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Assay Detail

CHEMBL919420

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

Functional
Antagonist activity at human bradykinin B1 receptor expressed in CHOD cells assessed as effect on DAK-induced calcium flux
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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
IC50 35 7.24 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL227713 1 9.10
CHEMBL415848 1 8.47
CHEMBL227655 1 8.03
CHEMBL390311 1 8.02
CHEMBL389249 1 8.00
CHEMBL227721 1 7.98
CHEMBL412762 1 7.96
CHEMBL390539 1 7.83
CHEMBL389478 1 7.83
CHEMBL227879 1 7.77
CHEMBL227870 1 7.76
CHEMBL227600 1 7.71
CHEMBL425490 1 7.70
CHEMBL227786 1 7.61
CHEMBL227690 1 7.34
CHEMBL227977 1 7.33
CHEMBL224071 1 7.22
CHEMBL413786 1 7.21
CHEMBL268911 1 7.16
CHEMBL227778 1 7.11
CHEMBL390540 1 7.02
CHEMBL2113274 1 6.95
CHEMBL387982 1 6.90
CHEMBL427279 1 6.78
CHEMBL388720 1 6.69
CHEMBL390603 1 6.68
CHEMBL228014 1 6.67
CHEMBL442056 1 6.59
CHEMBL389054 1 6.48
CHEMBL227828 1 6.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL227713 IC50 = 0.8 nM 9.10
CHEMBL415848 IC50 = 3.4 nM 8.47
CHEMBL227655 IC50 = 9.4 nM 8.03
CHEMBL390311 IC50 = 9.6 nM 8.02
CHEMBL389249 IC50 = 9.9 nM 8.00
CHEMBL227721 IC50 = 10.5 nM 7.98
CHEMBL412762 IC50 = 10.9 nM 7.96
CHEMBL390539 IC50 = 14.8 nM 7.83
CHEMBL389478 IC50 = 14.8 nM 7.83
CHEMBL227879 IC50 = 17.0 nM 7.77
CHEMBL227870 IC50 = 17.4 nM 7.76
CHEMBL227600 IC50 = 19.7 nM 7.71
CHEMBL425490 IC50 = 20.1 nM 7.70
CHEMBL227786 IC50 = 24.3 nM 7.61
CHEMBL227690 IC50 = 45.9 nM 7.34
CHEMBL227977 IC50 = 46.2 nM 7.33
CHEMBL224071 IC50 = 60.2 nM 7.22
CHEMBL413786 IC50 = 60.9 nM 7.21
CHEMBL268911 IC50 = 69.9 nM 7.16
CHEMBL227778 IC50 = 78.4 nM 7.11
CHEMBL390540 IC50 = 96.3 nM 7.02
CHEMBL2113274 IC50 = 113.0 nM 6.95
CHEMBL387982 IC50 = 127.0 nM 6.90
CHEMBL427279 IC50 = 167.0 nM 6.78
CHEMBL388720 IC50 = 203.0 nM 6.69
CHEMBL390603 IC50 = 207.0 nM 6.68
CHEMBL228014 IC50 = 212.0 nM 6.67
CHEMBL442056 IC50 = 255.0 nM 6.59
CHEMBL389054 IC50 = 330.0 nM 6.48
CHEMBL227828 IC50 = 352.0 nM 6.45
CHEMBL389477 IC50 = 566.2 nM 6.25
CHEMBL228030 IC50 = 580.0 nM 6.24
CHEMBL227697 IC50 = 2000.0 nM 5.70
CHEMBL375709 IC50 = 2030.0 nM 5.69
CHEMBL228028 IC50 > 4000.0 nM -