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Assay Detail

CHEMBL2182428

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

Binding
Inhibition of TGFBR1
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and SAR of b-annulated 1,4-dihydropyridines define cardiomyogenic compounds as novel inhibitors of TGFβ signaling.
Schade D, Lanier M, Willems E, Okolotowicz K, Bushway P, Wahlquist C, Gilley C, Mercola M, Cashman JR.
J Med Chem (2012) 55 : 9946 -9957
PubMed 23130626 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.29 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL261454 1 7.40
CHEMBL440084 SB-431542 1 7.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL261454 IC50 = 40.0 nM 7.40
CHEMBL440084 SB-431542 IC50 = 66.0 nM 7.18