Compound name
THZ531
Protein family
Protein Kinase
Target name
CDK13
Affinity biochemical (nM)
69
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000090b
SMILES
CN(C)C/C=C/C(=O)Nc1ccc(C(=O)N2CCCC(Nc3ncc(Cl)c(-c4c[nH]c5ccccc45)n3)C2)cc1
InChIKey
RUBYHLPRZRMTJO-UXBLZVDNSA-N
NCBI gene ID
8621
UniProt ID
Q14004
Synonyms
CHED, CDC2L, KIAA1791
Mode of action
Covalent inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Radiometric kinase assay
Affinity Biochemical Source Knowledge
https://www.nature.com/articles/nchembio.2166
Affinity biochemical relation
=
Selectivity platform
Ambit KINOMEscanand KiNATiv profiling in Jurkat cells
Selectivity platform number of targets
211
Selectivity remarks
Screened at 1 µM, closest targets AURKA (54%), PLK(53%), CLK1(43%), all IC50 >3.5 µM, In-vitro potency of closest target (Radiometric kinase assay ): Kd(CDK12) = 158 nM, https://www.nature.com/articles/nchembio.2166;
Selectivity Source Knowledge
https://www.nature.com/articles/nchembio.2166