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Assay Detail

CHEMBL652643

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Binding
Ability to bind to human cloned B2 receptor in competition binding experiments with [3H]- bradykinin
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Synthesis and biological evaluation of bradykinin B(1)/B(2) and selective B(1) receptor antagonists.
Amblard M, Bedos P, Olivier C, Daffix I, Luccarini JM, Dodey P, Pruneau D, Paquet JL, Martinez J.
J Med Chem (2000) 43 : 2382 -2386
PubMed 10882364 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 8.51 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3142396 1 10.10
CHEMBL406291 BRADYKININ 2.0 1 9.96
CHEMBL412824 1 9.40
CHEMBL408846 1 8.36
CHEMBL3085458 1 8.04
CHEMBL3142391 1 7.21
CHEMBL216618 1 6.49
CHEMBL80472 1 -
CHEMBL2369827 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3142396 Ki = 0.08 nM 10.10
CHEMBL406291 BRADYKININ Ki = 0.11 nM 9.96
CHEMBL412824 Ki = 0.4 nM 9.40
CHEMBL408846 Ki = 4.4 nM 8.36
CHEMBL3085458 Ki = 9.2 nM 8.04
CHEMBL3142391 Ki = 62.0 nM 7.21
CHEMBL216618 Ki = 325.0 nM 6.49
CHEMBL80472 Ki > 10.0 nM -
CHEMBL2369827 Ki > 10.0 nM -