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Assay Detail

CHEMBL952241

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

Binding
Displacement of [3H]des-arg10leu9kallidin from human bradykinin B1 receptor expressed in CHO cells by Wallac beta-plate scintillation counting
11
Total Activities
10
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

B1 bradykinin receptor (CHEMBL4308)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Bradykinin B1 receptor antagonists: an alpha-hydroxy amide with an improved metabolism profile.
Kuduk SD, Chang RK, Dipardo RM, Di Marco CN, Murphy KL, Ransom RW, Reiss DR, Tang C, Prueksaritanont T, Pettibone DJ, Bock MG.
Bioorg Med Chem Lett (2008) 18 : 5107 -5110
PubMed 18722115 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 9.17 9.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL496530 1 9.41
CHEMBL484055 1 9.39
CHEMBL521735 1 9.32
CHEMBL402831 1 9.30
CHEMBL484881 1 9.17
CHEMBL484882 2 9.17
CHEMBL482829 1 9.16
CHEMBL496529 1 9.10
CHEMBL483858 1 9.02
CHEMBL521454 1 8.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL496530 Ki = 0.39 nM 9.41
CHEMBL484055 Ki = 0.41 nM 9.39
CHEMBL521735 Ki = 0.48 nM 9.32
CHEMBL402831 Ki = 0.5 nM 9.30
CHEMBL484881 Ki = 0.67 nM 9.17
CHEMBL484882 Ki = 0.67 nM 9.17
CHEMBL482829 Ki = 0.69 nM 9.16
CHEMBL496529 Ki = 0.8 nM 9.10
CHEMBL483858 Ki = 0.96 nM 9.02
CHEMBL484882 Ki = 1.0 nM 9.00
CHEMBL521454 Ki = 1.6 nM 8.80