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Assay Detail

CHEMBL642728

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

Binding
Inhibition of Activin like receptor kinase 5, TGF beta type I receptor
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Identification of novel inhibitors of the transforming growth factor beta1 (TGF-beta1) type 1 receptor (ALK5).
Callahan JF, Burgess JL, Fornwald JA, Gaster LM, Harling JD, Harrington FP, Heer J, Kwon C, Lehr R, Mathur A, Olson BA, Weinstock J, Laping NJ.
J Med Chem (2002) 45 : 999 -1001
PubMed 11855979 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.00 7.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL440084 SB-431542 1 7.03
CHEMBL6250 1 6.77
CHEMBL267228 1 6.58
CHEMBL6252 1 6.40
CHEMBL268889 1 6.34
CHEMBL269339 1 5.82
CHEMBL266706 1 5.80
CHEMBL269341 1 5.53
CHEMBL6204 1 5.29
CHEMBL6304 1 5.24
CHEMBL10 SB-203580 1 5.22
CHEMBL266707 1 -
CHEMBL6294 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL440084 SB-431542 IC50 = 94.0 nM 7.03
CHEMBL6250 IC50 = 170.0 nM 6.77
CHEMBL267228 IC50 = 260.0 nM 6.58
CHEMBL6252 IC50 = 400.0 nM 6.40
CHEMBL268889 IC50 = 460.0 nM 6.34
CHEMBL269339 IC50 = 1500.0 nM 5.82
CHEMBL266706 IC50 = 1600.0 nM 5.80
CHEMBL269341 IC50 = 2950.0 nM 5.53
CHEMBL6204 IC50 = 5100.0 nM 5.29
CHEMBL6304 IC50 = 5800.0 nM 5.24
CHEMBL10 SB-203580 IC50 = 6000.0 nM 5.22
CHEMBL266707 IC50 > 50000.0 nM -
CHEMBL6294 IC50 > 50000.0 nM -