BMS-820132

BMS-820132 : Partial Activator of GCK

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

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Probe BMS-820132 is in the process of SERP review.

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Information

Partial Activator

1 µM
Reviewer recommended concentration: Based on the reported chronic experiment, repeated dosing of 30 mg/kg daily was safe and efficacious in mouse and would be the in vivo dose I'd recommend in mouse.

Probe Availability:

MedChemExpress

In Vitro Validations

Uniprot ID: P35557

Target Class: Kinase

Target SubClass: Hexokinase

Potency: Activity

Potency Value: 29 nM; max activation 143%

Potency Assay: Enzymatic GK activation assay using purified recombinant human islet GK

PDB ID for probe-target interaction (3D structure): 7T79

Target aliases:

Hexokinase-4, GCK, HXK4_HUMAN, HK IV, HK4, Hexokin ...

DOI Reference: 10.1021/acs.jmedchem.1c02110

In Cell Validations

No in Cell Validations available

In Vivo Data

I have extra information to add

SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

Activity in biochemical assay but no cellular data was reported for the compound. It should be mentioned that While the PK data are reported for mouse, rat, dog and cyno, the biochemical activity was reported only for human and mouse GK.

(last updated: 22 Dec 2022 )