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Target Report Card

Target Name and Classification

Target ID CHEMBL3105
Target Type SINGLE PROTEIN
Preferred Name Poly [ADP-ribose] polymerase-1
Synonyms ADP-ribosyltransferase diphtheria toxin-like 1 | ADPRT 1 | ADPRT | ARTD1 | NAD(+) ADP-ribosyltransferase 1 | PARP-1 | PARP1 | PPOL | Poly [ADP-ribose] polymerase 1 | Poly[ADP-ribose] synthase 1
Organism Homo sapiens
Species Group No
Protein Target Classification
  • enzyme

Target Components

Component Description Relationship Accession
Poly [ADP-ribose] polymerase 1 SINGLE PROTEIN P09874

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL3390820 PARP 1, 2 and 3 PROTEIN FAMILY

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL1094636 NIRAPARIB Poly [ADP-ribose] polymerase-1 inhibitor 4 PubMed
CHEMBL3137320 TALAZOPARIB Poly [ADP-ribose] polymerase-1 inhibitor 3 PubMed
CHEMBL3137318 TALAZOPARIB TOSYLATE Poly [ADP-ribose] polymerase-1 inhibitor 2 PubMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000143799
Ensembl ENSG00000143799
GO Cellular Component GO:0000784 (nuclear chromosome, telomeric region)
GO:0005634 (nucleus)
GO:0005635 (nuclear envelope)
GO:0005654 (nucleoplasm)
GO:0005667 (transcription factor complex)
GO:0005730 (nucleolus)
GO:0005739 (mitochondrion)
GO:0016020 (membrane)
GO:0032991 (macromolecular complex)
GO:0032993 (protein-DNA complex)
GO Molecular Function GO:0000977 (RNA polymerase II regulatory region sequence-specific DNA binding)
GO:0001228 (transcriptional activator activity, RNA polymerase II transcription regulatory region sequence-specific binding)
GO:0003677 (DNA binding)
GO:0003723 (RNA binding)
GO:0003910 (DNA ligase (ATP) activity)
GO:0003950 (NAD+ ADP-ribosyltransferase activity)
GO:0005515 (protein binding)
GO:0008134 (transcription factor binding)
GO:0008270 (zinc ion binding)
GO:0016740 (transferase activity)
GO:0016757 (transferase activity, transferring glycosyl groups)
GO:0019899 (enzyme binding)
GO:0019901 (protein kinase binding)
GO:0030331 (estrogen receptor binding)
GO:0042802 (identical protein binding)
GO:0042826 (histone deacetylase binding)
GO:0046332 (SMAD binding)
GO:0046872 (metal ion binding)
GO:0047485 (protein N-terminus binding)
GO:0051287 (NAD binding)
GO:0070412 (R-SMAD binding)
GO:1990404 (protein ADP-ribosylase activity)
GO Biological Process GO:0000122 (negative regulation of transcription from RNA polymerase II promoter)
GO:0000715 (nucleotide-excision repair, DNA damage recognition)
GO:0000717 (nucleotide-excision repair, DNA duplex unwinding)
GO:0000723 (telomere maintenance)
GO:0000724 (double-strand break repair via homologous recombination)
GO:0006273 (lagging strand elongation)
GO:0006281 (DNA repair)
GO:0006293 (nucleotide-excision repair, preincision complex stabilization)
GO:0006294 (nucleotide-excision repair, preincision complex assembly)
GO:0006295 (nucleotide-excision repair, DNA incision, 3'-to lesion)
GO:0006296 (nucleotide-excision repair, DNA incision, 5'-to lesion)
GO:0006302 (double-strand break repair)
GO:0006351 (transcription, DNA-templated)
GO:0006355 (regulation of transcription, DNA-templated)
GO:0006366 (transcription from RNA polymerase II promoter)
GO:0006471 (protein ADP-ribosylation)
GO:0006915 (apoptotic process)
GO:0006974 (cellular response to DNA damage stimulus)
GO:0007005 (mitochondrion organization)
GO:0007179 (transforming growth factor beta receptor signaling pathway)
GO:0010332 (response to gamma radiation)
GO:0010613 (positive regulation of cardiac muscle hypertrophy)
GO:0010990 (regulation of SMAD protein complex assembly)
GO:0016540 (protein autoprocessing)
GO:0018312 (peptidyl-serine ADP-ribosylation)
GO:0023019 (signal transduction involved in regulation of gene expression)
GO:0030225 (macrophage differentiation)
GO:0032042 (mitochondrial DNA metabolic process)
GO:0032869 (cellular response to insulin stimulus)
GO:0033148 (positive regulation of intracellular estrogen receptor signaling pathway)
GO:0033683 (nucleotide-excision repair, DNA incision)
GO:0034599 (cellular response to oxidative stress)
GO:0034644 (cellular response to UV)
GO:0036211 (protein modification process)
GO:0042769 (DNA damage response, detection of DNA damage)
GO:0043504 (mitochondrial DNA repair)
GO:0044030 (regulation of DNA methylation)
GO:0045944 (positive regulation of transcription from RNA polymerase II promoter)
GO:0050790 (regulation of catalytic activity)
GO:0051103 (DNA ligation involved in DNA repair)
GO:0051901 (positive regulation of mitochondrial depolarization)
GO:0060391 (positive regulation of SMAD protein import into nucleus)
GO:0070212 (protein poly-ADP-ribosylation)
GO:0070911 (global genome nucleotide-excision repair)
GO:0071294 (cellular response to zinc ion)
GO:0071560 (cellular response to transforming growth factor beta stimulus)
GO:1900182 (positive regulation of protein localization to nucleus)
GO:1901216 (positive regulation of neuron death)
GO:1903376 (regulation of oxidative stress-induced neuron intrinsic apoptotic signaling pathway)
GO:1903518 (positive regulation of single strand break repair)
GO:1903827 (regulation of cellular protein localization)
GO:1904044 (response to aldosterone)
GO:1904357 (negative regulation of telomere maintenance via telomere lengthening)
GO:1904646 (cellular response to beta-amyloid)
GO:1904762 (positive regulation of myofibroblast differentiation)
GO:1990966 (ATP generation from poly-ADP-D-ribose)
GO:2000679 (positive regulation of transcription regulatory region DNA binding)
GO:2001170 (negative regulation of ATP biosynthetic process)
Wikipedia PARP1

Target Cross References - Protein

canSAR P09874
Human Protein Atlas ENSG00000143799
IntAct P09874
Guide to Pharmacology 2771
Open Targets ENSG00000143799
PharmGKB PA32
Reactome R-HSA-110362 (POLB-Dependent Long Patch Base Excision Repair.)
R-HSA-2173795 (Downregulation of SMAD2/3:SMAD4 transcriptional activity.)
R-HSA-3108214 (SUMOylation of DNA damage response and repair proteins.)
R-HSA-5685939 (HDR through MMEJ (alt-NHEJ).)
R-HSA-5696394 (DNA Damage Recognition in GG-NER.)
R-HSA-5696395 (Formation of Incision Complex in GG-NER.)
R-HSA-5696400 (Dual Incision in GG-NER.)
UniProt B1ANJ4 P09874 Q8IUZ9

Target Cross References - Domain

InterPro IPR001357 (BRCT_dom.)
IPR001510 (Znf_PARP.)
IPR004102 (Poly(ADP-ribose)pol_reg_dom.)
IPR008288 (PARP.)
IPR008893 (WGR_domain.)
IPR012317 (Poly(ADP-ribose)pol_cat_dom.)
IPR012982 (PADR1.)
IPR036420 (BRCT_dom_sf.)
IPR036616 (Poly(ADP-ribose)pol_reg_dom_sf.)
IPR036930 (WGR_dom_sf.)
IPR036957 (Znf_PARP_sf.)
Pfam PF00533 (BRCT)
PF00644 (PARP)
PF00645 (zf-PARP)
PF02877 (PARP_reg)
PF05406 (WGR)
PF08063 (PADR1)

Target Cross References - Structure

PDBe 1UK0 1UK1 1WOK 2RCW 2RD6 2RIQ 3GJW 3GN7 3L3L 3L3M 3OD8 3ODA 3ODC 3ODE 4AV1 4DQY 4GV7 4HHY 4HHZ 4L6S 4OPX 4OQA 4OQB 4PJT More...
CREDO 1UK0 1UK1 1WOK 2RCW 2RD6 2RIQ 3GJW 3GN7 3L3L 3L3M 3OD8 3ODA 3ODC 3ODE 4AV1 4DQY 4GV7 4HHY 4HHZ 4L6S 4OPX 4OQA 4OQB 4PJT More...
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