General Information of the Protein
Protein ID
PT02202
Protein Name
Poly [ADP-ribose] polymerase tankyrase-1
Secondarily
Protein Name
ADP-ribosyltransferase diphtheria toxin-like 5
Poly [ADP-ribose] polymerase 5A
Protein poly-ADP-ribosyltransferase tankyrase-1
TNKS-1
TRF1-interacting ankyrin-related ADP-ribose polymerase
Tankyrase I
Tankyrase-1
Gene Name
TNKS
Secondarily
Gene Name
PARP5A
PARPL
TIN1
TINF1
TNKS1
Sequence
MAASRRSQHHHHHHQQQLQPAPGASAPPPPPPPPLSPGLAPGTTPASPTASGLAPFASPRHGLALPEGDGSRDPPDRPRSPDPVDGTSCCSTTSTICTVAAAPVVPAVSTSSAAGVAPNPAGSGSNNSPSSSSSPTSSSSSSPSSPGSSLAESPEAAGVSSTAPLGPGAAGPGTGVPAVSGALRELLEACRNGDVSRVKRLVDAANVNAKDMAGRKSSPLHFAAGFGRKDVVEHLLQMGANVHARDDGGLIPLHNACSFGHAEVVSLLLCQGADPNARDNWNYTPLHEAAIKGKIDVCIVLLQHGADPNIRNTDGKSALDLADPSAKAVLTGEYKKDELLEAARSGNEEKLMALLTPLNVNCHASDGRKSTPLHLAAGYNRVRIVQLLLQHGADVHAKDKGGLVPLHNACSYGHYEVTELLLKHGACVNAMDLWQFTPLHEAASKNRVEVCSLLLSHGADPTLVNCHGKSAVDMAPTPELRERLTYEFKGHSLLQAAREADLAKVKKTLALEIINFKQPQSHETALHCAVASLHPKRKQVTELLLRKGANVNEKNKDFMTPLHVAAERAHNDVMEVLHKHGAKMNALDTLGQTALHRAALAGHLQTCRLLLSYGSDPSIISLQGFTAAQMGNEAVQQILSESTPIRTSDVDYRLLEASKAGDLETVKQLCSSQNVNCRDLEGRHSTPLHFAAGYNRVSVVEYLLHHGADVHAKDKGGLVPLHNACSYGHYEVAELLVRHGASVNVADLWKFTPLHEAAAKGKYEICKLLLKHGADPTKKNRDGNTPLDLVKEGDTDIQDLLRGDAALLDAAKKGCLARVQKLCTPENINCRDTQGRNSTPLHLAAGYNNLEVAEYLLEHGADVNAQDKGGLIPLHNAASYGHVDIAALLIKYNTCVNATDKWAFTPLHEAAQKGRTQLCALLLAHGADPTMKNQEGQTPLDLATADDIRALLIDAMPPEALPTCFKPQATVVSASLISPASTPSCLSAASSIDNLTGPLAELAVGGASNAGDGAAGTERKEGEVAGLDMNISQFLKSLGLEHLRDIFETEQITLDVLADMGHEELKEIGINAYGHRHKLIKGVERLLGGQQGTNPYLTFHCVNQGTILLDLAPEDKEYQSVEEEMQSTIREHRDGGNAGGIFNRYNVIRIQKVVNKKLRERFCHRQKEVSEENHNHHNERMLFHGSPFINAIIHKGFDERHAYIGGMFGAGIYFAENSSKSNQYVYGIGGGTGCPTHKDRSCYICHRQMLFCRVTLGKSFLQFSTMKMAHAPPGHHSVIGRPSVNGLAYAEYVIYRGEQAYPEYLITYQIMKPEAPSQTATAAEQKT
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Transferase
Function
Poly-ADP-ribosyltransferase involved in various processes such as Wnt signaling pathway, telomere length and vesicle trafficking (PubMed:10988299, PubMed:11739745, PubMed:16076287, PubMed:19759537, PubMed:21478859, PubMed:22864114, PubMed:23622245, PubMed:25043379). Acts as an activator of the Wnt signaling pathway by mediating poly-ADP-ribosylation (PARsylation) of AXIN1 and AXIN2, 2 key components of the beta-catenin destruction complex: poly-ADP-ribosylated target proteins are recognized by RNF146, which mediates their ubiquitination and subsequent degradation (PubMed:19759537, PubMed:21478859). Also mediates PARsylation of BLZF1 and CASC3, followed by recruitment of RNF146 and subsequent ubiquitination (PubMed:21478859). Mediates PARsylation of TERF1, thereby contributing to the regulation of telomere length (PubMed:11739745). Involved in centrosome maturation during prometaphase by mediating PARsylation of HEPACAM2/MIKI (PubMed:22864114). May also regulate vesicle trafficking and modulate the subcellular distribution of SLC2A4/GLUT4-vesicles (PubMed:10988299). May be involved in spindle pole assembly through PARsylation of NUMA1 (PubMed:16076287). Stimulates 26S proteasome activity (PubMed:23622245).
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Uniprot ID
Primary ID:
O95271

Secondarily ID:
O95272
Q4G0F2
Q59FX0
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Ensembl ID
ENSG00000173273
HGNC ID
HGNC:11941
Subcellular Location
Cytoplasm
Golgi apparatus membrane
Cytoplasm
Cytoskeleton
Microtubule organizing center
Centrosome
Nucleus
Nuclear pore complex
Chromosome
Telomere
Cytoplasm
Cytoskeleton
Spindle pole
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: CL000006 , HEK293
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0508441
 Compound Info 
(4-pyrimidin-4-ylpiperazin-1-yl)-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]methanone
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C23H20N10O
  1
1
IC50 = 6.31 nM
 Bioactivity Info 
   TI
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CP0154599
 Compound Info 
(4-pyrimidin-2-ylpiperazin-1-yl)-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]methanone
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C23H20N10O
  1
1
IC50 = 19.95 nM
 Bioactivity Info 
   TI
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CP0154554
 Compound Info 
[4-(1-methylimidazole-4-carbonyl)piperazin-1-yl]-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]methanone
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C24H22N10O2
  1
1
IC50 = 31.62 nM
 Bioactivity Info 
   TI
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CP0458446
 Compound Info 
(4-pyridin-3-ylpiperazin-1-yl)-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]methanone
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C24H21N9O
  1
1
IC50 = 63.1 nM
 Bioactivity Info 
   TI
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CP0454432
 Compound Info 
N-methyl-N-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]acetamide
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C17H15N7O
  1
1
IC50 = 79.43 nM
 Bioactivity Info 
   TI
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CP0539024
 Compound Info 
N-(2-methoxyethyl)-N-methyl-4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)benzamide
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C19H19N7O2
  1
1
IC50 = 79.43 nM
 Bioactivity Info 
   TI
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CP0447057
 Compound Info 
1-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]pyrrolidin-2-one
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C18H15N7O
  1
1
IC50 = 100 nM
 Bioactivity Info 
   TI
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CP0454433
 Compound Info 
4-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]morpholin-3-one
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C18H15N7O2
  1
1
IC50 = 100 nM
 Bioactivity Info 
   TI
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CP0454455
 Compound Info 
[4-(1-methylpyrazole-3-carbonyl)piperazin-1-yl]-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]methanone
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C24H22N10O2
  1
1
IC50 = 100 nM
 Bioactivity Info 
   TI
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CP0492107
 Compound Info 
(4-pyridin-2-ylpiperazin-1-yl)-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]methanone
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C24H21N9O
  1
1
IC50 = 100 nM
 Bioactivity Info 
   TI
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CP0432544
 Compound Info 
(4-pyridin-4-ylpiperazin-1-yl)-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]methanone
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C24H21N9O
  1
1
IC50 = 125.89 nM
 Bioactivity Info 
   TI
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CP0462220
 Compound Info 
1-[4-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)benzoyl]piperazin-1-yl]ethanone
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C21H20N8O2
  1
1
IC50 = 125.89 nM
 Bioactivity Info 
   TI
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CP0468722
 Compound Info 
[4-(1H-pyrazole-5-carbonyl)piperazin-1-yl]-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]methanone
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C23H20N10O2
  1
1
IC50 = 125.89 nM
 Bioactivity Info 
   TI
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CP0118849
 Compound Info 
morpholin-4-yl-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]methanone
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C19H17N7O2
  1
1
IC50 = 158.49 nM
 Bioactivity Info 
   TI
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CP0154596
 Compound Info 
N-(4-propan-2-ylphenyl)tetrazolo[1,5-a]quinoxalin-4-amine
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C17H16N6
  1
1
IC50 = 199.53 nM
 Bioactivity Info 
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CP0558598
 Compound Info 
oxan-4-yl-[4-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)benzoyl]piperazin-1-yl]methanone
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C25H26N8O3
  1
1
IC50 = 199.53 nM
 Bioactivity Info 
   TI
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CP0412937
 Compound Info 
[4-(1H-imidazole-5-carbonyl)piperazin-1-yl]-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]methanone
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C23H20N10O2
  1
1
IC50 = 251.19 nM
 Bioactivity Info 
   TI
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CP0492105
 Compound Info 
N-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]acetamide
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C16H13N7O
  1
1
IC50 = 251.19 nM
 Bioactivity Info 
   TI
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CP0492106
 Compound Info 
[4-(oxan-4-yl)piperazin-1-yl]-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]methanone
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C24H26N8O2
  1
1
IC50 = 251.19 nM
 Bioactivity Info 
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CP0454456
 Compound Info 
[4-(3-methylimidazole-4-carbonyl)piperazin-1-yl]-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]methanone
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C24H22N10O2
  1
1
IC50 = 398.11 nM
 Bioactivity Info 
   TI
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CP0533477
 Compound Info 
[4-(pyrimidine-2-carbonyl)piperazin-1-yl]-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]methanone
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C24H20N10O2
  1
1
IC50 = 398.11 nM
 Bioactivity Info 
   TI
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CP0432542
 Compound Info 
piperidin-1-yl-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]methanone
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C20H19N7O
  1
1
IC50 = 501.19 nM
 Bioactivity Info 
   TI
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CP0558588
 Compound Info 
N-(2-methoxyethyl)-4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)benzamide
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C18H17N7O2
  1
1
IC50 = 630.96 nM
 Bioactivity Info 
   TI
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CP0454457
 Compound Info 
piperazin-1-yl-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]methanone
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C19H18N8O
  1
1
IC50 = 794.33 nM
 Bioactivity Info 
   TI
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CP0447257
 Compound Info 
N-(4-chlorophenyl)tetrazolo[1,5-a]quinoxalin-4-amine
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C14H9ClN6
  1
1
IC50 = 1258.93 nM
 Bioactivity Info 
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CP0447258
 Compound Info 
4-N,4-N-dimethyl-1-N-(tetrazolo[1,5-a]quinoxalin-4-yl)benzene-1,4-diamine
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C16H15N7
  1
1
IC50 = 1258.93 nM
 Bioactivity Info 
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CP0565590
 Compound Info 
N-(4-methylphenyl)tetrazolo[1,5-a]quinoxalin-4-amine
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C15H12N6
  1
1
IC50 = 1258.93 nM
 Bioactivity Info 
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CP0425188
 Compound Info 
MLS000686692
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C14H10N6
  1
1
IC50 = 1995.26 nM
 Bioactivity Info 
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CP0492104
 Compound Info 
N-(4-fluorophenyl)tetrazolo[1,5-a]quinoxalin-4-amine
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C14H9FN6
  1
1
IC50 = 3981.07 nM
 Bioactivity Info 
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CP0432543
 Compound Info 
cyclopropyl-[4-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)benzoyl]piperazin-1-yl]methanone
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C23H22N8O2
  1
1
IC50 = 5011.87 nM
 Bioactivity Info 
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CP0358921
 Compound Info 
N-(3-methylphenyl)tetrazolo[1,5-a]quinoxalin-4-amine
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C15H12N6
  1
1
IC50 > 10000 nM
 Bioactivity Info 
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CP0393904
 Compound Info 
N-(3-propan-2-ylphenyl)tetrazolo[1,5-a]quinoxalin-4-amine
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C17H16N6
  1
1
IC50 > 10000 nM
 Bioactivity Info 
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CP0447058
 Compound Info 
morpholin-4-yl-[3-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]methanone
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C19H17N7O2
  1
1
IC50 > 10000 nM
 Bioactivity Info 
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CP0454434
 Compound Info 
[3-fluoro-4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]-morpholin-4-ylmethanone
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C19H16FN7O2
  1
1
IC50 > 10000 nM
 Bioactivity Info 
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CP0458578
 Compound Info 
N-(2-methylphenyl)tetrazolo[1,5-a]quinoxalin-4-amine
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C15H12N6
  1
1
IC50 > 10000 nM
 Bioactivity Info 
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CP0458580
 Compound Info 
4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)benzoic acid
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C15H10N6O2
  1
1
IC50 > 10000 nM
 Bioactivity Info 
   TI
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Cell Line ID: CL000012 , Sf21
 Cell Line Info 
Cell Line ID: CL000013 , Sf9
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0053018
 Compound Info 
2-(4-(Trifluoromethyl)phenyl)-7,8-dihydro-5H-thiopyrano-[4,3-d]pyrimidin-4-ol
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C14H11F3N2OS
  9
1 IC50 = 1.9 nM
2 IC50 = 10 nM
3 IC50 = 11 nM
4 IC50 = 11.1 nM
5 IC50 = 13 nM
6 IC50 = 15 nM
7 IC50 = 17 nM
8 IC50 = 68 nM
9 Kd = 100 nM
CP0251373
 Compound Info 
2-(4-tert-butylphenyl)-3H-quinazolin-4-one
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C18H18N2O
  1
1 IC50 = 5 nM
CP0154599
 Compound Info 
(4-pyrimidin-2-ylpiperazin-1-yl)-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]methanone
   Show/Hide
C23H20N10O
  1
1 IC50 = 15.85 nM
CP0154554
 Compound Info 
[4-(1-methylimidazole-4-carbonyl)piperazin-1-yl]-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]methanone
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C24H22N10O2
  1
1 IC50 = 31.62 nM
CP0092236
 Compound Info 
2-Phenyl-3H-quinazolin-4-one
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C14H10N2O
  2
1 IC50 = 59 nM
2 IC50 = 1406 nM
CP0040799
 Compound Info 
2-(4-Methoxy-phenyl)-quinazolin-4-ol
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C15H12N2O2
  2
1 IC50 = 67 nM
2 IC50 = 250 nM
CP0120515
 Compound Info 
4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbonyl]-4-fluorophenyl}methyl)-1,2-dihydrophthalazin-1-one
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C24H23FN4O3
  3
1 IC50 = 1500 nM
2 IC50 = 1568 nM
3 IC50 > 70000 nM
Clinical Information about the Protein
Target 1 ( Tankyrase-1 (TNKS-1) )
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
 Drug Info 
Phase 2
Ovarian cancer
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT01425 Poly [ADP-ribose] polymerase tankyrase-2 Homo sapiens, Human
 Protein Info