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Assay Detail

CHEMBL953205

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Binding
Inhibition of c-Met by HTRF assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

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 20 7.94 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL494985 1 9.00
CHEMBL497118 1 9.00
CHEMBL523386 1 8.70
CHEMBL523413 1 8.52
CHEMBL494984 1 8.52
CHEMBL497117 1 8.40
CHEMBL494979 1 8.40
CHEMBL498769 1 8.22
CHEMBL494983 1 8.22
CHEMBL494793 1 8.15
CHEMBL494630 1 8.15
CHEMBL522196 1 8.05
CHEMBL496102 AMG-208 2.0 1 8.05
CHEMBL505896 1 8.00
CHEMBL497968 1 7.92
CHEMBL497119 1 7.54
CHEMBL494794 1 7.17
CHEMBL495898 1 6.92
CHEMBL495899 1 6.21
CHEMBL496101 1 5.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL494985 IC50 = 1.0 nM 9.00
CHEMBL497118 IC50 = 1.0 nM 9.00
CHEMBL523386 IC50 = 2.0 nM 8.70
CHEMBL523413 IC50 = 3.0 nM 8.52
CHEMBL494984 IC50 = 3.0 nM 8.52
CHEMBL497117 IC50 = 4.0 nM 8.40
CHEMBL494979 IC50 = 4.0 nM 8.40
CHEMBL498769 IC50 = 6.0 nM 8.22
CHEMBL494983 IC50 = 6.0 nM 8.22
CHEMBL494793 IC50 = 7.0 nM 8.15
CHEMBL494630 IC50 = 7.0 nM 8.15
CHEMBL522196 IC50 = 9.0 nM 8.05
CHEMBL496102 AMG-208 IC50 = 9.0 nM 8.05
CHEMBL505896 IC50 = 10.0 nM 8.00
CHEMBL497968 IC50 = 12.0 nM 7.92
CHEMBL497119 IC50 = 29.0 nM 7.54
CHEMBL494794 IC50 = 67.0 nM 7.17
CHEMBL495898 IC50 = 120.0 nM 6.92
CHEMBL495899 IC50 = 610.0 nM 6.21
CHEMBL496101 IC50 = 2100.0 nM 5.68