poly(ADP-ribose) polymerase 1 | Poly ADP-ribose polymerases | IUPHAR/BPS Guide to PHARMACOLOGY

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poly(ADP-ribose) polymerase 1

Target not currently curated in GtoImmuPdb

Target id: 2771

Nomenclature: poly(ADP-ribose) polymerase 1

Abbreviated Name: PARP1

Family: Poly ADP-ribose polymerases

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1014 1q41-q42 PARP1 poly(ADP-ribose) polymerase 1
Mouse - 1014 1 H5 Parp1 poly (ADP-ribose) polymerase family, member 1
Rat - 1014 13q26 Parp1 poly (ADP-ribose) polymerase 1
Previous and Unofficial Names
poly (ADP-ribose) polymerase family, member 1 | poly (ADP-ribose) polymerase family | ADP-ribosyltransferase | ADPRT | poly (ADP-ribose) polymerase 1 | PPOL
Database Links
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Structure of PARP1 catalytic domain bound to inhibitor BMN 673 (talazoparib)
Ligand:  talazoparib
Resolution:  2.35Å
Species:  Human
References:  1
Image of receptor 3D structure from RCSB PDB
Description:  Structure of human PARP1 catalytic domain bound to an isoindolinone inhibitor
Ligand:  compound 10b [PMID: 26222319]
Resolution:  1.9Å
Species:  Human
References:  6
Enzyme Reaction
EC Number:

Download all structure-activity data for this target as a CSV file

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 10b [PMID: 26222319] Hs Inhibition 7.1 pKd 6
pKd 7.1 (Kd 8.7x10-8 M) [6]
rucaparib Hs Inhibition 8.9 pKi 8
pKi 8.9 (Ki 1.4x10-9 M) [8]
AG14361 Hs Inhibition 8.2 pKi 7
pKi 8.2 (Ki 5.8x10-9 M) [7]
niraparib Hs Binding 8.4 pIC50 3
pIC50 8.4 (IC50 3.8x10-9 M) [3]
olaparib Hs Inhibition 8.3 pIC50 2,5
pIC50 8.3 (IC50 5x10-9 M) [2,5]
Description: Assayed using PARP-1 isolated from HeLa cells, in a scintillation proximity ELISA.
ME0328 Hs Inhibition 5.2 pIC50 4
pIC50 5.2 (IC50 6.3x10-6 M) [4]
talazoparib Hs Inhibition - - 1


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1. Aoyagi-Scharber M, Gardberg AS, Yip BK, Wang B, Shen Y, Fitzpatrick PA. (2014) Structural basis for the inhibition of poly(ADP-ribose) polymerases 1 and 2 by BMN 673, a potent inhibitor derived from dihydropyridophthalazinone. Acta Crystallogr F Struct Biol Commun, 70 (Pt 9): 1143-9. [PMID:25195882]

2. Dillon KJ, Smith GC, Martin NM. (2003) A FlashPlate assay for the identification of PARP-1 inhibitors. J Biomol Screen, 8 (3): 347-52. [PMID:12857389]

3. Jones P, Altamura S, Boueres J, Ferrigno F, Fonsi M, Giomini C, Lamartina S, Monteagudo E, Ontoria JM, Orsale MV et al.. (2009) Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors. J. Med. Chem., 52 (22): 7170-85. [PMID:19873981]

4. Lindgren AE, Karlberg T, Ekblad T, Spjut S, Thorsell AG, Andersson CD, Nhan TT, Hellsten V, Weigelt J, Linusson A et al.. (2013) Chemical probes to study ADP-ribosylation: synthesis and biochemical evaluation of inhibitors of the human ADP-ribosyltransferase ARTD3/PARP3. J. Med. Chem., 56 (23): 9556-68. [PMID:24188023]

5. Menear KA, Adcock C, Boulter R, Cockcroft XL, Copsey L, Cranston A, Dillon KJ, Drzewiecki J, Garman S, Gomez S et al.. (2008) 4-[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: a novel bioavailable inhibitor of poly(ADP-ribose) polymerase-1. J. Med. Chem., 51 (20): 6581-91. [PMID:18800822]

6. Papeo G, Posteri H, Borghi D, Busel AA, Caprera F, Casale E, Ciomei M, Cirla A, Corti E, D'Anello M et al.. (2015) Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy. J. Med. Chem., 58 (17): 6875-98. [PMID:26222319]

7. Skalitzky DJ, Marakovits JT, Maegley KA, Ekker A, Yu XH, Hostomsky Z, Webber SE, Eastman BW, Almassy R, Li J et al.. (2003) Tricyclic benzimidazoles as potent poly(ADP-ribose) polymerase-1 inhibitors. J. Med. Chem., 46 (2): 210-3. [PMID:12519059]

8. Thomas HD, Calabrese CR, Batey MA, Canan S, Hostomsky Z, Kyle S, Maegley KA, Newell DR, Skalitzky D, Wang LZ et al.. (2007) Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial. Mol. Cancer Ther., 6 (3): 945-56. [PMID:17363489]

How to cite this page

Poly ADP-ribose polymerases: poly(ADP-ribose) polymerase 1. Last modified on 28/11/2018. Accessed on 09/12/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2771.