poly(ADP-ribose) polymerase 2 | Poly ADP-ribose polymerases | IUPHAR/BPS Guide to PHARMACOLOGY

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poly(ADP-ribose) polymerase 2

Target not currently curated in GtoImmuPdb

Target id: 2772

Nomenclature: poly(ADP-ribose) polymerase 2

Abbreviated Name: PARP2

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 - 583 14q11.2-q12 PARP2 poly(ADP-ribose) polymerase 2
Mouse - 559 14 C1 Parp2 poly (ADP-ribose) polymerase family, member 2
Rat - 558 15p14 Parp2 poly (ADP-ribose) polymerase 2
Previous and Unofficial Names
poly (ADP-ribose) polymerase family, member 2 | poly (ADP-ribose) polymerase family | ADPRTL2 | poly (ADP-ribose) polymerase 2
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 PARP2 catalytic domain bound to inhibitor BMN 673 (talazoparib)
Ligand:  talazoparib
Resolution:  2.5Å
Species:  Human
References:  1
Image of receptor 3D structure from RCSB PDB
Description:  Structure of PARP2 catalytic domain bound to an isoindolinone inhibitor
Ligand:  compound 10b [PMID: 26222319]
Resolution:  1.65Å
Species:  Human
References:  7
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 6.9 pKd 7
pKd 6.9 (Kd 1.25x10-7 M) [7]
olaparib Hs Inhibition 9.0 pIC50 2,5
pIC50 9.0 (IC50 1x10-9 M) [2,5]
Description: Assayed using PARP-2 isolated from HeLa cells, in a scintillation proximity ELISA.
niraparib Hs Binding 8.7 pIC50 4
pIC50 8.7 (IC50 2.1x10-9 M) [4]
compound 5 [Tomassi et al., 2020] Hs Inhibition 7.4 pIC50 8
pIC50 7.4 (IC50 3.78x10-8 M) [8]
AZ1366 Hs Inhibition 6.6 pIC50 3
pIC50 6.6 (IC50 2.32x10-7 M) [3]
MC2050 Hs Inhibition 5.7 – 6.3 pIC50 6,8
pIC50 6.3 (IC50 5.49x10-7 M) [8]
pIC50 5.7 (IC50 1.8x10-6 M) [6]
Description: Inhibitory effect of MC2050 in vitro on recombinant PARP2.
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. Johannes JW, Almeida L, Barlaam B, Boriack-Sjodin PA, Casella R, Croft RA, Dishington AP, Gingipalli L, Gu C, Hawkins JL et al.. (2015) Pyrimidinone nicotinamide mimetics as selective tankyrase and wnt pathway inhibitors suitable for in vivo pharmacology. ACS Med Chem Lett, 6 (3): 254-9. [PMID:25815142]

4. 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]

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. Mosca L, Rotili D, Tempera I, Masci A, Fontana M, Chiaraluce R, Mastromarino P, d'Erme M, Mai A. (2011) Biological effects of MC2050, a quinazoline-based PARP-1 inhibitor, in human neuroblastoma and EBV-positive Burkitt's lymphoma cells. ChemMedChem, 6 (4): 606-11. [PMID:21365766]

7. 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]

8. Tomassi S, Pfahler J, Mautone N, Rovere A, Esposito C, Passeri D, Pellicciari R, Novellino E, Pannek M, Steegborn C et al.. (2020) From PARP1 to TNKS2 Inhibition: A Structure-Based Approach. ACS Med Chem Lett, [Articles ASAP]. DOI: 10.1021/acsmedchemlett.9b00654

How to cite this page

Poly ADP-ribose polymerases: poly(ADP-ribose) polymerase 2. Last modified on 14/02/2020. Accessed on 09/07/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2772.