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Assay Detail

CHEMBL652637

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

Binding
Binding affinity against human cloned Bradykinin receptor B2 expressed in CHO cells using [3H]-bradykinin as radioligand
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

B2 bradykinin receptor (CHEMBL3157)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of potent bradykinin agonists containing a benzothiazepine moiety.
Amblard M, Daffix I, Bedos P, Bergé G, Pruneau D, Paquet JL, Luccarini JM, Bélichard P, Dodey P, Martinez J.
J Med Chem (1999) 42 : 4185 -4192
PubMed 10514288 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 8.49 10.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2028850 ICATIBANT 4.0 1 10.19
CHEMBL406291 BRADYKININ 2.0 1 9.19
CHEMBL2112698 1 9.15
CHEMBL413386 1 7.89
CHEMBL2105864 LABRADIMIL 2.0 1 7.72
CHEMBL2111889 1 6.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2028850 ICATIBANT Ki = 0.064 nM 10.19
CHEMBL406291 BRADYKININ Ki = 0.65 nM 9.19
CHEMBL2112698 Ki = 0.7 nM 9.15
CHEMBL413386 Ki = 13.0 nM 7.89
CHEMBL2105864 LABRADIMIL Ki = 19.0 nM 7.72
CHEMBL2111889 Ki = 162.0 nM 6.79