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Assay Detail

CHEMBL652384

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Functional
In vitro Bradykinin receptor B2 antagonist activity by using rat uterus functional assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Uterus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

B2 bradykinin receptor (CHEMBL2501)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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
Kd 15 7.90 9.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2028850 ICATIBANT 4.0 1 9.50
CHEMBL3038099 1 9.31
CHEMBL3038100 1 9.09
CHEMBL3038095 1 8.88
CHEMBL2372283 1 8.79
CHEMBL3038094 1 8.50
CHEMBL3038106 1 8.48
CHEMBL3038096 1 7.73
CHEMBL3038101 1 7.68
CHEMBL2372278 1 7.65
CHEMBL3038102 1 7.30
CHEMBL2372276 1 7.29
CHEMBL3038104 1 6.76
CHEMBL3038103 1 5.85
CHEMBL3038105 1 5.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2028850 ICATIBANT Kd = 0.3162 nM 9.50
CHEMBL3038099 Kd = 0.4898 nM 9.31
CHEMBL3038100 Kd = 0.8128 nM 9.09
CHEMBL3038095 Kd = 1.318 nM 8.88
CHEMBL2372283 Kd = 1.622 nM 8.79
CHEMBL3038094 Kd = 3.162 nM 8.50
CHEMBL3038106 Kd = 3.311 nM 8.48
CHEMBL3038096 Kd = 18.62 nM 7.73
CHEMBL3038101 Kd = 20.89 nM 7.68
CHEMBL2372278 Kd = 22.39 nM 7.65
CHEMBL3038102 Kd = 50.12 nM 7.30
CHEMBL2372276 Kd = 51.29 nM 7.29
CHEMBL3038104 Kd = 173.78 nM 6.76
CHEMBL3038103 Kd = 1412.54 nM 5.85
CHEMBL3038105 Kd = 2137.96 nM 5.67