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Assay Detail

CHEMBL1837510

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Functional
Inhibition of rabbit B1 receptor by cellular calcium flux assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

B1 bradykinin receptor (CHEMBL4087)
Type SINGLE PROTEIN
Organism Oryctolagus cuniculus

Publication

Discovery of potent, orally bioavailable phthalazinone bradykinin B1 receptor antagonists.
Biswas K, Peterkin TA, Bryan MC, Arik L, Lehto SG, Sun H, Hsieh FY, Xu C, Fremeau RT, Allen JR.
J Med Chem (2011) 54 : 7232 -7246
PubMed 21902230 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 8.07 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1834752 1 9.22
CHEMBL1834619 1 8.96
CHEMBL1834751 1 8.66
CHEMBL1777958 1 8.39
CHEMBL455642 1 7.95
CHEMBL1834750 1 7.76
CHEMBL1834616 1 7.67
CHEMBL1834620 1 7.51
CHEMBL1834749 1 6.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1834752 IC50 = 0.6 nM 9.22
CHEMBL1834619 IC50 = 1.1 nM 8.96
CHEMBL1834751 IC50 = 2.2 nM 8.66
CHEMBL1777958 IC50 = 4.1 nM 8.39
CHEMBL455642 IC50 = 11.2 nM 7.95
CHEMBL1834750 IC50 = 17.5 nM 7.76
CHEMBL1834616 IC50 = 21.4 nM 7.67
CHEMBL1834620 IC50 = 31.1 nM 7.51
CHEMBL1834749 IC50 = 342.3 nM 6.47