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Assay Detail

CHEMBL3269341

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

Binding
Inhibition of GST-fused recombinant human ALK5 expressed in baculovirus-infected insect Sf9 cells using casein as substrate by radioisotope-based assay
16
Total Activities
16
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 Autocuration

Target

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

Publication

4-([1,2,4]Triazolo[1,5-a]pyridin-6-yl)-5(3)-(6-methylpyridin-2-yl)imidazole and -pyrazole derivatives as potent and selective inhibitors of transforming growth factor-β type I receptor kinase.
Jin CH, Krishnaiah M, Sreenu D, Subrahmanyam VB, Park HJ, Park SJ, Sheen YY, Kim DK.
Bioorg Med Chem (2014) 22 : 2724 -2732
PubMed 24704197 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.39 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL492634 1 7.77
CHEMBL3261096 1 7.75
CHEMBL3261090 1 7.66
CHEMBL3261093 1 7.57
CHEMBL3261088 1 7.57
CHEMBL3261095 1 7.54
CHEMBL3261094 1 7.44
CHEMBL3261089 1 7.44
CHEMBL3261084 1 7.43
CHEMBL3261087 1 7.32
CHEMBL226838 1 7.27
CHEMBL3261083 1 7.24
CHEMBL3261091 1 7.11
CHEMBL3261092 1 7.07
CHEMBL3261085 1 7.05
CHEMBL3261086 1 6.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL492634 IC50 = 17.0 nM 7.77
CHEMBL3261096 IC50 = 18.0 nM 7.75
CHEMBL3261090 IC50 = 22.0 nM 7.66
CHEMBL3261093 IC50 = 27.0 nM 7.57
CHEMBL3261088 IC50 = 27.0 nM 7.57
CHEMBL3261095 IC50 = 29.0 nM 7.54
CHEMBL3261094 IC50 = 36.0 nM 7.44
CHEMBL3261089 IC50 = 36.0 nM 7.44
CHEMBL3261084 IC50 = 37.0 nM 7.43
CHEMBL3261087 IC50 = 48.0 nM 7.32
CHEMBL226838 IC50 = 54.0 nM 7.27
CHEMBL3261083 IC50 = 57.0 nM 7.24
CHEMBL3261091 IC50 = 78.0 nM 7.11
CHEMBL3261092 IC50 = 85.0 nM 7.07
CHEMBL3261085 IC50 = 90.0 nM 7.05
CHEMBL3261086 IC50 = 106.0 nM 6.97