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Assay Detail

CHEMBL5339368

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

Binding
Inhibition of c-Met (unknown origin)
9
Total Activities
9
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

Identification of (S)-1-(2-(2,4-difluorophenyl)-4-oxothiazolidin-3-yl)-3-(4-((7-(3-(4-ethylpiperazin-1-yl)propoxy)-6-methoxyquinolin-4-yl)oxy)-3,5-difluorophenyl)urea as a potential anti-colorectal cancer agent.
Qi B, Wang F, He H, Fan M, Hu L, Xiong L, Gong G, Shi S, Song X.
Eur J Med Chem (2022) 239 : 114561 -114561
PubMed 35763868 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 8.75 9.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3188267 CAPMATINIB 4.0 1 9.89
CHEMBL1230609 FORETINIB 2.0 1 9.40
CHEMBL2323775 MK-8033 1.0 1 9.00
CHEMBL2105717 CABOZANTINIB 4.0 1 8.89
CHEMBL460702 BMS-777607 2.0 1 8.41
CHEMBL2133806 JNJ-38877605 1.0 1 8.40
CHEMBL3402762 TEPOTINIB 4.0 1 8.40
CHEMBL5414779 1 8.22
CHEMBL601719 CRIZOTINIB 4.0 1 8.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3188267 CAPMATINIB IC50 = 0.13 nM 9.89
CHEMBL1230609 FORETINIB IC50 = 0.4 nM 9.40
CHEMBL2323775 MK-8033 IC50 = 1.0 nM 9.00
CHEMBL2105717 CABOZANTINIB IC50 = 1.3 nM 8.89
CHEMBL460702 BMS-777607 IC50 = 3.9 nM 8.41
CHEMBL2133806 JNJ-38877605 IC50 = 4.0 nM 8.40
CHEMBL3402762 TEPOTINIB IC50 = 4.0 nM 8.40
CHEMBL5414779 IC50 = 6.0 nM 8.22
CHEMBL601719 CRIZOTINIB IC50 = 8.0 nM 8.10