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Assay Detail

CHEMBL656787

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Functional
In vitro Bradykinin receptor B1 antagonist activity in functional tissue within rabbit aorta
12
Total Activities
12
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Tissue Aorta
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Bradykinin receptor antagonists containing N-substituted amino acids: in vitro and in vivo B(2) and B(1) receptor antagonist activity.
Goodfellow VS, Marathe MV, Kuhlman KG, Fitzpatrick TD, Cuadrado D, Hanson W, Zuzack JS, Ross SE, Wieczorek M, Burkard M, Whalley ET.
J Med Chem (1996) 39 : 1472 -1484
PubMed 8691478 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.77 6.41
-Log IC50 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3038105 1 6.41
CHEMBL3038104 1 5.79
CHEMBL3038096 1 5.52
CHEMBL3038103 1 5.34
CHEMBL3038099 1 -
CHEMBL2028982 1 -
CHEMBL3038095 1 -
CHEMBL3038102 1 -
CHEMBL3038098 1 -
CHEMBL3038097 1 -
CHEMBL3038094 1 -
CHEMBL2028850 ICATIBANT 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3038105 IC50 = 389.05 nM 6.41
CHEMBL3038104 IC50 = 1621.81 nM 5.79
CHEMBL3038096 IC50 = 3019.95 nM 5.52
CHEMBL3038103 IC50 = 4570.88 nM 5.34
CHEMBL3038099 IC50 > 10000.0 nM -
CHEMBL2028982 IC50 > 10000.0 nM -
CHEMBL3038095 -Log IC50 - -
CHEMBL3038102 IC50 > 10000.0 nM -
CHEMBL3038098 IC50 > 10000.0 nM -
CHEMBL3038097 IC50 > 10000.0 nM -
CHEMBL3038094 IC50 > 10000.0 nM -
CHEMBL2028850 ICATIBANT -Log IC50 - -