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Target Report Card

Target Name and Classification

Target ID CHEMBL1781
Preferred Name DNA topoisomerase I
Synonyms DNA topoisomerase 1 | DNA topoisomerase I | TOP1
Organism Homo sapiens
Species Group No
Protein Target Classification
  • enzyme > isomerase

Target Components

Component Description Relationship Accession
DNA topoisomerase 1 SINGLE PROTEIN P11387

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL3989514 IRINOTECAN HYDROCHLORIDE DNA topoisomerase I inhibitor 4 DailyMed
CHEMBL2107313 BECATECARIN DNA topoisomerase I inhibitor 3 PubMed PubMed
CHEMBL3039558 ETIRINOTECAN PEGOL DNA topoisomerase I inhibitor 3 PubMed
CHEMBL3039564 IRINOTECAN SUCROSOFATE DNA topoisomerase I inhibitor 3 PubMed PubMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000198900
Ensembl ENSG00000198900
GO Cellular Component GO:0000228 (nuclear chromosome)
GO:0000932 (cytoplasmic mRNA processing body)
GO:0001650 (fibrillar center)
GO:0005634 (nucleus)
GO:0005654 (nucleoplasm)
GO:0005694 (chromosome)
GO:0005730 (nucleolus)
GO:0005737 (cytoplasm)
GO:0009330 (DNA topoisomerase complex (ATP-hydrolyzing))
GO:0031298 (replication fork protection complex)
GO:0032993 (protein-DNA complex)
GO:0043204 (perikaryon)
GO Molecular Function GO:0001046 (core promoter sequence-specific DNA binding)
GO:0003677 (DNA binding)
GO:0003682 (chromatin binding)
GO:0003690 (double-stranded DNA binding)
GO:0003697 (single-stranded DNA binding)
GO:0003723 (RNA binding)
GO:0003916 (DNA topoisomerase activity)
GO:0003917 (DNA topoisomerase type I activity)
GO:0004674 (protein serine/threonine kinase activity)
GO:0005515 (protein binding)
GO:0005524 (ATP binding)
GO:0016853 (isomerase activity)
GO:0019904 (protein domain specific binding)
GO:0097100 (supercoiled DNA binding)
GO Biological Process GO:0006260 (DNA replication)
GO:0006265 (DNA topological change)
GO:0006338 (chromatin remodeling)
GO:0007059 (chromosome segregation)
GO:0007623 (circadian rhythm)
GO:0012501 (programmed cell death)
GO:0016032 (viral process)
GO:0016310 (phosphorylation)
GO:0016925 (protein sumoylation)
GO:0018105 (peptidyl-serine phosphorylation)
GO:0032922 (circadian regulation of gene expression)
GO:0040016 (embryonic cleavage)
GO:0042493 (response to drug)
GO:0048511 (rhythmic process)
Wikipedia TOP1

Target Cross References - Protein

canSAR P11387
Human Protein Atlas ENSG00000198900
IntAct P11387
Open Targets ENSG00000198900
PharmGKB PA353
Reactome R-HSA-4615885 (SUMOylation of DNA replication proteins.)
UniProt A8KA78 E1P5W3 O43256 P11387 Q12855 Q12856 Q15610 Q5TFY3 Q9UJN0

Target Cross References - Domain

InterPro IPR001631 (TopoI.)
IPR008336 (TopoI_DNA-bd_euk.)
IPR011010 (DNA_brk_join_enz.)
IPR013030 (DNA_topo_DNA_db_N_dom2.)
IPR013034 (DNA_topo_DNA_db_N_dom1.)
IPR013499 (TopoI_euk.)
IPR013500 (TopoI_cat_euk.)
IPR014711 (TopoI_cat_a-hlx-sub_euk.)
IPR014727 (TopoI_cat_a/b-sub_euk.)
IPR018521 (TopoI_AS.)
IPR025834 (TopoI_C_dom.)
IPR036202 (TopoI_DNA-bd_euk_N_sf.)
Pfam PF01028 (Topoisom_I)
PF02919 (Topoisom_I_N)
PF14370 (Topo_C_assoc)

Target Cross References - Structure

PDBe 1A31 1A35 1A36 1EJ9 1K4S 1K4T 1LPQ 1NH3 1R49 1RR8 1RRJ 1SC7 1SEU 1T8I 1TL8
CREDO 1A31 1A35 1A36 1EJ9 1K4S 1K4T 1LPQ 1NH3 1R49 1RR8 1RRJ 1SC7 1SEU 1T8I 1TL8