General Information of the Protein
Protein ID
PT02382
Protein Name
Tyrosyl-DNA phosphodiesterase 1
Gene Name
TDP1
Sequence
MSQEGDYGRWTISSSDESEEEKPKPDKPSTSSLLCARQGAANEPRYTCSEAQKAAHKRKISPVKFSNTDSVLPPKRQKSGSQEDLGWCLSSSDDELQPEMPQKQAEKVVIKKEKDISAPNDGTAQRTENHGAPACHRLKEEEDEYETSGEGQDIWDMLDKGNPFQFYLTRVSGVKPKYNSGALHIKDILSPLFGTLVSSAQFNYCFDVDWLVKQYPPEFRKKPILLVHGDKREAKAHLHAQAKPYENISLCQAKLDIAFGTHHTKMMLLLYEEGLRVVIHTSNLIHADWHQKTQGIWLSPLYPRIADGTHKSGESPTHFKADLISYLMAYNAPSLKEWIDVIHKHDLSETNVYLIGSTPGRFQGSQKDNWGHFRLKKLLKDHASSMPNAESWPVVGQFSSVGSLGADESKWLCSEFKESMLTLGKESKTPGKSSVPLYLIYPSVENVRTSLEGYPAGGSLPYSIQTAEKQNWLHSYFHKWSAETSGRSNAMPHIKTYMRPSPDFSKIAWFLVTSANLSKAAWGALEKNGTQLMIRSYELGVLFLPSAFGLDSFKVKQKFFAGSQEPMATFPVPYDLPPELYGSKDRPWIWNIPYVKAPDTHGNMWVPS
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Phosphodiesterase
Function
DNA repair enzyme that can remove a variety of covalent adducts from DNA through hydrolysis of a 3'-phosphodiester bond, giving rise to DNA with a free 3' phosphate. Catalyzes the hydrolysis of dead-end complexes between DNA and the topoisomerase I active site tyrosine residue. Hydrolyzes 3'-phosphoglycolates on protruding 3' ends on DNA double-strand breaks due to DNA damage by radiation and free radicals. Acts on blunt-ended double-strand DNA breaks and on single-stranded DNA. Has low 3'exonuclease activity and can remove a single nucleoside from the 3'end of DNA and RNA molecules with 3'hydroxyl groups. Has no exonuclease activity towards DNA or RNA with a 3'phosphate.
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Uniprot ID
Primary ID:
Q9NUW8

Secondarily ID:
Q2HXX4
Q86TV8
Q96BK7
Q9NZM7
Q9NZM8
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Ensembl ID
ENSG00000042088
HGNC ID
HGNC:18884
Subcellular Location
Nucleus
Cytoplasm
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: CL000302 , DT40
Compound ID Compound Name Compound Formula
CP0769721
Sodium(Z)-4-((2-Oxo-4-thioxothiazolidin-5-ylidene)methyl)-benzoate
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C11H6NNaO3S2
 1
1
IC50 = 6900 nM
   TI
   LI
   LO
   TS
CP0774617
(Z)-4-((2-Oxo-4-thioxothiazolidin-5-ylidene)methyl)benzoic Acid
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C11H7NO3S2
 1
1
IC50 = 11000 nM
   TI
   LI
   LO
   TS
CP0667047
(Z)-4-Thioxo-5-(2,3,4-trihydroxybenzylidene)thiazolidin-2-one
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C10H7NO4S2
 1
1
IC50 = 35000 nM
   TI
   LI
   LO
   TS
CP0727807
(Z)-Methyl 4-((2-oxo-4-thioxothiazolidin-5-ylidene)methyl)-benzoate
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C12H9NO3S2
 1
1
IC50 = 38000 nM
   TI
   LI
   LO
   TS
CP0759833
(Z)-5-(3,4-Dihydroxybenzylidene)-4-thioxothiazolidin-2-one
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C10H7NO3S2
 1
1
IC50 = 41000 nM
   TI
   LI
   LO
   TS
CP0769720
(Z)-(4-((2-Oxo-4-thioxothiazolidin-5-ylidene)methyl)phenyl)-phosphonic Acid
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C10H8NO4PS2
 1
1
IC50 = 69000 nM
   TI
   LI
   LO
   TS
CP0658653
(Z)-5-(2,5-Dihydroxybenzylidene)-4-thioxothiazolidin-2-one
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C10H7NO3S2
 1
1
IC50 = 76000 nM
   TI
   LI
   LO
   TS
CP0769722
(Z)-5-(2,4-Dihydroxybenzylidene)-4-thioxothiazolidin-2-one
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C10H7NO3S2
 1
1
IC50 = 76000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0667047
(Z)-4-Thioxo-5-(2,3,4-trihydroxybenzylidene)thiazolidin-2-one
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C10H7NO4S2
 2
1 IC50 = 870 nM
2 IC50 = 2800 nM
CP0769720
(Z)-(4-((2-Oxo-4-thioxothiazolidin-5-ylidene)methyl)phenyl)-phosphonic Acid
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C10H8NO4PS2
 1
1 IC50 = 2200 nM
CP0759833
(Z)-5-(3,4-Dihydroxybenzylidene)-4-thioxothiazolidin-2-one
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C10H7NO3S2
 1
1 IC50 = 2600 nM
CP0769722
(Z)-5-(2,4-Dihydroxybenzylidene)-4-thioxothiazolidin-2-one
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C10H7NO3S2
 1
1 IC50 = 4100 nM
CP0727807
(Z)-Methyl 4-((2-oxo-4-thioxothiazolidin-5-ylidene)methyl)-benzoate
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C12H9NO3S2
 1
1 IC50 = 6700 nM
CP0658653
(Z)-5-(2,5-Dihydroxybenzylidene)-4-thioxothiazolidin-2-one
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C10H7NO3S2
 1
1 IC50 = 7100 nM
CP0769721
Sodium(Z)-4-((2-Oxo-4-thioxothiazolidin-5-ylidene)methyl)-benzoate
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C11H6NNaO3S2
 1
1 IC50 = 7800 nM
CP0774617
(Z)-4-((2-Oxo-4-thioxothiazolidin-5-ylidene)methyl)benzoic Acid
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C11H7NO3S2
 1
1 IC50 = 16000 nM
Clinical Information about the Protein
Target 1 ( Tyrosyl-DNA phosphodiesterase 1 (TDP1) )
Target Type Patented-recorded Target