General Information of the Protein
Protein ID
PT01010
Protein Name
Thymidylate synthase
Gene Name
TYMS
Secondarily
Gene Name
TS
OK/SW-cl.29
Sequence
MPVAGSELPRRPLPPAAQERDAEPRPPHGELQYLGQIQHILRCGVRKDDRTGTGTLSVFGMQARYSLRDEFPLLTTKRVFWKGVLEELLWFIKGSTNAKELSSKGVKIWDANGSRDFLDSLGFSTREEGDLGPVYGFQWRHFGAEYRDMESDYSGQGVDQLQRVIDTIKTNPDDRRIIMCAWNPRDLPLMALPPCHALCQFYVVNSELSCQLYQRSGDMGLGVPFNIASYALLTYMIAHITGLKPGDFIHTLGDAHIYLNHIEPLKIQLQREPRPFPKLRILRKVEKIDDFKAEDFQIEGYNPHPTIKMEMAV
    Show/Hide
Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Transferase
Function
Catalyzes the reductive methylation of 2'-deoxyuridine 5'-monophosphate (dUMP) to thymidine 5'-monophosphate (dTMP), using the cosubstrate, 5,10- methylenetetrahydrofolate (CH2H4folate) as a 1-carbon donor and reductant and contributes to the de novo mitochondrial thymidylate biosynthesis pathway.
    Show/Hide
Uniprot ID
Primary ID:
P04818

Secondarily ID:
Q8WYK3
Q8WYK4
    Show/Hide
Ensembl ID
ENSG00000176890
HGNC ID
HGNC:12441
Subcellular Location
Nucleus
Cytoplasm
Mitochondrion
Mitochondrion matrix
Mitochondrion inner membrane
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: CL000768 , AML-1
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0046656
 Compound Info 
(2S)-2-[(4-{[(2-amino-4-oxo-1,4-dihydroquinazolin-6-yl)methyl](prop-2-yn-1-yl)amino}phenyl)formamido]pentanedioic acid
   Show/Hide
C24H23N5O6
  1
1
Ki = 7 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0401470
 Compound Info 
2-{4-[(2-Amino-4-oxo-1,4-dihydro-pteridin-6-ylmethyl)-methyl-amino]-benzoylamino}-pentanedioic acid(10-methylfolate)
   Show/Hide
C20H21N7O6
  1
1
Ki = 1000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0068879
 Compound Info 
(2S)-2-[[4-[(2-amino-4-oxo-1H-pteridin-6-yl)methylamino]benzoyl]amino]pentanedioic acid
   Show/Hide
C19H19N7O6
  1
1
Ki = 40000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000017 , HeLa
 Cell Line Info 
Cell Line ID: CL000002 , K-562
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0046656
 Compound Info 
(2S)-2-[(4-{[(2-amino-4-oxo-1,4-dihydroquinazolin-6-yl)methyl](prop-2-yn-1-yl)amino}phenyl)formamido]pentanedioic acid
   Show/Hide
C24H23N5O6
  11
1 IC50 = 19.95 nM
2 IC50 = 20 nM
3 IC50 = 36 nM
4 IC50 = 64 nM
5 IC50 = 72 nM
6 IC50 = 85 nM
7 IC50 = 150 nM
8 IC50 = 180 nM
9 IC50 = 1500 nM
10 IC50 = 5000 nM
11 Ki = 30 nM
Clinical Information about the Protein
Target 1 ( Thymidylate synthase messenger RNA (TYMS mRNA) )
Target Type Successful Target
Disease 1 Target-related Disease  1
1 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Approved Drug(s) 1 Approved Drug  1
1 Fluorouracil
 Drug Info 
Approved
Solid tumour/cancer
Target 2 ( Thymidylate synthase (TYMS) )
Target Type Clinical trial Target