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SR-4835

SR-4835 : ATP competitive inhibitor of CDK12, CDK13

Structure

Information

  • CDK12
  • CDK13
  • ATP competitive
  • up to 1 uM

In Vitro Validations

Uniprot ID: Q9NYV4
Target Class: Kinase
Target SubClass: CMGC
Potency: Kd
Potency Value: 98 nM
Potency Assay: Binding affinity (DiscoverX)
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Cyclin-dependent kinase 12, KIAA0904, CRKRS, CRK7, ...

DOI Reference: 10.1016/j.ccell.2019.09.004

Uniprot ID: Q9NYV4
Target Class: Kinase
Target SubClass: CMGC
Potency: IC50
Potency Value: 99.0 ± 10.5 nM
Potency Assay: ADP-glo kinase assay
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Cyclin-dependent kinase 12, KIAA0904, CRKRS, CRK7, ...

DOI Reference: 10.1016/j.ccell.2019.09.004

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): SR-4835 was highly selective toward CDK12 and CDK13 when tested in a panel of over 450 kinases at 10 μM. Kinases with weak affinities were further analyzed and only kinase bound were CDK6 (Kd = 5.1 µM), GSK3A (Kd = 1.2 µM) and GSK3B (Kd = 810 nM) had measurable Kd. SR-4835 had no affinity to BRD4 at any of the concentrations tested nor did it inhibit PARP activity.
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SERP ratings and comments

No SERP comments found for SR-4835