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Target Report Card

Target Name and Classification

Target ID CHEMBL3024
Preferred Name Serine/threonine-protein kinase PLK1
Synonyms PLK | PLK-1 | PLK1 | Polo-like kinase 1 | STPK13 | Serine/threonine-protein kinase 13 | Serine/threonine-protein kinase PLK1
Organism Homo sapiens
Species Group No
Protein Target Classification
  • enzyme > kinase > protein kinase > other protein kinase group > other protein kinase plk family

Target Components

Component Description Relationship Accession
Serine/threonine-protein kinase PLK1 SINGLE PROTEIN P53350

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL1233528 VOLASERTIB Serine/threonine-protein kinase PLK1 inhibitor 3 PubMed
CHEMBL513909 BI-2536 Serine/threonine-protein kinase PLK1 inhibitor 2 PubMed PubMed PubMed
CHEMBL1094408 NMS-1286937 Serine/threonine-protein kinase PLK1 inhibitor 1 PubMed PubMed
CHEMBL1908394 GSK-461364 Serine/threonine-protein kinase PLK1 inhibitor 1 PubMed PubMed
CHEMBL2392545 TAK-960 Serine/threonine-protein kinase PLK1 inhibitor 1 PubMed
CHEMBL3545077 MK-1496 Serine/threonine-protein kinase PLK1 inhibitor 1 Other
CHEMBL3545354 Cafusertib Serine/threonine-protein kinase PLK1 inhibitor 1 Other
CHEMBL3545431 HMN-214 Serine/threonine-protein kinase PLK1 inhibitor 1 PubMed PubMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000166851
Ensembl ENSG00000166851
GO Cellular Component GO:0000775 (chromosome, centromeric region)
GO:0000776 (kinetochore)
GO:0000777 (condensed chromosome kinetochore)
GO:0000780 (condensed nuclear chromosome, centromeric region)
GO:0000785 (chromatin)
GO:0000795 (synaptonemal complex)
GO:0000922 (spindle pole)
GO:0000942 (condensed nuclear chromosome outer kinetochore)
GO:0005634 (nucleus)
GO:0005654 (nucleoplasm)
GO:0005694 (chromosome)
GO:0005730 (nucleolus)
GO:0005737 (cytoplasm)
GO:0005813 (centrosome)
GO:0005815 (microtubule organizing center)
GO:0005819 (spindle)
GO:0005829 (cytosol)
GO:0005856 (cytoskeleton)
GO:0005876 (spindle microtubule)
GO:0015630 (microtubule cytoskeleton)
GO:0030496 (midbody)
GO:0051233 (spindle midzone)
GO Molecular Function GO:0000166 (nucleotide binding)
GO:0004672 (protein kinase activity)
GO:0004674 (protein serine/threonine kinase activity)
GO:0005515 (protein binding)
GO:0005524 (ATP binding)
GO:0008017 (microtubule binding)
GO:0010997 (anaphase-promoting complex binding)
GO:0016301 (kinase activity)
GO:0016740 (transferase activity)
GO:0019901 (protein kinase binding)
GO Biological Process GO:0000070 (mitotic sister chromatid segregation)
GO:0000086 (G2/M transition of mitotic cell cycle)
GO:0000122 (negative regulation of transcription from RNA polymerase II promoter)
GO:0000281 (mitotic cytokinesis)
GO:0000910 (cytokinesis)
GO:0001578 (microtubule bundle formation)
GO:0006468 (protein phosphorylation)
GO:0007049 (cell cycle)
GO:0007062 (sister chromatid cohesion)
GO:0007067 (mitotic nuclear division)
GO:0007077 (mitotic nuclear envelope disassembly)
GO:0007094 (mitotic spindle assembly checkpoint)
GO:0007346 (regulation of mitotic cell cycle)
GO:0008283 (cell proliferation)
GO:0010800 (positive regulation of peptidyl-threonine phosphorylation)
GO:0016310 (phosphorylation)
GO:0016321 (female meiosis chromosome segregation)
GO:0016567 (protein ubiquitination)
GO:0018105 (peptidyl-serine phosphorylation)
GO:0030071 (regulation of mitotic metaphase/anaphase transition)
GO:0031145 (anaphase-promoting complex-dependent catabolic process)
GO:0031572 (G2 DNA damage checkpoint)
GO:0031648 (protein destabilization)
GO:0032436 (positive regulation of proteasomal ubiquitin-dependent protein catabolic process)
GO:0042787 (protein ubiquitination involved in ubiquitin-dependent protein catabolic process)
GO:0043066 (negative regulation of apoptotic process)
GO:0043393 (regulation of protein binding)
GO:0045143 (homologous chromosome segregation)
GO:0045184 (establishment of protein localization)
GO:0045736 (negative regulation of cyclin-dependent protein serine/threonine kinase activity)
GO:0045862 (positive regulation of proteolysis)
GO:0051297 (centrosome organization)
GO:0051301 (cell division)
GO:0051437 (positive regulation of ubiquitin-protein ligase activity involved in regulation of mitotic cell cycle transition)
GO:0051439 (regulation of ubiquitin-protein ligase activity involved in mitotic cell cycle)
GO:0051443 (positive regulation of ubiquitin-protein transferase activity)
GO:0051726 (regulation of cell cycle)
GO:0070194 (synaptonemal complex disassembly)
GO:0071168 (protein localization to chromatin)
GO:1900182 (positive regulation of protein localization to nucleus)
GO:1901673 (regulation of mitotic spindle assembly)
GO:1902749 (regulation of cell cycle G2/M phase transition)
GO:1904668 (positive regulation of ubiquitin protein ligase activity)
Wikipedia PLK1

Target Cross References - Protein

canSAR P53350
Human Protein Atlas ENSG00000166851
IntAct P53350
Guide to Pharmacology 2168
Open Targets ENSG00000166851
PharmGKB PA33410
Pharos P53350 (Tchem)
Reactome R-HSA-156711 (Polo-like kinase mediated events.)
R-HSA-162658 (Golgi Cisternae Pericentriolar Stack Reorganization.)
R-HSA-174178 (APC/C:Cdh1 mediated degradation of Cdc20 and other APC/C:Cdh1 targeted proteins in late mitosis/early G1.)
R-HSA-176412 (Phosphorylation of the APC/C.)
R-HSA-176417 (Phosphorylation of Emi1.)
R-HSA-2299718 (Condensation of Prophase Chromosomes.)
R-HSA-2467813 (Separation of Sister Chromatids.)
R-HSA-2500257 (Resolution of Sister Chromatid Cohesion.)
R-HSA-2565942 (Regulation of PLK1 Activity at G2/M Transition.)
R-HSA-2980767 (Activation of NIMA Kinases NEK9, NEK6, NEK7.)
R-HSA-380259 (Loss of Nlp from mitotic centrosomes.)
R-HSA-380270 (Recruitment of mitotic centrosome proteins and complexes.)
R-HSA-380284 (Loss of proteins required for interphase microtubule organization from the centrosome.)
R-HSA-5620912 (Anchoring of the basal body to the plasma membrane.)
R-HSA-5663220 (RHO GTPases Activate Formins.)
R-HSA-68877 (Mitotic Prometaphase.)
R-HSA-68881 (Mitotic Metaphase/Anaphase Transition.)
R-HSA-68884 (Mitotic Telophase/Cytokinesis.)
R-HSA-69273 (Cyclin A/B1 associated events during G2/M transition.)
R-HSA-8852276 (The role of GTSE1 in G2/M progression after G2 checkpoint.)
R-HSA-8854518 (AURKA Activation by TPX2.)
UniProt P53350 Q15153 Q99746

Target Cross References - Domain

InterPro IPR000719 (Prot_kinase_dom.)
IPR000959 (POLO_box_dom.)
IPR008271 (Ser/Thr_kinase_AS.)
IPR011009 (Kinase-like_dom.)
IPR017441 (Protein_kinase_ATP_BS.)
IPR033695 (POLO_box_2.)
IPR033701 (POLO_box_1.)
IPR033702 (PLK1_cat.)
Pfam PF00069 (Pkinase)
PF00659 (POLO_box)

Target Cross References - Structure

PDBe 1Q4K 1Q4O 1UMW 2OGQ 2OJX 2OU7 2OWB 2RKU 2V5Q 2YAC 3BZI 3C5L 3FC2 3FVH 3HIH 3HIK 3KB7 3P2W 3P2Z 3P34 3P35 3P36 3P37 3Q1I More...
CREDO 1Q4K 1Q4O 1UMW 2OGQ 2OJX 2OU7 2OWB 2RKU 2V5Q 2YAC 3BZI 3C5L 3FC2 3FVH 3HIH 3HIK 3KB7 3P2W 3P2Z 3P34 3P35 3P36 3P37 3Q1I More...