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Potency data for probe BI-113823 and control BI-5832


In vitro potency


Target name Target information Species Assay description Compound conc. Probe result (SD) Control result (SD) Publication of assay conditions
BDKRB1 Membranes of CHO-K1 cells expressing human recombinant B1R Homo sapiens Radioligand binding assay (displacement of kallidin, hBDKRB1 ) : Non-specific binding is estimated in the presence of 10 µM Des-Arg9- (Leu8)-Bradykinin. Membranes are filtered and washed, the filters are then counted to determine [3H]Kallidin[des-Arg10, Leu9] specifically bound. 10 µM Ki = 5.300 nM Ki = 431 nM DOI: 10.1111/j.1533-2500.2011.00528.x
BDKRB1 Rattus norvegicus Radioligand binding assay (displacement of kallidin, rat BDKRB1 ) : Non-specific binding is estimated in the presence of 10 µM Des-Arg9- (Leu8)-Bradykinin. Membranes are filtered and washed, the filters are then counted to determine [3H]Kallidin[des-Arg10, Leu9] specifically bound. 10 µM Ki = 13.300 nM DOI: 10.1111/j.1533-2500.2011.00528.x
BDKRB1 Oryctolagus cuniculus Radioligand binding assay (displacement of kallidin, rabbit BDKRB1 ) : Non-specific binding is estimated in the presence of 10 µM Des-Arg9- (Leu8)-Bradykinin. Membranes are filtered and washed, the filters are then counted to determine [3H]Kallidin[des-Arg10, Leu9] specifically bound. 10 µM Ki = 15.300 nM DOI: 10.1111/j.1533-2500.2011.00528.x
BDKRB2 Homo sapiens Radioligand binding assay (displacement of kallidin, human BDKRB2 ) : Non-specific binding is estimated in the presence of 10 µM Des-Arg9- (Leu8)-Bradykinin. Membranes are filtered and washed, the filters are then counted to determine [3H]Kallidin[des-Arg10, Leu9] specifically bound. 10 µM Ki > 10 µM DOI: 10.1111/j.1533-2500.2011.00528.x

In cell potency


Target name Target information Species Assay description Compound conc. Probe result (SD) Control result (SD) Publication of assay conditions
BDKRB1 HEK-cells expressing hBDKRB1 Homo sapiens Measurement of intracellular calcium in HEK-cells expressing hBDKRB1: The compound antagonizes the effects of the specific B1 agonist [Lys-des-Arg9 ]-Bradykinin (10 nM) in a concentration-dependent manner. up to 1 µM IC50 = 7 nM IC50 = 699 nM