GFB-12630

GFB-12630 : Inhibitor of CDK5

Structure

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Probe GFB-12630 is in the process of SERP review.

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Information

CDK5

Inhibitor

up to 1 µM

In Vitro Validations

Uniprot ID: Q00535

Target Class: Kinase

Target SubClass: CMGC

Potency: IC50

Potency Value: 3.2 nM

Potency Assay: In vitro kinase assay

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

Target aliases:

Cyclin-dependent kinase 5, PSSALRE, CDKN5, CDK5, C ...

DOI Reference: 10.1021/acs.jmedchem.1c02069

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay, off target (cells): GFB-12630 was tested in NanoBRET assays developed against other CDK family members, confirming the cellular specificity for CDK5. NanoBRET IC50 (nM): CDK5/p35 1.2, CDK1/CycB1 58, CDK6/CycD3 >10000, CDK7/CycH 1332, CDK9/CycT1 1414

Potency assay (off target): GFB-12630 was selective within family against CDK2 (IC50 301 nM), CDK6 (IC50 701 nM), CDK7 (IC50 334 nM) and CDK9 (IC50 523 nM). GFB-12630 was tested for inhibition of a set of 54 kinases representing the diversity of the kinome at a single concentration of 500 nM. No inhibition greater than 50% was observed against any kinase at this concentration.

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(last updated: 4 Jul 2024 )