General Information of the Protein
Protein ID
PT01328
Protein Name
Poly [ADP-ribose] polymerase 2
Secondarily
Protein Name
ADP-ribosyltransferase diphtheria toxin-like 2
DNA ADP-ribosyltransferase PARP2
NAD(+) ADP-ribosyltransferase 2
Poly[ADP-ribose] synthase 2
Protein poly-ADP-ribosyltransferase PARP2
Gene Name
PARP2
Secondarily
Gene Name
ADPRT2
ADPRTL2
Sequence
MAARRRRSTGGGRARALNESKRVNNGNTAPEDSSPAKKTRRCQRQESKKMPVAGGKANKDRTEDKQDGMPGRSWASKRVSESVKALLLKGKAPVDPECTAKVGKAHVYCEGNDVYDVMLNQTNLQFNNNKYYLIQLLEDDAQRNFSVWMRWGRVGKMGQHSLVACSGNLNKAKEIFQKKFLDKTKNNWEDREKFEKVPGKYDMLQMDYATNTQDEEETKKEESLKSPLKPESQLDLRVQELIKLICNVQAMEEMMMEMKYNTKKAPLGKLTVAQIKAGYQSLKKIEDCIRAGQHGRALMEACNEFYTRIPHDFGLRTPPLIRTQKELSEKIQLLEALGDIEIAIKLVKTELQSPEHPLDQHYRNLHCALRPLDHESYEFKVISQYLQSTHAPTHSDYTMTLLDLFEVEKDGEKEAFREDLHNRMLLWHGSRMSNWVGILSHGLRIAPPEAPITGYMFGKGIYFADMSSKSANYCFASRLKNTGLLLLSEVALGQCNELLEANPKAEGLLQGKHSTKGLGKMAPSSAHFVTLNGSTVPLGPASDTGILNPDGYTLNYNEYIVYNPNQVRMRYLLKVQFNFLQLW
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Transferase
Function
Poly-ADP-ribosyltransferase that mediates poly-ADP-ribosylation of proteins and plays a key role in DNA repair (PubMed:10364231, PubMed:25043379, PubMed:27471034, PubMed:30104678, PubMed:32028527, PubMed:32939087, PubMed:34486521, PubMed:34874266, PubMed:34108479). Mediates glutamate, aspartate or serine ADP-ribosylation of proteins: the ADP-D-ribosyl group of NAD(+) is transferred to the acceptor carboxyl group of target residues and further ADP-ribosyl groups are transferred to the 2'-position of the terminal adenosine moiety, building up a polymer with an average chain length of 20-30 units (PubMed:25043379, PubMed:30104678, PubMed:30321391). Serine ADP-ribosylation of proteins constitutes the primary form of ADP-ribosylation of proteins in response to DNA damage (PubMed:32939087). Mediates glutamate and aspartate ADP-ribosylation of target proteins in absence of HPF1 (PubMed:25043379). Following interaction with HPF1, catalyzes serine ADP-ribosylation of target proteins; HPF1 conferring serine specificity by completing the PARP2 active site (PubMed:28190768, PubMed:32028527, PubMed:34486521, PubMed:34874266, PubMed:34108479). PARP2 initiates the repair of double-strand DNA breaks: recognizes and binds DNA breaks within chromatin and recruits HPF1, licensing serine ADP-ribosylation of target proteins, such as histones, thereby promoting decompaction of chromatin and the recruitment of repair factors leading to the reparation of DNA strand breaks (PubMed:10364231, PubMed:32939087, PubMed:34108479). HPF1 initiates serine ADP-ribosylation but restricts the polymerase activity of PARP2 in order to limit the length of poly-ADP-ribose chains (PubMed:34732825, PubMed:34795260). Specifically mediates formation of branched poly-ADP-ribosylation (PubMed:30104678). Branched poly-ADP-ribose chains are specifically recognized by some factors, such as APLF (PubMed:30104678). In addition to proteins, also able to ADP-ribosylate DNA: preferentially acts on 5'-terminal phosphates at DNA strand breaks termini in nicked duplex (PubMed:27471034, PubMed:29361132).
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Uniprot ID
Primary ID:
Q9UGN5

Secondarily ID:
Q8TEU4
Q9NUV2
Q9UMR4
Q9Y6C8
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Ensembl ID
ENSG00000129484
HGNC ID
HGNC:272
Subcellular Location
Nucleus
Chromosome
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000013 , Sf9
Compound ID Compound Name Compound Formula
CP0120515
4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbonyl]-4-fluorophenyl}methyl)-1,2-dihydrophthalazin-1-one
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C24H23FN4O3
 2
1
IC50 = 0.5 nM
   TI
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2
IC50 = 2.81 nM
   TI
   LI
   LO
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CP0132947
BMN 673
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C19H14F2N6O
 1
1
IC50 = 0.6 nM
   TI
   LI
   LO
   TS
CP0120402
AG-014699
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C19H18FN3O
 2
1
IC50 = 0.8 nM
   TI
   LI
   LO
   TS
2
Ki = 0.7 nM
   TI
   LI
   LO
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CP0902702
(R)-4-(4-(3-(5-amino-7-fluoro-1-oxo-1,2-dihydroisoquinolin-3-yl)cyclopent-2-en-1-yl)piperazin-1-yl)benzonitrile
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C25H24FN5O
 1
1
IC50 = 1.3 nM
   TI
   LI
   LO
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CP0907079
(R)-4-(4-(3-(5-amino-1-oxo-1,2-dihydroisoquinolin-3-yl)cyclopent-2-en-1-yl)piperazin-1-yl)benzonitrile
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C25H25N5O
 1
1
IC50 = 1.5 nM
   TI
   LI
   LO
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CP0229896
(E)-3-[4-[[4-[2-fluoro-5-[(4-oxo-3H-phthalazin-1-yl)methyl]benzoyl]piperazin-1-yl]methyl]phenyl]-N-hydroxyprop-2-enamide
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C30H28FN5O4
 1
1
IC50 = 2.53 nM
   TI
   LI
   LO
   TS
CP0910531
(R)-4-(4-(3-(5-amino-7-fluoro-1-oxo-1,2-dihydroisoquinolin-3-yl)cyclopent-2-enyl)piperazin-1-yl)-3-fluorobenzonitrile
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C25H23F2N5O
 1
1
IC50 = 2.6 nM
   TI
   LI
   LO
   TS
CP0514715
4-[4-[3-(5-amino-7-fluoro-1-oxo-2H-isoquinolin-3-yl)propyl]piperazin-1-yl]benzonitrile
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C23H24FN5O
 1
1
IC50 = 3.9 nM
   TI
   LI
   LO
   TS
CP0471164
4-[4-[3-(5-amino-7-fluoro-1-oxo-2H-isoquinolin-3-yl)propyl]piperazin-1-yl]benzamide
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C23H26FN5O2
 1
1
IC50 = 4.6 nM
   TI
   LI
   LO
   TS
CP0236214
2-fluoro-N-[2-[4-[(E)-3-(hydroxyamino)-3-oxoprop-1-enyl]phenyl]ethyl]-5-[(4-oxo-3H-phthalazin-1-yl)methyl]benzamide
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C27H23FN4O4
 1
1
IC50 = 5.02 nM
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CP0423422
4-[4-[3-(5-amino-1-oxo-2H-isoquinolin-3-yl)propyl]piperazin-1-yl]benzonitrile
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C23H25N5O
 1
1
IC50 = 7.2 nM
   TI
   LI
   LO
   TS
CP0701437
(R)-4-(4-(3-(5-oxo-5,6-dihydro-1,6-naphthyridin-7-yl)cyclopent-2-en-1-yl)piperazin-1-yl)benzonitrile
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C24H23N5O
 1
1
IC50 = 8.1 nM
   TI
   LI
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   TS
CP0496431
5-amino-7-fluoro-3-[3-[4-(4-fluorophenyl)piperazin-1-yl]propyl]-2H-isoquinolin-1-one
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C22H24F2N4O
 1
1
IC50 = 9.5 nM
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CP0044519
2-[(2R)-2-methylpyrrolidin-2-yl]-1H-1,3-benzodiazole-4-carboxamide
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C13H16N4O
 1
1
IC50 < 10 nM
   TI
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CP0416019
(2Z)-2-[[4-[3-(hydroxymethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazine-7-carbonyl]phenyl]methylidene]-3-oxo-1-benzofuran-7-carboxamide
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C23H19N5O5
 1
1
IC50 < 10 nM
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CP0416021
(2Z)-2-[[4-[2-(1H-benzimidazol-2-yl)ethylcarbamoyl]phenyl]methylidene]-3-oxo-1-benzofuran-7-carboxamide
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C26H20N4O4
 1
1
IC50 = 10 nM
   TI
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CP0420894
(2Z)-2-[[4-[3-[(3-fluorophenyl)methyl]-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazine-7-carbonyl]phenyl]methylidene]-3-oxo-1-benzofuran-7-carboxamide
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C29H22FN5O4
 1
1
IC50 < 10 nM
   TI
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CP0484282
(2Z)-2-[[4-(3-methyl-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazine-7-carbonyl)phenyl]methylidene]-3-oxo-1-benzofuran-7-carboxamide
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C23H19N5O4
 1
1
IC50 < 10 nM
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CP0540730
4-[4-[3-(5-amino-7-fluoro-1-oxo-2H-isoquinolin-3-yl)propyl]piperazin-1-yl]-N-methylbenzamide
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C24H28FN5O2
 1
1
IC50 = 10.8 nM
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CP0047264
2-(dimethylamino)-N-(6-oxo-5,6-dihydrophenanthridin-2-yl)acetamide
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C17H17N3O2
 1
1
IC50 = 14.7 nM
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CP0957575
(R)-6-(4-(3-(5-oxo-5,6-dihydro-1,6-naphthyridin-7-yl)cyclopent-2-en-1-yl)piperazin-1-yl)nicotinonitrile
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C23H22N6O
 1
1
IC50 = 16.6 nM
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CP0902704
(R)-4-(4-(3-(3-fluoro-5-oxo-5,6-dihydro-1,6-naphthyridin-7-yl)cyclopent-2-en-1-yl)piperazin-1-yl)benzonitrile
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C24H22FN5O
 1
1
IC50 = 26.9 nM
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CP0228522
4-[[4-[2-fluoro-5-[(4-oxo-3H-phthalazin-1-yl)methyl]benzoyl]piperazin-1-yl]methyl]-N-hydroxybenzamide
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C28H26FN5O4
 1
1
IC50 = 31.52 nM
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CP0076480
2-[2-[4-[2-[(4-oxo-3H-quinazolin-2-yl)sulfanyl]ethyl]piperazin-1-yl]ethylsulfanyl]-3H-quinazolin-4-one
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C24H26N6O2S2
 1
1
IC50 = 37.8 nM
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CP0360699
2-[4-[[4-[2-fluoro-5-[(4-oxo-3H-phthalazin-1-yl)methyl]benzoyl]piperazin-1-yl]methyl]phenyl]-N-hydroxyacetamide
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C29H28FN5O4
 1
1
IC50 = 49.12 nM
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CP0416015
(2Z)-2-[[4-[4-(4-methoxypyrimidin-2-yl)piperazine-1-carbonyl]phenyl]methylidene]-3-oxo-1-benzofuran-7-carboxamide
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C26H23N5O5
 1
1
IC50 < 50 nM
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CP0416026
(2Z)-3-oxo-2-[[3-(2H-tetrazol-5-yl)phenyl]methylidene]-1-benzofuran-7-carboxamide
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C17H11N5O3
 1
1
IC50 < 50 nM
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CP0416031
(2Z)-3-oxo-2-[[3-(4-pyrazin-2-ylpiperazine-1-carbonyl)phenyl]methylidene]-1-benzofuran-7-carboxamide
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C25H21N5O4
 1
1
IC50 < 50 nM
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CP0420890
(2Z)-2-[[4-[4-[4-[5-(methoxymethyl)-1,2,4-oxadiazol-3-yl]pyrimidin-2-yl]piperazine-1-carbonyl]phenyl]methylidene]-3-oxo-1-benzofuran-7-carboxamide
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C29H25N7O6
 1
1
IC50 < 50 nM
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CP0420896
(2Z)-3-oxo-2-[[4-(4-pyrimidin-2-ylpiperazin-1-yl)phenyl]methylidene]-1-benzofuran-7-carboxamide
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C24H21N5O3
 1
1
IC50 < 50 nM
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CP0420897
(2Z)-2-[[3-fluoro-4-(2H-tetrazol-5-yl)phenyl]methylidene]-3-oxo-1-benzofuran-7-carboxamide
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C17H10FN5O3
 1
1
IC50 < 50 nM
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CP0420899
(2Z)-3-oxo-2-[[4-(4-pyrazin-2-ylpiperazine-1-carbonyl)phenyl]methylidene]-1-benzofuran-7-carboxamide
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C25H21N5O4
 1
1
IC50 < 50 nM
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CP0420907
(2Z)-3-oxo-2-[[4-[(4-pyrimidin-2-ylpiperazin-1-yl)methyl]phenyl]methylidene]-1-benzofuran-7-carboxamide
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C25H23N5O3
 1
1
IC50 < 50 nM
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CP0421438
(2Z)-3-oxo-2-[[3-(4-pyrimidin-2-ylpiperazine-1-carbonyl)phenyl]methylidene]-1-benzofuran-7-carboxamide
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C25H21N5O4
 1
1
IC50 < 50 nM
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CP0457081
(2Z)-2-[[3-[4-(4-methoxypyrimidin-2-yl)piperazine-1-carbonyl]phenyl]methylidene]-3-oxo-1-benzofuran-7-carboxamide
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C26H23N5O5
 1
1
IC50 < 50 nM
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CP0491024
(2Z)-3-oxo-2-[[4-(4-pyrimidin-2-ylpiperazine-1-carbonyl)phenyl]methylidene]-1-benzofuran-7-carboxamide
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C25H21N5O4
 1
1
IC50 < 50 nM
   TI
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CP0870470
(S)-4-(4-(3-(5-amino-7-fluoro-1-oxo-1,2-dihydroisoquinolin-3-yl)cyclopent-2-enyl)piperazin-1-yl)-3-fluorobenzonitrile
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C25H23F2N5O
 1
1
IC50 = 58 nM
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CP0870563
(S)-4-(4-(3-(5-amino-1-oxo-1,2-dihydroisoquinolin-3-yl)cyclopent-2-en-1-yl)piperazin-1-yl)benzonitrile
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C25H25N5O
 1
1
IC50 = 167 nM
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CP0907078
(S)-4-(4-(3-(5-amino-7-fluoro-1-oxo-1,2-dihydroisoquinolin-3-yl)cyclopent-2-en-1-yl)piperazin-1-yl)benzonitrile
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C25H24FN5O
 1
1
IC50 = 200 nM
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CP0076475
2-[2-[4-[3-(4-phenylphenoxy)propyl]piperazin-1-yl]ethylsulfanyl]-3H-quinazolin-4-one
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C29H32N4O2S
 1
1
IC50 = 340 nM
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CP0076478
1'-[2-[4-[2-[(4-oxo-3H-quinazolin-2-yl)sulfanyl]ethyl]piperazin-1-yl]acetyl]spiro[3H-chromene-2,4'-piperidine]-4-one
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C29H33N5O4S
 1
1
IC50 = 347 nM
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CP0368203
2-[2-[4-[3-(3-phenyl-1,2,4-oxadiazol-5-yl)propyl]piperazin-1-yl]ethylsulfanyl]-3H-quinazolin-4-one
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C25H28N6O2S
 1
1
IC50 = 370 nM
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CP0368202
2-[2-(4-pyridin-2-ylpiperazin-1-yl)ethylsulfanyl]-3H-quinazolin-4-one
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C19H21N5OS
 1
1
IC50 = 549 nM
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CP0391453
benzyl 4-[2-[(4-oxo-3H-quinazolin-2-yl)sulfanyl]ethyl]piperazine-1-carboxylate
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C22H24N4O3S
 1
1
IC50 = 963 nM
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CP0346125
6,8-difluoro-2-[4-(2-hydroxypropan-2-yl)phenyl]-3H-quinazolin-4-one
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C17H14F2N2O2
 1
1
IC50 = 1000 nM
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CP0113878
4-[(1R,2R,6S,7S)-3,5-dioxo-4-azatricyclo[5.2.1.02,6]decan-4-yl]-N-quinolin-8-ylbenzamide
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C25H21N3O3
 1
1
IC50 > 100000 nM
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CP0416022
(2Z)-2-[[3-[2-(1H-benzimidazol-2-yl)ethylcarbamoyl]phenyl]methylidene]-3-oxo-1-benzofuran-7-carboxamide
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C26H20N4O4
 1
1
IC50 > 10 nM
   TI
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CP0416023
(2Z)-2-[[4-[4-(1H-benzimidazol-2-yl)piperidine-1-carbonyl]phenyl]methylidene]-3-oxo-1-benzofuran-7-carboxamide
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C29H24N4O4
 1
1
IC50 > 10 nM
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CP0416035
(2Z)-2-[[4-[[1-(1H-benzimidazol-2-yl)-2-methylpropan-2-yl]carbamoyl]phenyl]methylidene]-3-oxo-1-benzofuran-7-carboxamide
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C28H24N4O4
 1
1
IC50 > 10 nM
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CP0420891
(2Z)-3-oxo-2-[[3-[3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazine-7-carbonyl]phenyl]methylidene]-1-benzofuran-7-carboxamide
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C23H16F3N5O4
 1
1
IC50 > 10 nM
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CP0420892
(2Z)-2-[[4-[2-(6-methoxy-1H-benzimidazol-2-yl)ethylcarbamoyl]phenyl]methylidene]-3-oxo-1-benzofuran-7-carboxamide
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C27H22N4O5
 1
1
IC50 > 10 nM
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CP0420893
(2Z)-2-[[4-[3-(1H-benzimidazol-2-yl)propylcarbamoyl]phenyl]methylidene]-3-oxo-1-benzofuran-7-carboxamide
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C27H22N4O4
 1
1
IC50 > 10 nM
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CP0420902
(2Z)-2-[[4-(6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazine-7-carbonyl)phenyl]methylidene]-3-oxo-1-benzofuran-7-carboxamide
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C22H17N5O4
 1
1
IC50 > 10 nM
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CP0420906
(2Z)-2-[[4-[3-(1H-benzimidazol-2-yl)azetidine-1-carbonyl]phenyl]methylidene]-3-oxo-1-benzofuran-7-carboxamide
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C27H20N4O4
 1
1
IC50 > 10 nM
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CP0420909
(2Z)-2-[[3-[2-(6-fluoro-1H-benzimidazol-2-yl)ethylcarbamoyl]phenyl]methylidene]-3-oxo-1-benzofuran-7-carboxamide
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C26H19FN4O4
 1
1
IC50 > 10 nM
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CP0421445
(2Z)-2-[[3-(6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazine-7-carbonyl)phenyl]methylidene]-3-oxo-1-benzofuran-7-carboxamide
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C22H17N5O4
 1
1
IC50 > 10 nM
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CP0426414
(2Z)-2-[[4-[2-(6-fluoro-1H-benzimidazol-2-yl)ethylcarbamoyl]phenyl]methylidene]-3-oxo-1-benzofuran-7-carboxamide
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C26H19FN4O4
 1
1
IC50 > 10 nM
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CP0420900
(2Z)-3-oxo-2-[[4-(4-pyrimidin-2-ylpiperidine-1-carbonyl)phenyl]methylidene]-1-benzofuran-7-carboxamide
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C26H22N4O4
 1
1
IC50 > 50 nM
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Biochemical Assays
Compound ID Compound Name Compound Formula
CP0120515
4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbonyl]-4-fluorophenyl}methyl)-1,2-dihydrophthalazin-1-one
   Show/Hide
C24H23FN4O3
 14
1 IC50 = 0.1 nM
2 IC50 = 0.4 nM
3 IC50 = 0.45 nM
4 IC50 = 1 nM
5 IC50 = 1.01 nM
6 IC50 = 1.2 nM
7 IC50 = 1.87 nM
8 IC50 = 2.26 nM
9 IC50 = 2.81 nM
10 IC50 = 2.93 nM
11 IC50 = 3 nM
12 Kd = 0.27 nM
13 Kd = 0.28 nM
14 Kd = 0.5 nM
CP0132947
BMN 673
   Show/Hide
C19H14F2N6O
 5
1 IC50 = 0.2 nM
2 IC50 = 1 nM
3 Kd = 3.3 nM
4 Ki = 0.85 nM
5 Ki = 0.9 nM
CP0120402
AG-014699
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C19H18FN3O
 5
1 IC50 = 0.4 nM
2 IC50 = 0.5 nM
3 IC50 = 1.5 nM
4 IC50 = 38.9 nM
5 Kd = 26 nM
CP0044519
2-[(2R)-2-methylpyrrolidin-2-yl]-1H-1,3-benzodiazole-4-carboxamide
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C13H16N4O
 6
1 IC50 = 1.3 nM
2 IC50 = 70 nM
3 Kd = 5.8 nM
4 Kd = 11 nM
5 Ki = 5 nM
6 Ki = 17.5 nM
CP0229896
(E)-3-[4-[[4-[2-fluoro-5-[(4-oxo-3H-phthalazin-1-yl)methyl]benzoyl]piperazin-1-yl]methyl]phenyl]-N-hydroxyprop-2-enamide
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C30H28FN5O4
 1
1 IC50 = 2.53 nM
CP0519410
6-[(2S,6R)-2,6-dimethylmorpholin-4-yl]-4-fluoro-1-methyl-1'-(8-methyl-4-oxo-3,5,6,7-tetrahydropyrido[2,3-d]pyrimidin-2-yl)spiro[indole-3,4'-piperidine]-2-one
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C27H35FN6O3
 1
1 IC50 = 1240 nM
CP0383109
2-[4-(2-methoxyphenyl)piperazin-1-yl]-5,6,7,8-tetrahydro-3H-quinazolin-4-one
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C19H24N4O2
 1
1 IC50 = 2230 nM
CP0013089
2-[4,6-difluoro-1-(2-hydroxyethyl)spiro[2H-indole-3,4'-piperidine]-1'-yl]-5,6,7,8-tetrahydro-3H-quinazolin-4-one
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C22H26F2N4O2
 1
1 IC50 = 2717 nM
Clinical Information about the Protein
Target 1 ( Poly [ADP-ribose] polymerase 2 (PARP2) )
Target Type Clinical trial Target
Disease 1 Target-related Disease  1
1 Ovarian cancer [ICD-11: 2C73]
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 PMID27841036-Compound-37 Phase 2
Ovarian cancer