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Assay Detail

CHEMBL953206

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

Binding
Inhibition of HGF-mediated c-Met phosphorylation in serum-starved human PC2 cells
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type PC2
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery and optimization of triazolopyridazines as potent and selective inhibitors of the c-Met kinase.
Albrecht BK, Harmange JC, Bauer D, Berry L, Bode C, Boezio AA, Chen A, Choquette D, Dussault I, Fridrich C, Hirai S, Hoffman D, Larrow JF, Kaplan-Lefko P, Lin J, Lohman J, Long AM, Moriguchi J, O'Connor A, Potashman MH, Reese M, Rex K, Siegmund A, Shah K, Shimanovich R, Springer SK, Teffera Y, Yang Y, Zhang Y, Bellon SF.
J Med Chem (2008) 51 : 2879 -2882
PubMed 18426196 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.83 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL523413 1 8.70
CHEMBL497118 1 8.70
CHEMBL494985 1 8.70
CHEMBL494984 1 8.52
CHEMBL523386 1 8.22
CHEMBL494979 1 8.15
CHEMBL494630 1 7.85
CHEMBL494983 1 7.80
CHEMBL494793 1 7.70
CHEMBL522196 1 7.58
CHEMBL497117 1 7.54
CHEMBL497968 1 7.38
CHEMBL496102 AMG-208 2.0 1 7.34
CHEMBL497119 1 6.88
CHEMBL494794 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL523413 IC50 = 2.0 nM 8.70
CHEMBL497118 IC50 = 2.0 nM 8.70
CHEMBL494985 IC50 = 2.0 nM 8.70
CHEMBL494984 IC50 = 3.0 nM 8.52
CHEMBL523386 IC50 = 6.0 nM 8.22
CHEMBL494979 IC50 = 7.0 nM 8.15
CHEMBL494630 IC50 = 14.0 nM 7.85
CHEMBL494983 IC50 = 16.0 nM 7.80
CHEMBL494793 IC50 = 20.0 nM 7.70
CHEMBL522196 IC50 = 26.0 nM 7.58
CHEMBL497117 IC50 = 29.0 nM 7.54
CHEMBL497968 IC50 = 42.0 nM 7.38
CHEMBL496102 AMG-208 IC50 = 46.0 nM 7.34
CHEMBL497119 IC50 = 132.0 nM 6.88
CHEMBL494794 IC50 = 400.0 nM 6.40