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Assay Detail

CHEMBL889560

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

Binding
Inhibition of human recombinant ALK5 phosphorylation expressed in Sf9 cells
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Expert

Target

TGF-beta receptor type-1 (CHEMBL4439)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of 4(5)-(6-alkylpyridin-2-yl)imidazoles as transforming growth factor-beta type 1 receptor kinase inhibitors.
Kim DK, Jang Y, Lee HS, Park HJ, Yoo J.
J Med Chem (2007) 50 : 3143 -3147
PubMed 17552507 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.13 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL229599 1 8.00
CHEMBL387748 1 7.92
CHEMBL376119 1 7.82
CHEMBL389078 1 7.68
CHEMBL226734 1 7.62
CHEMBL229546 1 7.38
CHEMBL387747 1 7.34
CHEMBL229598 1 7.34
CHEMBL229548 1 7.33
CHEMBL229496 1 7.14
CHEMBL229654 1 7.12
CHEMBL226733 1 7.04
CHEMBL229547 1 6.92
CHEMBL445934 1 6.82
CHEMBL229495 1 6.76
CHEMBL229597 1 6.58
CHEMBL229497 1 6.44
CHEMBL389079 1 6.42
CHEMBL440084 SB-431542 1 5.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL229599 IC50 = 10.0 nM 8.00
CHEMBL387748 IC50 = 12.0 nM 7.92
CHEMBL376119 IC50 = 15.0 nM 7.82
CHEMBL389078 IC50 = 21.0 nM 7.68
CHEMBL226734 IC50 = 24.0 nM 7.62
CHEMBL229546 IC50 = 42.0 nM 7.38
CHEMBL387747 IC50 = 46.0 nM 7.34
CHEMBL229598 IC50 = 46.0 nM 7.34
CHEMBL229548 IC50 = 47.0 nM 7.33
CHEMBL229496 IC50 = 73.0 nM 7.14
CHEMBL229654 IC50 = 75.0 nM 7.12
CHEMBL226733 IC50 = 92.0 nM 7.04
CHEMBL229547 IC50 = 119.0 nM 6.92
CHEMBL445934 IC50 = 153.0 nM 6.82
CHEMBL229495 IC50 = 174.0 nM 6.76
CHEMBL229597 IC50 = 262.0 nM 6.58
CHEMBL229497 IC50 = 360.0 nM 6.44
CHEMBL389079 IC50 = 385.0 nM 6.42
CHEMBL440084 SB-431542 IC50 = 1542.0 nM 5.81