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Assay Detail

CHEMBL4339043

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

Binding
Inhibition of TGFbetaR1 in TGFbeta-stimulated mouse NIH3T3 cells assessed as reduction in SMAD3 phosphorylation
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type NIH3T3
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

TGF-beta receptor type-1 (CHEMBL2021750)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGFβR1 Inhibitor as an Immuno-oncology Agent.
Velaparthi U, Darne CP, Warrier J, Liu P, Rahaman H, Augustine-Rauch K, Parrish K, Yang Z, Swanson J, Brown J, Dhar G, Anandam A, Holenarsipur VK, Palanisamy K, Wautlet BS, Fereshteh MP, Lippy J, Tebben AJ, Sheriff S, Ruzanov M, Yan C, Gupta A, Gupta AK, Vetrichelvan M, Mathur A, Gelman M, Singh R, Kinsella T, Murtaza A, Fargnoli J, Vite G, Borzilleri RM.
ACS Med Chem Lett (2020) 11 : 172 -178
PubMed 32071685 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.30 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4514379 1 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4514379 IC50 = 50.0 nM 7.30