General Information of the Protein
Protein ID
PT01425
Protein Name
Poly [ADP-ribose] polymerase tankyrase-2
Secondarily
Protein Name
ADP-ribosyltransferase diphtheria toxin-like 6
Poly [ADP-ribose] polymerase 5B
Protein poly-ADP-ribosyltransferase tankyrase-2
TNKS-2
TRF1-interacting ankyrin-related ADP-ribose polymerase 2
Tankyrase II
Tankyrase-2
Tankyrase-like protein
Tankyrase-related protein
Gene Name
TNKS2
Secondarily
Gene Name
PARP5B
TANK2
TNKL
Sequence
MSGRRCAGGGAACASAAAEAVEPAARELFEACRNGDVERVKRLVTPEKVNSRDTAGRKSTPLHFAAGFGRKDVVEYLLQNGANVQARDDGGLIPLHNACSFGHAEVVNLLLRHGADPNARDNWNYTPLHEAAIKGKIDVCIVLLQHGAEPTIRNTDGRTALDLADPSAKAVLTGEYKKDELLESARSGNEEKMMALLTPLNVNCHASDGRKSTPLHLAAGYNRVKIVQLLLQHGADVHAKDKGDLVPLHNACSYGHYEVTELLVKHGACVNAMDLWQFTPLHEAASKNRVEVCSLLLSYGADPTLLNCHNKSAIDLAPTPQLKERLAYEFKGHSLLQAAREADVTRIKKHLSLEMVNFKHPQTHETALHCAAASPYPKRKQICELLLRKGANINEKTKEFLTPLHVASEKAHNDVVEVVVKHEAKVNALDNLGQTSLHRAAYCGHLQTCRLLLSYGCDPNIISLQGFTALQMGNENVQQLLQEGISLGNSEADRQLLEAAKAGDVETVKKLCTVQSVNCRDIEGRQSTPLHFAAGYNRVSVVEYLLQHGADVHAKDKGGLVPLHNACSYGHYEVAELLVKHGAVVNVADLWKFTPLHEAAAKGKYEICKLLLQHGADPTKKNRDGNTPLDLVKDGDTDIQDLLRGDAALLDAAKKGCLARVKKLSSPDNVNCRDTQGRHSTPLHLAAGYNNLEVAEYLLQHGADVNAQDKGGLIPLHNAASYGHVDVAALLIKYNACVNATDKWAFTPLHEAAQKGRTQLCALLLAHGADPTLKNQEGQTPLDLVSADDVSALLTAAMPPSALPSCYKPQVLNGVRSPGATADALSSGPSSPSSLSAASSLDNLSGSFSELSSVVSSSGTEGASSLEKKEVPGVDFSITQFVRNLGLEHLMDIFEREQITLDVLVEMGHKELKEIGINAYGHRHKLIKGVERLISGQQGLNPYLTLNTSGSGTILIDLSPDDKEFQSVEEEMQSTVREHRDGGHAGGIFNRYNILKIQKVCNKKLWERYTHRRKEVSEENHNHANERMLFHGSPFVNAIIHKGFDERHAYIGGMFGAGIYFAENSSKSNQYVYGIGGGTGCPVHKDRSCYICHRQLLFCRVTLGKSFLQFSAMKMAHSPPGHHSVTGRPSVNGLALAEYVIYRGEQAYPEYLITYQIMRPEGMVDG
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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:11739745, PubMed:11802774, PubMed:19759537, PubMed:21478859, PubMed:23622245, PubMed:25043379). Acts as an activator of the Wnt signaling pathway by mediating poly-ADP-ribosylation 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 poly-ADP-ribosylation of BLZF1 and CASC3, followed by recruitment of RNF146 and subsequent ubiquitination (PubMed:21478859). Mediates poly-ADP-ribosylation of TERF1, thereby contributing to the regulation of telomere length (PubMed:11739745). Stimulates 26S proteasome activity (PubMed:23622245).
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Uniprot ID
Primary ID:
Q9H2K2

Secondarily ID:
B2RBD3
Q9H8F2
Q9HAS4
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HGNC ID
HGNC:15677
Subcellular Location
Cytoplasm
Golgi apparatus membrane
Nucleus
Chromosome
Telomere
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
Compound ID Compound Name Compound Formula
CP0155059
1-[3-[4-(2-chlorophenyl)-5-pyrimidin-4-yl-1,2,4-triazol-3-yl]cyclobutyl]-2-oxo-3H-benzimidazole-5-carbonitrile
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C24H17ClN8O
 1
1
IC50 = 19 nM
   TI
   LI
   LO
   TS
CP0468769
1-[4-[4-(2-chlorophenyl)-5-pyrimidin-4-yl-1,2,4-triazol-3-yl]cyclohexyl]-2-oxo-3H-benzimidazole-5-carbonitrile
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C26H21ClN8O
 1
1
IC50 = 120 nM
   TI
   LI
   LO
   TS
CP0513932
3-[3-[4-(2-chlorophenyl)-5-pyrimidin-4-yl-1,2,4-triazol-3-yl]cyclobutyl]-1H-benzimidazol-2-one
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C23H18ClN7O
 1
1
IC50 = 200 nM
   TI
   LI
   LO
   TS
CP0273375
3-[4-[4-(2-chlorophenyl)-5-pyrimidin-4-yl-1,2,4-triazol-3-yl]cyclohexyl]-1H-benzimidazol-2-one
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C25H22ClN7O
 1
1
IC50 = 1060 nM
   TI
   LI
   LO
   TS
CP0273376
1-[4-[4-(2-chlorophenyl)-5-pyrimidin-4-yl-1,2,4-triazol-3-yl]phenyl]-2-oxo-3H-benzimidazole-5-carbonitrile
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C26H15ClN8O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0051607
4-[3-(8-methyl-4-oxo-3H-quinazolin-2-yl)propanoylamino]-N-quinolin-8-ylbenzamide
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C28H23N5O3
 1
1 IC50 = 0.1 nM
CP0053018
2-(4-(Trifluoromethyl)phenyl)-7,8-dihydro-5H-thiopyrano-[4,3-d]pyrimidin-4-ol
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C14H11F3N2OS
 9
1 IC50 = 2.1 nM
2 IC50 = 3.6 nM
3 IC50 = 4 nM
4 IC50 = 5 nM
5 IC50 = 5.3 nM
6 IC50 = 9.6 nM
7 IC50 = 15 nM
8 IC50 = 17 nM
9 Kd = 10 nM
CP0120515
4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbonyl]-4-fluorophenyl}methyl)-1,2-dihydrophthalazin-1-one
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C24H23FN4O3
 2
1 IC50 = 5.2 nM
2 IC50 = 4090.5 nM
CP0513932
CHEMBL4074540
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C23H18ClN7O
 1
1 IC50 = 9.8 nM
CP0040805
2-[4-(trifluoromethyl)phenyl]-3H-quinazolin-4-one
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C15H9F3N2O
 1
1 IC50 = 21.5 nM
CP0669064
4-((1S,2S,6R,7R)-3,5-Dioxo-4-aza-tricyclo[5.2.1.0*2,6*]dec-8-en-4-yl)-N-quinolin-8-yl-benzamide
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C25H19N3O3
 1
1 IC50 = 29.2 nM
CP0040799
2-(4-Methoxy-phenyl)-quinazolin-4-ol
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C15H12N2O2
 1
1 IC50 = 52 nM
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 = 56 nM
CP0057061
2-[4-(aminomethyl)phenyl]-8-methyl-3H-quinazolin-4-one;hydrobromide
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C16H15N3O
 1
1 IC50 = 100 nM
CP0054324
2-Ethylquinazolin-4(3H)-one
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C14H9ClN2O
 1
1 IC50 = 200 nM
CP0468769
CHEMBL4102763
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C26H21ClN8O
 1
1 IC50 = 330 nM
CP0273376
1-[4-[4-(2-chlorophenyl)-5-pyrimidin-4-yl-1,2,4-triazol-3-yl]phenyl]-2-oxo-3H-benzimidazole-5-carbonitrile
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C26H15ClN8O
 1
1 IC50 = 340 nM
CP0273375
CHEMBL4084811
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C25H22ClN7O
 1
1 IC50 = 430 nM
Clinical Information about the Protein
Target 1 ( Tankyrase-2 (TNKS-2) )
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
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT02202 Poly [ADP-ribose] polymerase tankyrase-1 Homo sapiens, Human