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Assay Detail

CHEMBL1038131

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

Binding
Inhibition of HGF-mediated human c-Met autophosphorylation expressed in human PC3 cells after 1 hr by electrochemiluminescent immunoassay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type PC-3
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors.
Boezio AA, Berry L, Albrecht BK, Bauer D, Bellon SF, Bode C, Chen A, Choquette D, Dussault I, Fang M, Hirai S, Kaplan-Lefko P, Larrow JF, Lin MH, Lohman J, Potashman MH, Qu Y, Rex K, Santostefano M, Shah K, Shimanovich R, Springer SK, Teffera Y, Yang Y, Zhang Y, Harmange JC.
Bioorg Med Chem Lett (2009) 19 : 6307 -6312
PubMed 19819693 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.09 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL568138 1 8.52
CHEMBL566685 1 8.52
CHEMBL566242 1 8.15
CHEMBL565843 1 8.15
CHEMBL566875 1 7.85
CHEMBL496102 AMG-208 2.0 1 7.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL568138 IC50 = 3.0 nM 8.52
CHEMBL566685 IC50 = 3.0 nM 8.52
CHEMBL566242 IC50 = 7.0 nM 8.15
CHEMBL565843 IC50 = 7.0 nM 8.15
CHEMBL566875 IC50 = 14.0 nM 7.85
CHEMBL496102 AMG-208 IC50 = 46.0 nM 7.34