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Assay Detail

CHEMBL4427615

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

Binding
Inhibition of ALK5 in TGF beta1-stimulated HEK293T cells by SMAD binding element-driven beta lactamase reporter gene assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Design, synthesis and optimization of novel Alk5 (activin-like kinase 5) inhibitors.
Wang H, Lawson JD, Scorah N, Kamran R, Hixon MS, Atienza J, Dougan DR, Sabat M.
Bioorg Med Chem Lett (2016) 26 : 4334 -4339
PubMed 27460209 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 15 7.39 8.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4467267 1 8.04
CHEMBL4470706 1 8.02
CHEMBL4452818 1 7.78
CHEMBL4555703 1 7.75
CHEMBL4443611 1 7.75
CHEMBL4437930 1 7.70
CHEMBL4447510 1 7.70
CHEMBL4483492 1 7.65
CHEMBL4446613 1 7.60
CHEMBL4576833 1 7.30
CHEMBL4470980 1 7.29
CHEMBL4572312 1 6.80
CHEMBL4564126 TP-008 1 6.63
CHEMBL4569690 1 6.48
CHEMBL4515962 1 6.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4467267 EC50 = 9.12 nM 8.04
CHEMBL4470706 EC50 = 9.55 nM 8.02
CHEMBL4452818 EC50 = 16.6 nM 7.78
CHEMBL4555703 EC50 = 17.78 nM 7.75
CHEMBL4443611 EC50 = 17.78 nM 7.75
CHEMBL4437930 EC50 = 19.95 nM 7.70
CHEMBL4447510 EC50 = 19.95 nM 7.70
CHEMBL4483492 EC50 = 22.39 nM 7.65
CHEMBL4446613 EC50 = 25.12 nM 7.60
CHEMBL4576833 EC50 = 50.12 nM 7.30
CHEMBL4470980 EC50 = 51.29 nM 7.29
CHEMBL4572312 EC50 = 158.49 nM 6.80
CHEMBL4564126 TP-008 EC50 = 234.42 nM 6.63
CHEMBL4569690 EC50 = 331.13 nM 6.48
CHEMBL4515962 EC50 = 457.09 nM 6.34