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Assay Detail

CHEMBL5369205

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

Binding
Inhibition of c-Met (unknown origin)
5
Total Activities
5
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

Discovery of Novel, Thienopyridine-Based Tyrosine Kinase Inhibitors Targeting Tumorigenic RON Splice Variants.
Ryu H, Kim H, Park I, Lee M, Park YS, Jin DH, Hur SC, Park J, Lee H.
ACS Med Chem Lett (2023) 14 : 1198 -1207
PubMed 37736180 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.35 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2105717 CABOZANTINIB 4.0 1 8.89
CHEMBL5404435 1 8.40
CHEMBL3545307 MERESTINIB 2.0 1 8.33
CHEMBL601719 CRIZOTINIB 4.0 1 8.10
CHEMBL445799 1 8.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2105717 CABOZANTINIB IC50 = 1.3 nM 8.89
CHEMBL5404435 IC50 = 4.0 nM 8.40
CHEMBL3545307 MERESTINIB IC50 = 4.7 nM 8.33
CHEMBL601719 CRIZOTINIB IC50 = 8.0 nM 8.10
CHEMBL445799 IC50 = 9.0 nM 8.05