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Assay Detail

CHEMBL4339088

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

Binding
Inhibition of TGFBR1 in human whole blood assessed as apparent inhibition constant by measuring reduction in TGFbeta-induced SMAD phosphorylation
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

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
Ki 1 9.10 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4514379 1 9.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4514379 Ki = 0.8 nM 9.10