BI-5121

BI-5121 : Antagonist of HCRTR1

Structure

SERP Rating

Probe BI-5121 is in the process of SERP review.

Please continue to check back for new reviews and commentary.

Information

HCRTR1

Antagonist

up to 100 nM

Additional Data

SGC image SGC Chemical Probe Collection

In Vitro Validations

Uniprot ID: O43613

Target Class: GPCR

Target SubClass: Orexin/Hypocretin receptor

Potency: IC50

Potency Value: <3 nM

Potency Assay: Eurofins radio-displacement assay

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Orexin/Hypocretin receptor type 1, HCRTR1, OX1R_HU ...

Other Reference: peer reviewed at SGC

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Eurofins radio-displacement assay (HCRTR2 binding): IC50 = 140 nM (> 40 fold selectivity), OX2 (HCRTR2) ANTA IP1: IC50 = 62.6 nM (> 39 fold selectivity). GPCR screen (44 targets): clean (OPRK1: IC50 = 730 nM (> 200 fold selectivity)).

Potency assay (off target): Eurofins SafteyScreen (47 targets) at 10 µM: BI-5121 was tested against 47 class A GPCRs in a selectivity panel and showed an excellent selectivity for all off-targets (≤ 50% inhibition @ 10 µM with the exception of KAPPAR, 55% Inhib). With an IC50 of 730 nM, BI-5121 shows >200-fold selectivity against KAPPAR.

Potency assay (off target): BI-5121 shows a >40-fold selectivity in a binding assay and 39-fold selectivity in a functional, cellular assay against OX2R

I have extra information to add

SERP ratings and comments

No SERP comments found for BI-5121