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Assay Detail

CHEMBL2019580

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Antagonist activity at rat bradykinin B1 receptor
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

B1 bradykinin receptor (CHEMBL4613)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Quinolinyl- and phenantridinyl-acetamides as bradykinin B1 receptor antagonists.
Eles J, Beke G, Vágó I, Bozó E, Huszár J, Tarcsay A, Kolok S, Schmidt E, Vastag M, Hornok K, Farkas S, Domány G, Keserű GM.
Bioorg Med Chem Lett (2012) 22 : 3095 -3099
PubMed 22483585 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.42 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2018873 1 7.68
CHEMBL2018868 1 7.68
CHEMBL2018867 1 7.55
CHEMBL2018872 1 7.38
CHEMBL2018874 1 7.37
CHEMBL2018871 1 7.35
CHEMBL2018869 1 7.28
CHEMBL2018870 1 7.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2018873 IC50 = 21.0 nM 7.68
CHEMBL2018868 IC50 = 21.0 nM 7.68
CHEMBL2018867 IC50 = 28.0 nM 7.55
CHEMBL2018872 IC50 = 42.0 nM 7.38
CHEMBL2018874 IC50 = 43.0 nM 7.37
CHEMBL2018871 IC50 = 45.0 nM 7.35
CHEMBL2018869 IC50 = 52.0 nM 7.28
CHEMBL2018870 IC50 = 81.0 nM 7.09