Protein Information

General Information of the Protein

Protein ID	PT01138
Protein Name	Thymidine kinase, cytosolic
Gene Name	TK1
Sequence	MSCINLPTVLPGSPSKTRGQIQVILGPMFSGKSTELMRRVRRFQIAQYKCLVIKYAKDTRYSSSFCTHDRNTMEALPACLLRDVAQEALGVAVIGIDEGQFFPDIVEFCEAMANAGKTVIVAALDGTFQRKPFGAILNLVPLAESVVKLTAVCMECFREAAYTKRLGTEKEVEVIGGADKYHSVCRLCYFKKASGQPAGPDNKENCPVPGKPGEAVAARKLFAPQQILQCSPAN Show/Hide
Organism	Homo sapiens, Human
Protein Classification	Enzyme > Transferase
Function	Cell-cycle-regulated enzyme of importance in nucleotide metabolism (PubMed:9575153). Catalyzes the first enzymatic step in the salvage pathway converting thymidine into thymidine monophosphate (PubMed:22385435). Transcriptional regulation limits expression to the S phase of the cell cycle and transient expression coincides with the oscillation in the intracellular dTTP concentration (Probable). Also important for the activation of anticancer and antiviral nucleoside analog prodrugs such as 1-b-d-arabinofuranosylcytosine (AraC) and 3c-azido-3c-deoxythymidine (AZT) (PubMed:22385435). Show/Hide
Uniprot ID	Primary ID: P04183 Secondarily ID: B2RC58 Q969V0 Q9UMG9 Show/Hide
Ensembl ID	ENSG00000167900
HGNC ID	HGNC:11830
Subcellular Location	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: CL000057 , Vero

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0172903 Compound Info	FIALURIDINE Show/Hide	C9H10FIN2O5	1
1	Km = 53000 nM Bioactivity Info	TI LI LO TS
CP0097715 Compound Info	1-[(2R,3S,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-methylpyrimidine-2,4-dione Show/Hide	C10H13FN2O5	1
1	Km = 60000 nM Bioactivity Info	TI LI LO TS
CP0104249 Compound Info	5-ethyl-1-[(2R,3S,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidine-2,4-dione Show/Hide	C11H15FN2O5	1
1	Km = 3154700 nM Bioactivity Info	TI LI LO TS
CP0689145 Compound Info	2-Amino-9-(2-hydroxy-ethoxymethyl)-5,9-dihydro-purin-6-one (ACV) Show/Hide	C8H11N5O3	1
1	Km > 4920000 nM Bioactivity Info	TI LI LO TS

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0041607 Compound Info	(AZT) 1-(4-Azido-5-hydroxymethyl-tetrahydro-furan-2-yl)-5-methyl-1H-pyrimidine-2,4-dione Show/Hide	C10H13N5O4	4
1	IC50 = 3000 nM
2	Ki = 2900 nM
3	Ki = 7000 nM
4	Km = 3500 nM
CP0104249 Compound Info	5-ethyl-1-[(2R,3S,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidine-2,4-dione Show/Hide	C11H15FN2O5	2
1	Ki = 90 nM
2	Ki = 440 nM
CP0172903 Compound Info	FIALURIDINE Show/Hide	C9H10FIN2O5	2
1	Ki = 140 nM
2	Ki = 950 nM
CP0097715 Compound Info	1-[(2R,3S,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-methylpyrimidine-2,4-dione Show/Hide	C10H13FN2O5	2
1	Ki = 180 nM
2	Ki = 1400 nM
CP0049058 Compound Info	dT Show/Hide	C10H14N2O5	10
1	Ki = 200 nM
2	Ki = 2000 nM
3	Km = 290 nM
4	Km = 660 nM
5	Km = 1000 nM
6	Km = 1800 nM
7	Km = 2800 nM
8	Km = 3000 nM
9	Km = 4000 nM
10	Km = 49000 nM
CP0689145 Compound Info	2-Amino-9-(2-hydroxy-ethoxymethyl)-5,9-dihydro-purin-6-one (ACV) Show/Hide	C8H11N5O3	1
1	Ki = 45000 nM
CP0077024 Compound Info	2-Amino-9-(2-hydroxy-ethoxymethyl)-5,9-dihydro-purin-6-one Show/Hide	C8H11N5O3	1
1	Km = 1500 nM
CP0736210 Compound Info	SID124893542 Show/Hide	C8H11N5O3	1
1	Km = 12800 nM

Clinical Information about the Protein

Target 1 ( Thymidine kinase 1 (TK1) )

Target Type	Successful Target
Disease	4 Target-related Diseases				4
1	Acute myeloid leukaemia [ICD-11: 2A60]
2	Human immunodeficiency virus infection [ICD-11: 1C62]
3	Pancreatic cancer [ICD-11: 2C10]
4	Cardiovascular disease [ICD-11: BA00-BE2Z]
Approved Drug(s)	2 Approved Drugs				2
1	DEOXYCYTIDINE	Drug Info	Approved	Acute myeloid leukaemia
2	Penciclovir	Drug Info	Approved	Human immunodeficiency virus infection
Clinical Trial Drug(s)	2 Clinical Trial Drugs				2
1	RP101	Drug Info	Phase 2/3	Pancreatic cancer
2	Rilapladib	Drug Info	Phase 1	Cardiovascular disease