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ChEMBL Statistics
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Target Report Card

Target Name and Classification

Target ID CHEMBL1806
Target Type SINGLE PROTEIN
Preferred Name DNA topoisomerase II alpha
Synonyms DNA topoisomerase 2-alpha | DNA topoisomerase II, alpha isozyme | TOP2 | TOP2A
Organism Homo sapiens
Species Group No
Protein Target Classification
  • enzyme > isomerase

Target Components

Component Description Relationship Accession
DNA topoisomerase 2-alpha SINGLE PROTEIN P11388

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL2094255 DNA topoisomerase II PROTEIN FAMILY

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL178 DAUNORUBICIN DNA topoisomerase II alpha inhibitor 4 DailyMed DailyMed
CHEMBL1563 DAUNORUBICIN HYDROCHLORIDE DNA topoisomerase II alpha inhibitor 4 DailyMed DailyMed
CHEMBL359744 DOXORUBICIN HYDROCHLORIDE DNA topoisomerase II alpha inhibitor 4 FDA
CHEMBL1096885 VALRUBICIN DNA topoisomerase II alpha inhibitor 4 DailyMed
CHEMBL1200475 DAUNORUBICIN CITRATE DNA topoisomerase II alpha inhibitor 4 DailyMed DailyMed
CHEMBL1200645 ETOPOSIDE PHOSPHATE DNA topoisomerase II alpha inhibitor 4 DailyMed
CHEMBL1200976 IDARUBICIN HYDROCHLORIDE DNA topoisomerase II alpha inhibitor 4 DailyMed
CHEMBL1417019 MITOXANTRONE HYDROCHLORIDE DNA topoisomerase II alpha inhibitor 4 DailyMed
CHEMBL481958 AMRUBICIN HYDROCHLORIDE DNA topoisomerase II alpha inhibitor 3 PubMed
CHEMBL1186894 AMRUBICIN DNA topoisomerase II alpha inhibitor 3 PubMed
CHEMBL2107818 ALDOXORUBICIN DNA topoisomerase II alpha inhibitor 3 PubMed
CHEMBL3833344 MM-302 DNA topoisomerase II alpha inhibitor 2 PubMed PubMed PubMed
More...

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000131747
Ensembl ENSG00000131747
GO Cellular Component GO:0000228 (nuclear chromosome)
GO:0000793 (condensed chromosome)
GO:0005634 (nucleus)
GO:0005654 (nucleoplasm)
GO:0005730 (nucleolus)
GO:0005737 (cytoplasm)
GO:0005814 (centriole)
GO:0009330 (DNA topoisomerase complex (ATP-hydrolyzing))
GO:0019035 (viral integration complex)
GO:0032991 (macromolecular complex)
GO:1990904 (ribonucleoprotein complex)
GO Molecular Function GO:0000166 (nucleotide binding)
GO:0000287 (magnesium ion binding)
GO:0003677 (DNA binding)
GO:0003682 (chromatin binding)
GO:0003723 (RNA binding)
GO:0003916 (DNA topoisomerase activity)
GO:0003918 (DNA topoisomerase type II (ATP-hydrolyzing) activity)
GO:0005080 (protein kinase C binding)
GO:0005515 (protein binding)
GO:0005524 (ATP binding)
GO:0008022 (protein C-terminus binding)
GO:0008094 (DNA-dependent ATPase activity)
GO:0008144 (drug binding)
GO:0008301 (DNA binding, bending)
GO:0016853 (isomerase activity)
GO:0019899 (enzyme binding)
GO:0042803 (protein homodimerization activity)
GO:0042826 (histone deacetylase binding)
GO:0043130 (ubiquitin binding)
GO:0046872 (metal ion binding)
GO:0046982 (protein heterodimerization activity)
GO:0061505 (DNA topoisomerase II activity)
GO Biological Process GO:0000712 (resolution of meiotic recombination intermediates)
GO:0000819 (sister chromatid segregation)
GO:0002244 (hematopoietic progenitor cell differentiation)
GO:0006259 (DNA metabolic process)
GO:0006265 (DNA topological change)
GO:0006266 (DNA ligation)
GO:0006974 (cellular response to DNA damage stimulus)
GO:0007059 (chromosome segregation)
GO:0016925 (protein sumoylation)
GO:0030261 (chromosome condensation)
GO:0030263 (apoptotic chromosome condensation)
GO:0040016 (embryonic cleavage)
GO:0042752 (regulation of circadian rhythm)
GO:0043065 (positive regulation of apoptotic process)
GO:0044774 (mitotic DNA integrity checkpoint)
GO:0045070 (positive regulation of viral genome replication)
GO:0045870 (positive regulation of single stranded viral RNA replication via double stranded DNA intermediate)
GO:0045944 (positive regulation of transcription from RNA polymerase II promoter)
GO:0048511 (rhythmic process)
GO:1905463 (negative regulation of DNA duplex unwinding)
Wikipedia TOP2A

Target Cross References - Protein

canSAR P11388
Human Protein Atlas ENSG00000131747
IntAct P11388
Guide to Pharmacology 2637
Open Targets ENSG00000131747
PharmGKB PA354
Reactome R-HSA-1362277 (Transcription of E2F targets under negative control by DREAM complex.)
R-HSA-4615885 (SUMOylation of DNA replication proteins.)
UniProt B2RTS1 P11388 Q71UN1 Q71UQ5 Q9HB24 Q9HB25 Q9HB26 Q9UP44 Q9UQP9

Target Cross References - Domain

InterPro IPR001241 (Topo_IIA.)
IPR002205 (Topo_IIA_A/C.)
IPR003594 (HATPase_C.)
IPR006171 (TOPRIM_domain.)
IPR012542 (DTHCT.)
IPR013506 (Topo_IIA_bsu_dom2.)
IPR013758 (Topo_IIA_A/C_ab.)
IPR013759 (Topo_IIA_B_C.)
IPR013760 (Topo_IIA-like_dom_sf.)
IPR014721 (Ribosomal_S5_D2-typ_fold_subgr.)
IPR018522 (TopoIIA_CS.)
IPR020568 (Ribosomal_S5_D2-typ_fold.)
IPR031660 (TOPRIM_C.)
IPR034157 (TOPRIM_TopoII.)
IPR036890 (HATPase_C_sf.)
Pfam PF00204 (DNA_gyraseB)
PF00521 (DNA_topoisoIV)
PF01751 (Toprim)
PF02518 (HATPase_c)
PF08070 (DTHCT)
PF16898 (TOPRIM_C)

Target Cross References - Structure

PDBe 1ZXM 1ZXN 4FM9 4R1F 5GWK
CREDO 1ZXM 1ZXN 4FM9 4R1F 5GWK
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