BI-9627

BI-9627 : Antagonist of SLC9A1

Structure

Information

  • SLC9A1
  • Antagonist

In Vitro Validations

Uniprot ID: P19634
Target Class: Transporter
Target SubClass: Solute Carrier
Potency: IC50
Potency Value: 6 nM
Potency Assay: pHi change assay: SLC9A1
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Sodium/hydrogen exchanger 1, NHE1, APNH1, SLC9A1, ...

DOI Reference: 10.1021/jm300601d

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:
Solute carrier family 9 isoform selectivity: > 30-fold selective versus SLC9A2 (IC50 = 231 nM) and > 1000-fold versus SLC9A3 (IC50 > 16 µM). Eurofins-Panlabs screen on 68 targets @ 10 µM did not give strong hits. Clean GPCR scan with the closest hit on SLC6A3 (pKi = 5.8).
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SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 1 Feb 2022 )

SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 9 Feb 2022 )