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Assay Detail

CHEMBL3777322

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

Binding
Displacement of [3H]BK from cloned human B2 bradykinin receptor expressed in CHO cells after 2 hrs by liquid scintillation counter
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

B2 bradykinin receptor (CHEMBL3157)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Tactical Approaches to Interconverting GPCR Agonists and Antagonists.
Dosa PI, Amin EA.
J Med Chem (2016) 59 : 810 -840
PubMed 26390077 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.82 9.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3774617 1 9.44
CHEMBL99869 1 9.39
CHEMBL439737 1 8.96
CHEMBL1195824 1 7.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3774617 IC50 = 0.36 nM 9.44
CHEMBL99869 IC50 = 0.41 nM 9.39
CHEMBL439737 IC50 = 1.1 nM 8.96
CHEMBL1195824 IC50 = 34.0 nM 7.47