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Assay Detail

CHEMBL855157

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

Binding
Displacement of [3H]DAK from human bradykinin B1 receptor expressed in CHO-D cells
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Identification of a nonpeptidic and conformationally restricted bradykinin B1 receptor antagonist with anti-inflammatory activity.
D'Amico DC, Aya T, Human J, Fotsch C, Chen JJ, Biswas K, Riahi B, Norman MH, Willoughby CA, Hungate R, Reider PJ, Biddlecome G, Lester-Zeiner D, Staden CV, Johnson E, Kamassah A, Arik L, Wang J, Viswanadhan VN, Groneberg RD, Zhan J, Suzuki H, Toro A, Mareska DA, Clarke DE, Harvey DM, Burgess LE, Laird ER, Askew B, Ng G.
J Med Chem (2007) 50 : 607 -610
PubMed 17243660 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.76 9.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL218152 1 9.62
CHEMBL415848 1 9.11
CHEMBL373654 1 8.89
CHEMBL441188 1 8.80
CHEMBL412552 1 7.80
CHEMBL221925 1 7.77
CHEMBL385740 1 7.77
CHEMBL415629 1 7.51
CHEMBL426165 1 6.88
CHEMBL415849 1 6.84
CHEMBL221691 1 6.42
CHEMBL385741 1 5.72
CHEMBL414091 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL218152 Ki = 0.24 nM 9.62
CHEMBL415848 Ki = 0.77 nM 9.11
CHEMBL373654 Ki = 1.3 nM 8.89
CHEMBL441188 Ki = 1.6 nM 8.80
CHEMBL412552 Ki = 15.8 nM 7.80
CHEMBL221925 Ki = 17.0 nM 7.77
CHEMBL385740 Ki = 17.0 nM 7.77
CHEMBL415629 Ki = 31.0 nM 7.51
CHEMBL426165 Ki = 132.0 nM 6.88
CHEMBL415849 Ki = 143.0 nM 6.84
CHEMBL221691 Ki = 382.0 nM 6.42
CHEMBL385741 Ki = 1900.0 nM 5.72
CHEMBL414091 Ki = 241327.0 nM -