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Assay Detail

CHEMBL919419

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 CHOD cells
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Potent nonpeptide antagonists of the bradykinin B1 receptor: structure-activity relationship studies with novel diaminochroman carboxamides.
Biswas K, Li A, Chen JJ, D'Amico DC, Fotsch C, Han N, Human J, Liu Q, Norman MH, Riahi B, Yuan C, Suzuki H, Mareska DA, Zhan J, Clarke DE, Toro A, Groneberg RD, Burgess LE, Lester-Zeiner D, Biddlecome G, Manning BH, Arik L, Dong H, Huang M, Kamassah A, Loeloff R, Sun H, Hsieh FY, Kumar G, Ng GY, Hungate RW, Askew BC, Johnson E.
J Med Chem (2007) 50 : 2200 -2212
PubMed 17408249 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 35 7.76 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL227713 1 9.40
CHEMBL415848 1 9.15
CHEMBL412762 1 8.43
CHEMBL425490 1 8.33
CHEMBL389249 1 8.32
CHEMBL390311 1 8.30
CHEMBL227721 1 8.30
CHEMBL227879 1 8.27
CHEMBL227600 1 8.26
CHEMBL390539 1 8.24
CHEMBL389478 1 8.23
CHEMBL227655 1 8.17
CHEMBL227786 1 8.12
CHEMBL227690 1 8.08
CHEMBL224071 1 8.05
CHEMBL227977 1 8.00
CHEMBL390540 1 7.87
CHEMBL227870 1 7.85
CHEMBL227778 1 7.75
CHEMBL387982 1 7.69
CHEMBL268911 1 7.66
CHEMBL413786 1 7.61
CHEMBL388720 1 7.60
CHEMBL2113274 1 7.56
CHEMBL390603 1 7.39
CHEMBL389054 1 7.11
CHEMBL427279 1 7.07
CHEMBL389477 1 6.92
CHEMBL442056 1 6.90
CHEMBL228030 1 6.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL227713 Ki = 0.4 nM 9.40
CHEMBL415848 Ki = 0.7 nM 9.15
CHEMBL412762 Ki = 3.7 nM 8.43
CHEMBL425490 Ki = 4.7 nM 8.33
CHEMBL389249 Ki = 4.8 nM 8.32
CHEMBL390311 Ki = 5.0 nM 8.30
CHEMBL227721 Ki = 5.0 nM 8.30
CHEMBL227879 Ki = 5.4 nM 8.27
CHEMBL227600 Ki = 5.5 nM 8.26
CHEMBL390539 Ki = 5.7 nM 8.24
CHEMBL389478 Ki = 5.9 nM 8.23
CHEMBL227655 Ki = 6.7 nM 8.17
CHEMBL227786 Ki = 7.6 nM 8.12
CHEMBL227690 Ki = 8.3 nM 8.08
CHEMBL224071 Ki = 8.9 nM 8.05
CHEMBL227977 Ki = 10.0 nM 8.00
CHEMBL390540 Ki = 13.4 nM 7.87
CHEMBL227870 Ki = 14.0 nM 7.85
CHEMBL227778 Ki = 17.9 nM 7.75
CHEMBL387982 Ki = 20.6 nM 7.69
CHEMBL268911 Ki = 21.8 nM 7.66
CHEMBL413786 Ki = 24.8 nM 7.61
CHEMBL388720 Ki = 25.2 nM 7.60
CHEMBL2113274 Ki = 27.7 nM 7.56
CHEMBL390603 Ki = 40.6 nM 7.39
CHEMBL389054 Ki = 77.6 nM 7.11
CHEMBL427279 Ki = 84.8 nM 7.07
CHEMBL389477 Ki = 120.0 nM 6.92
CHEMBL442056 Ki = 127.0 nM 6.90
CHEMBL228030 Ki = 132.0 nM 6.88
CHEMBL228014 Ki = 138.0 nM 6.86
CHEMBL227828 Ki = 308.0 nM 6.51
CHEMBL227697 Ki = 367.0 nM 6.43
CHEMBL375709 Ki = 393.0 nM 6.41
CHEMBL228028 Ki > 50000.0 nM -