Compound name
TPKI-24
Protein family
Protein Kinase
Target name
PLK1
Affinity biochemical (nM)
0.09
Affinity on-target cellular (nM)
13.45
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0001350a
SMILES
COc1cc(C(=O)NC2CCN(C)CC2)ccc1Nc1ncc2c(n1)N(C1CCCC1)CC(F)(F)C(=O)N2C
InChIKey
DJNZZLZKAXGMMC-UHFFFAOYSA-N
NCBI gene ID
5347
UniProt ID
P53350
Mode of action
Inhibitor
Affinity biochemical definition
Kd
Affinity biochemical assay type
Binding assay (Ambit), Binding assay (Ambit)
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/22172702/
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Inhibition of PLK1 activity in NB4 cells
Affinity on-target cellular source knowledge
https://pubmed.ncbi.nlm.nih.gov/22172702/
Affinity on-target cellular relation
=
Selectivity platform
Kinase panel (Ambit)
Selectivity platform number of targets
293
Selectivity remarks
Screened at 1 µM, in-vitro potency of closest targets (binding assay, Ambit): Kd(ALK) = 230 nM, Kd(CAMKK1) = 1100 nM, Kd(CAMKK2) = 87 nM, Kd(DAPK1) = 100 nM, Kd(DAPK3) = 70 nM, Kd(FER) = 53 nM, Kd(GAK) = 87 nM, Kd(MYLK) = 170 nM, Kd(PTK2) = 84 nM, Kd(PTK2B) = 130 nM, Kd(RPS6KA6) = 560 nM, Kd(TTK) = 51 nM, Kd(PLK1) = 0.09 nM, https://pubmed.ncbi.nlm.nih.gov/22172702/;
Selectivity Number of Off-targets
4