BI-9787

BI-9787 : Inhibitor of KHK

Structure

SERP Rating

Probe BI-9787 is in the process of SERP review.

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Information

Inhibitor

up to 1 uM

Probe Availability:

MedChemExpress

In Vitro Validations

Uniprot ID: P50053

Target Class: Kinase

Target SubClass: Carbohydrate kinase

Potency: IC50

Potency Value: 12.8 nM

Potency Assay: Kinase activity of recombinant His-tagged KHK isoforms.

PDB ID for probe-target interaction (3D structure): 9FHD

Target aliases:

Ketohexokinase, KHK, KHK_HUMAN, Hepatic fructokina ...

DOI Reference: 10.1016/j.bmcl.2024.129930

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): BI-9787 was tested on 44 targets in a selectivity panel and showed ≥100 fold selectivity for 43 targets. Against PDE4D2, it still maintains an estimated selectivity factor of at least 30-fold (81% inhibition at 10 μM). The comparably selective negative control BI-2817 showed in only 3 out of 44 targets inhibition with more than 50% at 10 μM.

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SERP ratings and comments

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