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Assay Detail

CHEMBL772609

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

Functional
In vitro antagonistic activity against kinin-induced rabbit jugular vein contraction.
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Confidence 9 — Direct single protein target
Curated By Expert

Target

B2 bradykinin receptor (CHEMBL3453)
Type SINGLE PROTEIN
Organism Oryctolagus cuniculus

Publication

Design and synthesis of new linear and cyclic bradykinin antagonists.
Thurieau C, Félétou M, Hennig P, Raimbaud E, Canet E, Fauchère JL.
J Med Chem (1996) 39 : 2095 -2101
PubMed 8642569 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 23 6.47 7.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2028838 1 7.39
CHEMBL2028849 1 7.34
CHEMBL2028845 1 7.20
CHEMBL2028848 1 7.12
CHEMBL2028837 1 7.12
CHEMBL2028840 1 6.93
CHEMBL2028835 1 6.84
CHEMBL2028836 1 6.66
CHEMBL2028841 1 6.62
CHEMBL3142191 1 6.60
CHEMBL2028844 1 6.51
CHEMBL2028839 1 6.49
CHEMBL3142190 1 6.44
CHEMBL2028847 1 6.36
CHEMBL3142192 1 6.33
CHEMBL2028843 1 6.31
CHEMBL2028846 1 6.27
CHEMBL2369364 1 6.10
CHEMBL2369400 1 6.07
CHEMBL2369392 1 6.04
CHEMBL3142173 1 5.52
CHEMBL3142174 1 5.47
CHEMBL2372276 1 5.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2028838 Kd = 40.74 nM 7.39
CHEMBL2028849 Kd = 45.71 nM 7.34
CHEMBL2028845 Kd = 63.1 nM 7.20
CHEMBL2028848 Kd = 75.86 nM 7.12
CHEMBL2028837 Kd = 75.86 nM 7.12
CHEMBL2028840 Kd = 117.49 nM 6.93
CHEMBL2028835 Kd = 144.54 nM 6.84
CHEMBL2028836 Kd = 218.78 nM 6.66
CHEMBL2028841 Kd = 239.88 nM 6.62
CHEMBL3142191 Kd = 251.19 nM 6.60
CHEMBL2028844 Kd = 309.03 nM 6.51
CHEMBL2028839 Kd = 323.59 nM 6.49
CHEMBL3142190 Kd = 363.08 nM 6.44
CHEMBL2028847 Kd = 436.52 nM 6.36
CHEMBL3142192 Kd = 467.74 nM 6.33
CHEMBL2028843 Kd = 489.78 nM 6.31
CHEMBL2028846 Kd = 537.03 nM 6.27
CHEMBL2369364 Kd = 794.33 nM 6.10
CHEMBL2369400 Kd = 851.14 nM 6.07
CHEMBL2369392 Kd = 912.01 nM 6.04
CHEMBL3142173 Kd = 3019.95 nM 5.52
CHEMBL3142174 Kd = 3388.44 nM 5.47
CHEMBL2372276 Kd = 7413.1 nM 5.13