Compound name
FMF-04-159-2
Protein family
Protein Kinase
Target name
CDK16
Affinity biochemical (nM)
10.1
Affinity on-target cellular (nM)
803
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000057b
SMILES
CN(C)C/C=C/C(=O)Nc1cccc(S(=O)(=O)N2CCC(NC(=O)c3n[nH]cc3NC(=O)c3c(Cl)cc(Cl)cc3Cl)CC2)c1
InChIKey
HZPYSAHDRSBARR-QPJJXVBHSA-N
NCBI gene ID
5127
UniProt ID
Q00536
Synonyms
PCTAIRE, PCTAIRE1, PCTGAIRE, FLJ16665
Mode of action
Covalent inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
LanthaScreen Eu kinase binding assays (CDK16/CycY)
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/30930164/
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
NanoBRET assay (using CDK16/cylinY, HCT116 cells)
Affinity on-target cellular source knowledge
https://pubmed.ncbi.nlm.nih.gov/30930164/
Affinity on-target cellular relation
=
Selectivity platform
KiNativ profiling (using HCT116 cells)
Selectivity platform number of targets
289
Selectivity remarks
Screened at 1 µM, 4h incubation, closest target as % of inhibition: CDK17 (94.2%), CDK18 (8.%), full screening data are available as supporting info,https://pubmed.ncbi.nlm.nih.gov/30930164/;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/30930164/
Selectivity Number of Off-targets
1