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Assay Detail

CHEMBL5521817

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

Binding
Inhibition of c-Met (unknown origin)
4
Total Activities
4
Compounds Tested
2
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

Rational Design of PARP1/c-Met Dual Inhibitors for Overcoming PARP1 Inhibitor Resistance Induced by c-Met Overexpression.
Sun Z, Li L, Zhai B, Hu M, Huang L, Huang S, Ye L, Kong X, Xu J, Bai J, Yan J, Zhou Q, Hu Z, Zhang Y, Jiang Y, Zhang Y, Qiao Z, Zou Y, Xu Y, Zhu Q.
J Med Chem (2024) 67 : 4916 -4935
PubMed 38477575 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.80 9.40
Ki 1 6.47 6.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1230609 FORETINIB 2.0 1 9.40
CHEMBL2105717 CABOZANTINIB 4.0 1 8.89
CHEMBL601719 CRIZOTINIB 4.0 1 8.10
CHEMBL2103882 TIVANTINIB 3.0 1 6.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1230609 FORETINIB IC50 = 0.4 nM 9.40
CHEMBL2105717 CABOZANTINIB IC50 = 1.3 nM 8.89
CHEMBL601719 CRIZOTINIB IC50 = 8.0 nM 8.10
CHEMBL2103882 TIVANTINIB Ki = 335.0 nM 6.47