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Assay Detail

CHEMBL953404

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Binding
Inhibition of Met kinase
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 orally active pyrrolopyridine- and aminopyridine-based Met kinase inhibitors.
Cai ZW, Wei D, Schroeder GM, Cornelius LA, Kim K, Chen XT, Schmidt RJ, Williams DK, Tokarski JS, An Y, Sack JS, Manne V, Kamath A, Zhang Y, Marathe P, Hunt JT, Lombardo LJ, Fargnoli J, Borzilleri RM.
Bioorg Med Chem Lett (2008) 18 : 3224 -3229
PubMed 18479916 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.90 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL525260 1 8.70
CHEMBL524364 1 8.70
CHEMBL502531 1 8.70
CHEMBL500157 1 8.52
CHEMBL499886 1 8.40
CHEMBL525049 1 8.40
CHEMBL526929 1 8.30
CHEMBL499885 1 8.30
CHEMBL500422 1 8.30
CHEMBL502283 1 8.15
CHEMBL502232 1 7.96
CHEMBL508142 1 7.96
CHEMBL502544 1 7.72
CHEMBL527066 1 7.46
CHEMBL499878 1 7.36
CHEMBL500921 1 7.19
CHEMBL499618 1 7.00
CHEMBL503090 1 6.96
CHEMBL253223 1 6.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL525260 IC50 = 2.0 nM 8.70
CHEMBL524364 IC50 = 2.0 nM 8.70
CHEMBL502531 IC50 = 2.0 nM 8.70
CHEMBL500157 IC50 = 3.0 nM 8.52
CHEMBL499886 IC50 = 4.0 nM 8.40
CHEMBL525049 IC50 = 4.0 nM 8.40
CHEMBL526929 IC50 = 5.0 nM 8.30
CHEMBL499885 IC50 = 5.0 nM 8.30
CHEMBL500422 IC50 = 5.0 nM 8.30
CHEMBL502283 IC50 = 7.0 nM 8.15
CHEMBL502232 IC50 = 11.0 nM 7.96
CHEMBL508142 IC50 = 11.0 nM 7.96
CHEMBL502544 IC50 = 19.0 nM 7.72
CHEMBL527066 IC50 = 35.0 nM 7.46
CHEMBL499878 IC50 = 44.0 nM 7.36
CHEMBL500921 IC50 = 64.0 nM 7.19
CHEMBL499618 IC50 = 100.0 nM 7.00
CHEMBL503090 IC50 = 110.0 nM 6.96
CHEMBL253223 IC50 = 780.0 nM 6.11