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GFB-12811

GFB-12811 : Inhibitor of CDK5

Structure

Information

  • CDK5
  • Inhibitor
  • 1 µM

In Vitro Validations

Uniprot ID: Q00535
Target Class: Kinase
Target SubClass: CMGC
Potency: IC50
Potency Value: 2.3 nM
Potency Assay: In Vitro Kinase Assays (mobility shift 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

Uniprot ID: Q00535
Target Class: Kinase
Target SubClass: CMGC
Potency: Ki
Potency Value: 1 nM
Potency Assay: Calculated Ki
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): Selective against CDK2 (92x), CDK6 (1390x), CDK7 (312x), CDK9 (389x) Screened in a set of 54 kinases representing the diversity of the kinome at 500 nM: no inhibition greater than 50% was observed against any kinase at this concentration..
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SERP ratings and comments

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

GFB-12811 was not tested in a cellular target engagement assay but based on the NanoBRET IC50 of a related compound GFB-12630 of 1.2 nM against CDK5/p35 and 58 nM against CDK1/CycB1, using a concentration of around 100 would be more appropriate to get the required selectivity in cells. However, this should be confirmed with the GFB-12811 molecule itself.

(last updated: 26 Jun 2024 )

SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 10 Aug 2024 )