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Assay Detail

CHEMBL4376027

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

Binding
Inhibition of recombinant human N-terminal GST-tagged TGFbeta1 receptor (80 to end residues) expressed in baculovirus infected Sf9 insect cells using casein as substrate measured after 2 hrs by ADP-Glo assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Germacrane Sesquiterpenoids as a New Type of Anticardiac Fibrosis Agent Targeting Transforming Growth Factor β Type I Receptor.
Lou LL, Ni FQ, Chen L, Shaker S, Li W, Wang R, Tang GH, Yin S.
J Med Chem (2019) 62 : 7961 -7975
PubMed 31408333 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.50 7.83

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4533719 1 7.83
CHEMBL440084 SB-431542 1 7.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4533719 IC50 = 14.9 nM 7.83
CHEMBL440084 SB-431542 IC50 = 67.1 nM 7.17