BI-113823

BI-113823 : Antagonist of BDKRB1

Structure

Information

  • BDKRB1
  • Antagonist
  • 100 nM

In Vitro Validations

Uniprot ID: P46663
Target Class: GPCR
Target SubClass: BK-1
Potency: Ki
Potency Value: 5.3 nM
Potency Assay: Radioligand binding assay (displacement of kallidin) at 10 µM
PDB ID for probe-target interaction (3D structure): --
Target aliases:
B1 bradykinin receptor, BRADYB1, BDKRB1, BKRB1_HUM ...

DOI Reference: 10.1371/journal.pone.0051151

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Selectivity within target family: Radioligand binding assay at 10 µM: hBDKRB2 Ki > 10 µM Selectivity outside target family: Eurofins SafteyScreen (69 targets) at 10 µM: Closest off-targets are SIGMAR1 (70 % inh.), TMEM97 (55 % inh.)
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