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Assay Detail

CHEMBL917703

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

Binding
Displacement of [3H]des-arg10, leu9-kallidin from human bradykinin B1 receptor expressed in CHO cells
11
Total Activities
11
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 Expert

Target

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

Publication

2,3-diaminopyridine bradykinin B1 receptor antagonists.
Kuduk SD, Ng C, Feng DM, Wai JM, Chang RS, Harrell CM, Murphy KL, Ransom RW, Reiss D, Ivarsson M, Mason G, Boyce S, Tang C, Prueksaritanont T, Freidinger RM, Pettibone DJ, Bock MG.
J Med Chem (2004) 47 : 6439 -6442
PubMed 15588075 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 8.81 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL225607 1 9.40
CHEMBL387638 1 9.30
CHEMBL222038 1 9.30
CHEMBL225218 1 9.15
CHEMBL221998 1 9.15
CHEMBL375288 1 9.10
CHEMBL225006 1 8.96
CHEMBL225133 1 8.92
CHEMBL374779 1 8.70
CHEMBL221984 1 8.22
CHEMBL197462 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL225607 Ki = 0.4 nM 9.40
CHEMBL387638 Ki = 0.5 nM 9.30
CHEMBL222038 Ki = 0.5 nM 9.30
CHEMBL225218 Ki = 0.7 nM 9.15
CHEMBL221998 Ki = 0.7 nM 9.15
CHEMBL375288 Ki = 0.8 nM 9.10
CHEMBL225006 Ki = 1.1 nM 8.96
CHEMBL225133 Ki = 1.2 nM 8.92
CHEMBL374779 Ki = 2.0 nM 8.70
CHEMBL221984 Ki = 6.0 nM 8.22
CHEMBL197462 Ki = 200.0 nM 6.70