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Assay Detail

CHEMBL653556

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Binding
Inhibition of human bradykinin B1 receptor
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Benzodiazepines as potent and selective bradykinin B1 antagonists.
Wood MR, Kim JJ, Han W, Dorsey BD, Homnick CF, DiPardo RM, Kuduk SD, MacNeil T, Murphy KL, Lis EV, Ransom RW, Stump GL, Lynch JJ, O'Malley SS, Miller PJ, Chen TB, Harrell CM, Chang RS, Sandhu P, Ellis JD, Bondiskey PJ, Pettibone DJ, Freidinger RM, Bock MG.
J Med Chem (2003) 46 : 1803 -1806
PubMed 12723943 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.71 9.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1253497 1 9.23
CHEMBL1744084 1 8.88
CHEMBL1744083 1 8.86
CHEMBL1744082 1 8.24
CHEMBL1744085 1 7.87
CHEMBL52498 1 7.55
CHEMBL50208 1 7.26
CHEMBL299164 1 7.07
CHEMBL298860 1 7.01
CHEMBL30525 1 6.85
CHEMBL1788318 1 5.99
CHEMBL298158 1 -
CHEMBL299106 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1253497 Ki = 0.59 nM 9.23
CHEMBL1744084 Ki = 1.33 nM 8.88
CHEMBL1744083 Ki = 1.37 nM 8.86
CHEMBL1744082 Ki = 5.73 nM 8.24
CHEMBL1744085 Ki = 13.4 nM 7.87
CHEMBL52498 Ki = 28.0 nM 7.55
CHEMBL50208 Ki = 55.0 nM 7.26
CHEMBL299164 Ki = 85.0 nM 7.07
CHEMBL298860 Ki = 97.5 nM 7.01
CHEMBL30525 Ki = 141.0 nM 6.85
CHEMBL1788318 Ki = 1023.0 nM 5.99
CHEMBL298158 Ki > 10000.0 nM -
CHEMBL299106 Ki > 10000.0 nM -