Sun Y, Tasker AS, Xi N, Xu S, Yang Y, Zhang Y, Burgess TL, Dussault I, Kim TS.
J Med Chem (2008) 51 : 5766 -5779
PubMed 18763753 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 7.45 8.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL447602 1 8.47
CHEMBL453737 1 8.31
CHEMBL505896 1 8.05
CHEMBL449833 1 8.04
CHEMBL452680 1 8.02
CHEMBL450209 1 7.92
CHEMBL461831 1 7.85
CHEMBL460791 1 7.77
CHEMBL444560 1 7.77
CHEMBL451069 1 7.68
CHEMBL502331 1 7.54
CHEMBL500834 1 7.52
CHEMBL445958 1 7.48
CHEMBL461832 1 7.42
CHEMBL461648 1 7.41
CHEMBL462493 1 7.35
CHEMBL500536 1 7.28
CHEMBL518208 1 7.20
CHEMBL508350 1 7.15
CHEMBL459948 1 7.14
CHEMBL460774 1 7.05
CHEMBL460586 1 6.97
CHEMBL447894 1 6.87
CHEMBL460772 1 6.70
CHEMBL449159 1 6.43
CHEMBL460795 1 6.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL447602 Ki = 3.4 nM 8.47
CHEMBL453737 Ki = 4.9 nM 8.31
CHEMBL505896 Ki = 8.9 nM 8.05
CHEMBL449833 Ki = 9.2 nM 8.04
CHEMBL452680 Ki = 9.6 nM 8.02
CHEMBL450209 Ki = 12.0 nM 7.92
CHEMBL461831 Ki = 14.0 nM 7.85
CHEMBL460791 Ki = 17.0 nM 7.77
CHEMBL444560 Ki = 17.0 nM 7.77
CHEMBL451069 Ki = 21.0 nM 7.68
CHEMBL502331 Ki = 29.0 nM 7.54
CHEMBL500834 Ki = 30.0 nM 7.52
CHEMBL445958 Ki = 33.0 nM 7.48
CHEMBL461832 Ki = 38.0 nM 7.42
CHEMBL461648 Ki = 39.0 nM 7.41
CHEMBL462493 Ki = 45.0 nM 7.35
CHEMBL500536 Ki = 52.0 nM 7.28
CHEMBL518208 Ki = 63.0 nM 7.20
CHEMBL508350 Ki = 71.0 nM 7.15
CHEMBL459948 Ki = 72.0 nM 7.14
CHEMBL460774 Ki = 89.0 nM 7.05
CHEMBL460586 Ki = 107.0 nM 6.97
CHEMBL447894 Ki = 136.0 nM 6.87
CHEMBL460772 Ki = 201.0 nM 6.70
CHEMBL449159 Ki = 368.0 nM 6.43
CHEMBL460795 Ki = 489.0 nM 6.31