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Assay Detail

CHEMBL1003887

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Binding
Inhibition of MET
19
Total Activities
19
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 of pyrrolopyridine-pyridone based inhibitors of Met kinase: synthesis, X-ray crystallographic analysis, and biological activities.
Kim KS, Zhang L, Schmidt R, Cai ZW, Wei D, Williams DK, Lombardo LJ, Trainor GL, Xie D, Zhang Y, An Y, Sack JS, Tokarski JS, Darienzo C, Kamath A, Marathe P, Zhang Y, Lippy J, Jeyaseelan R, Wautlet B, Henley B, Gullo-Brown J, Manne V, Hunt JT, Fargnoli J, Borzilleri RM.
J Med Chem (2008) 51 : 5330 -5341
PubMed 18690676 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.73 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL459875 1 8.89
CHEMBL459876 1 8.74
CHEMBL509101 1 8.74
CHEMBL451809 1 8.72
CHEMBL503901 1 8.64
CHEMBL454356 1 8.55
CHEMBL454357 1 8.51
CHEMBL455386 1 8.47
CHEMBL508633 1 8.42
CHEMBL503139 1 8.30
CHEMBL453850 1 8.09
CHEMBL454101 1 8.00
CHEMBL453849 1 7.52
CHEMBL510316 1 7.16
CHEMBL508403 1 6.33
CHEMBL452306 1 6.00
CHEMBL508006 1 6.00
CHEMBL507573 1 6.00
CHEMBL451789 1 5.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL459875 IC50 = 1.3 nM 8.89
CHEMBL459876 IC50 = 1.8 nM 8.74
CHEMBL509101 IC50 = 1.8 nM 8.74
CHEMBL451809 IC50 = 1.9 nM 8.72
CHEMBL503901 IC50 = 2.3 nM 8.64
CHEMBL454356 IC50 = 2.8 nM 8.55
CHEMBL454357 IC50 = 3.1 nM 8.51
CHEMBL455386 IC50 = 3.4 nM 8.47
CHEMBL508633 IC50 = 3.8 nM 8.42
CHEMBL503139 IC50 = 5.0 nM 8.30
CHEMBL453850 IC50 = 8.2 nM 8.09
CHEMBL454101 IC50 = 10.0 nM 8.00
CHEMBL453849 IC50 = 30.0 nM 7.52
CHEMBL510316 IC50 = 70.0 nM 7.16
CHEMBL508403 IC50 = 470.0 nM 6.33
CHEMBL452306 IC50 = 1000.0 nM 6.00
CHEMBL508006 IC50 = 1000.0 nM 6.00
CHEMBL507573 IC50 = 1000.0 nM 6.00
CHEMBL451789 IC50 = 1400.0 nM 5.85