General Information of the Protein
Protein ID
PT03510
Protein Name
Oxidized purine nucleoside triphosphate hydrolase
Secondarily
Protein Name
2-hydroxy-dATP diphosphatase
7,8-dihydro-8-oxoguanine triphosphatase
8-oxo-dGTPase
Methylated purine nucleoside triphosphate hydrolase
Nucleoside diphosphate-linked moiety X motif 1
Gene Name
NUDT1
Secondarily
Gene Name
MTH1
Sequence
MGASRLYTLVLVLQPQRVLLGMKKRGFGAGRWNGFGGKVQEGETIEDGARRELQEESGLTVDALHKVGQIVFEFVGEPELMDVHVFCTDSIQGTPVESDEMRPCWFQLDQIPFKDMWPDDSYWFPLLLQKKKFHGYFKFQGQDTILDYTLREVDTV
    Show/Hide
Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Hydrolase
Function
Oxidized purine nucleoside triphosphate hydrolase which is a prominent sanitizer of the oxidized nucleotide pool (PubMed:8226881, PubMed:7713500, PubMed:10608900, PubMed:12857738, PubMed:22556419, PubMed:26238318, PubMed:24695224, PubMed:24695225, PubMed:28679043). Catalyzes the hydrolysis of 2-oxo-dATP (2-hydroxy-dATP) into 2-oxo-dAMP (PubMed:10373420). Has also a significant hydrolase activity toward 2-oxo-ATP, 8-oxo-dGTP and 8-oxo-dATP (PubMed:10373420, PubMed:11139615). Through the hydrolysis of oxidized purine nucleoside triphosphates, prevents their incorporation into DNA and the subsequent transversions A:T to C:G and G:C to T:A (PubMed:8226881, PubMed:10373420, PubMed:10608900, PubMed:11756418, PubMed:12857738, PubMed:16607562, PubMed:24695224, PubMed:24695225, PubMed:26999531, PubMed:28035004). Also catalyzes the hydrolysis of methylated purine nucleoside triphosphate preventing their integration into DNA (PubMed:30304478, PubMed:32144205). Through this antimutagenic activity protects cells from oxidative stress (PubMed:8226881, PubMed:7713500, PubMed:10608900, PubMed:12857738, PubMed:24695224, PubMed:24695225, PubMed:30304478, PubMed:32144205).
    Show/Hide
Uniprot ID
Primary ID:
P36639

Secondarily ID:
A4D205
Q6LES7
Q6P0Y6
Q7Z7N6
Q8IV95
Q9UBM0
Q9UBM9
    Show/Hide
Ensembl ID
ENSG00000106268
HGNC ID
HGNC:8048
Subcellular Location
Cytoplasm
Cytosol
Mitochondrion matrix
Nucleus
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: CL000002 , K-562
Compound ID Compound Name Compound Formula
CP0330041
N-cyclopropyl-4-(2-pyridin-2-ylpyrrolidin-1-yl)-1H-pyrrolo[2,3-b]pyridine-2-carboxamide
   Show/Hide
C20H21N5O
 1
1
EC50 = 1.995 nM
   TI
   LI
   LO
   TS
CP0547521
N-ethyl-4-(2-phenylpyrrolidin-1-yl)-1H-pyrrolo[2,3-b]pyridine-2-carboxamide
   Show/Hide
C20H22N4O
 1
1
EC50 = 1.995 nM
   TI
   LI
   LO
   TS
CP0349171
17-(methylamino)-8,11,14-trioxa-1,16,19,22-tetrazatetracyclo[13.5.2.13,7.018,21]tricosa-3(23),4,6,15,17,21-hexaen-20-one
   Show/Hide
C17H19N5O4
 1
1
EC50 = 3 nM
   TI
   LI
   LO
   TS
CP0229824
4-(4-chloro-2-fluoroanilino)-6,7-dimethoxy-N-methylquinoline-3-carboxamide
   Show/Hide
C19H17ClFN3O3
 1
1
EC50 = 7 nM
   TI
   LI
   LO
   TS
CP0354226
17-(methylamino)-8,14-dioxa-1,16,19,22-tetrazatetracyclo[13.5.2.13,7.018,21]tricosa-3(23),4,6,15,17,21-hexaen-20-one
   Show/Hide
C18H21N5O3
 1
1
EC50 = 9 nM
   TI
   LI
   LO
   TS
CP0390117
N-(oxetan-3-yl)-4-(2-pyridin-2-ylpyrrolidin-1-yl)-1H-pyrrolo[2,3-b]pyridine-2-carboxamide
   Show/Hide
C20H21N5O2
 1
1
EC50 = 10 nM
   TI
   LI
   LO
   TS
CP0274216
4-N-cyclopropyl-6-(2,3-dichlorophenyl)pyrimidine-2,4-diamine
   Show/Hide
C13H12Cl2N4
 2
1
EC50 = 10 nM
   TI
   LI
   LO
   TS
2
EC50 = 125.89 nM
   TI
   LI
   LO
   TS
CP0330038
4-(2-phenylpyrrolidin-1-yl)-1H-pyrrolo[2,3-b]pyridine
   Show/Hide
C17H17N3
 1
1
EC50 = 63.1 nM
   TI
   LI
   LO
   TS
CP0143330
4-[4-[2-(dimethylamino)ethyl]phenyl]quinazolin-2-amine
   Show/Hide
C18H20N4
 1
1
EC50 = 80 nM
   TI
   LI
   LO
   TS
CP0390118
4-(2-pyridin-3-ylpyrrolidin-1-yl)-1H-pyrazolo[3,4-b]pyridine
   Show/Hide
C15H15N5
 1
1
EC50 = 251.19 nM
   TI
   LI
   LO
   TS
CP0229823
4-(4-chloro-2-fluoroanilino)-6,7-dimethoxy-N,N-dimethylquinoline-3-carboxamide
   Show/Hide
C20H19ClFN3O3
 1
1
EC50 = 950 nM
   TI
   LI
   LO
   TS
CP0354227
9-benzyl-2-(2-methoxyethoxy)-6-(methylamino)-7H-purin-8-one
   Show/Hide
C16H19N5O3
 1
1
EC50 = 1500 nM
   TI
   LI
   LO
   TS
CP0229821
3-[(1S)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-(1-piperidin-4-ylpyrazol-4-yl)pyridin-2-amine
   Show/Hide
C21H22Cl2FN5O
 1
1
EC50 = 3600 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0330041
N-cyclopropyl-4-(2-pyridin-2-ylpyrrolidin-1-yl)-1H-pyrrolo[2,3-b]pyridine-2-carboxamide
   Show/Hide
C20H21N5O
 1
1 IC50 < 0.1 nM
CP0390117
N-(oxetan-3-yl)-4-(2-pyridin-2-ylpyrrolidin-1-yl)-1H-pyrrolo[2,3-b]pyridine-2-carboxamide
   Show/Hide
C20H21N5O2
 1
1 IC50 < 0.1 nM
CP0547521
N-ethyl-4-(2-phenylpyrrolidin-1-yl)-1H-pyrrolo[2,3-b]pyridine-2-carboxamide
   Show/Hide
C20H22N4O
 1
1 IC50 < 0.1 nM
CP0354226
17-(methylamino)-8,14-dioxa-1,16,19,22-tetrazatetracyclo[13.5.2.13,7.018,21]tricosa-3(23),4,6,15,17,21-hexaen-20-one
   Show/Hide
C18H21N5O3
 2
1 IC50 = 0.3 nM
2 Kd = 0.2 nM
CP0349171
17-(methylamino)-8,11,14-trioxa-1,16,19,22-tetrazatetracyclo[13.5.2.13,7.018,21]tricosa-3(23),4,6,15,17,21-hexaen-20-one
   Show/Hide
C17H19N5O4
 2
1 IC50 = 0.5 nM
2 Kd = 0.4 nM
CP0229824
4-(4-chloro-2-fluoroanilino)-6,7-dimethoxy-N-methylquinoline-3-carboxamide
   Show/Hide
C19H17ClFN3O3
 2
1 IC50 = 0.9 nM
2 Kd = 0.5 nM
CP0274216
4-N-cyclopropyl-6-(2,3-dichlorophenyl)pyrimidine-2,4-diamine
   Show/Hide
C13H12Cl2N4
 5
1 IC50 = 3 nM
2 IC50 = 5 nM
3 IC50 = 7 nM
4 IC50 = 10 nM
5 Kd = 5 nM
CP0330038
4-(2-phenylpyrrolidin-1-yl)-1H-pyrrolo[2,3-b]pyridine
   Show/Hide
C17H17N3
 1
1 IC50 = 5 nM
CP0143330
4-[4-[2-(dimethylamino)ethyl]phenyl]quinazolin-2-amine
   Show/Hide
C18H20N4
 2
1 IC50 = 9 nM
2 Kd = 3 nM
CP0390118
4-(2-pyridin-3-ylpyrrolidin-1-yl)-1H-pyrazolo[3,4-b]pyridine
   Show/Hide
C15H15N5
 1
1 IC50 = 30 nM
CP0229821
3-[(1S)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-(1-piperidin-4-ylpyrazol-4-yl)pyridin-2-amine
   Show/Hide
C21H22Cl2FN5O
 2
1 IC50 = 138 nM
2 Kd = 39 nM
CP0354227
9-benzyl-2-(2-methoxyethoxy)-6-(methylamino)-7H-purin-8-one
   Show/Hide
C16H19N5O3
 2
1 IC50 = 536 nM
2 Kd = 440 nM
CP0229823
4-(4-chloro-2-fluoroanilino)-6,7-dimethoxy-N,N-dimethylquinoline-3-carboxamide
   Show/Hide
C20H19ClFN3O3
 1
1 IC50 = 1220 nM