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Assay Detail

CHEMBL653555

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Binding
Compound was tested for inhibition against human bradykinin B1 receptor using FLIPR assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

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
IC50 7 7.48 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1253497 1 8.72
CHEMBL1744083 1 8.32
CHEMBL1744084 1 8.10
CHEMBL1744082 1 7.61
CHEMBL1744085 1 7.19
CHEMBL52498 1 6.79
CHEMBL1788318 1 5.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1253497 IC50 = 1.9 nM 8.72
CHEMBL1744083 IC50 = 4.83 nM 8.32
CHEMBL1744084 IC50 = 8.0 nM 8.10
CHEMBL1744082 IC50 = 24.7 nM 7.61
CHEMBL1744085 IC50 = 64.5 nM 7.19
CHEMBL52498 IC50 = 164.0 nM 6.79
CHEMBL1788318 IC50 = 2200.0 nM 5.66