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Literature summary extracted from

  • Jessop, T.C.; Tarver, J.E.; Carlsen, M.; Xu, A.; Healy, J.P.; Heim-Riether, A.; Fu, Q.; Taylor, J.A.; Augeri, D.J.; Shen, M.; Stouch, T.R.; Swanson, R.V.; Tari, L.W.; Hunter, M.; Hoffman, I.; Keyes, P.E.; Yu, X.C.; Miranda, M.; Liu, Q.; Swaffield, J.C.; David Kimball, S.; Nouraldeen, A.; Wilson, A.G.; Foushee, A.M.
    Lead optimization and structure-based design of potent and bioavailable deoxycytidine kinase inhibitors (2009), Bioorg. Med. Chem. Lett., 19, 6784-6787.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.1.74 3'-[[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]sulfamoyl]biphenyl-4-carboxamide
-
 Homo sapiens
2.7.1.74 4-(1-benzothiophen-2-yl)-6-[4-(2-oxo-2-pyrrolidin-1-ylethyl)piperazin-1-yl]pyrimidine
-
 Homo sapiens
2.7.1.74 5-Fluoro-2'-deoxycytidine competitive inhibitor Homo sapiens
2.7.1.74 N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]-2',4'-dichlorobiphenyl-3-sulfonamide
-
 Homo sapiens
2.7.1.74 N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]-2'-chlorobiphenyl-3-sulfonamide
-
 Homo sapiens
2.7.1.74 N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]-3'-chlorobiphenyl-3-carboxamide
-
 Homo sapiens
2.7.1.74 N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]-3'-chlorobiphenyl-3-sulfonamide
-
 Homo sapiens
2.7.1.74 N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]-3-bromobenzenesulfonamide
-
 Homo sapiens
2.7.1.74 N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]-4''-chloro-2''-methyl-1,1':4',1''-terphenyl-3-carboxamide
-
 Homo sapiens
2.7.1.74 N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]-4''-chloro-2''-methyl-1,1':4',1''-terphenyl-3-sulfonamide
-
 Homo sapiens
2.7.1.74 N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]-4'-(methylsulfonyl)biphenyl-3-sulfonamide
-
 Homo sapiens
2.7.1.74 N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]-4'-chlorobiphenyl-3-sulfonamide
-
 Homo sapiens
2.7.1.74 N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]-4'-cyanobiphenyl-3-sulfonamide
-
 Homo sapiens
2.7.1.74 N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]-4'-formylbiphenyl-3-sulfonamide
-
 Homo sapiens
2.7.1.74 N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]-4'-methoxybiphenyl-3-carboxamide
-
 Homo sapiens
2.7.1.74 N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]-4'-methoxybiphenyl-3-sulfonamide
-
 Homo sapiens
2.7.1.74 N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]-4'-methylbiphenyl-3-sulfonamide
-
 Homo sapiens
2.7.1.74 N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]-4-(1-benzothiophen-2-yl)pyridine-2-carboxamide potent, selective, and orally bioavailable inhibitor of dCK Homo sapiens
2.7.1.74 N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]-4-bromobenzenesulfonamide
-
 Homo sapiens
2.7.1.74 N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]-4-nitrobenzenesulfonamide
-
 Homo sapiens
2.7.1.74 N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]benzenesulfonamide
-
 Homo sapiens
2.7.1.74 N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]biphenyl-3-carboxamide
-
 Homo sapiens
2.7.1.74 N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]biphenyl-3-sulfonamide
-
 Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
2.7.1.74 Homo sapiens P27707
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.1.74 ATP + 2'-deoxycytidine
-
 Homo sapiens ADP + 2'-deoxycytidine 5'-phosphate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.1.74 dCK
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.1.74 ATP
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.1.74 0.0000017
-
-
 Homo sapiens N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]-4-(1-benzothiophen-2-yl)pyridine-2-carboxamide
2.7.1.74 0.000021
-
-
 Homo sapiens N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]-2',4'-dichlorobiphenyl-3-sulfonamide
2.7.1.74 0.000021
-
-
 Homo sapiens N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]-4''-chloro-2''-methyl-1,1':4',1''-terphenyl-3-sulfonamide
2.7.1.74 0.000021
-
-
 Homo sapiens N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]-4''-chloro-2''-methyl-1,1':4',1''-terphenyl-3-carboxamide
2.7.1.74 0.000023
-
-
 Homo sapiens N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]-3'-chlorobiphenyl-3-carboxamide
2.7.1.74 0.00003
-
-
 Homo sapiens N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]-4'-methoxybiphenyl-3-carboxamide
2.7.1.74 0.000042
-
-
 Homo sapiens N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]-4'-methoxybiphenyl-3-carboxamide
2.7.1.74 0.000045
-
-
 Homo sapiens N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]-2'-chlorobiphenyl-3-sulfonamide
2.7.1.74 0.000049
-
-
 Homo sapiens N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]-4'-cyanobiphenyl-3-sulfonamide
2.7.1.74 0.000051
-
-
 Homo sapiens N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]-4'-chlorobiphenyl-3-sulfonamide
2.7.1.74 0.000063
-
-
 Homo sapiens N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]-4'-(methylsulfonyl)biphenyl-3-sulfonamide
2.7.1.74 0.000064
-
-
 Homo sapiens N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]-4'-methoxybiphenyl-3-sulfonamide
2.7.1.74 0.000079
-
-
 Homo sapiens N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]-3'-chlorobiphenyl-3-sulfonamide
2.7.1.74 0.000089
-
-
 Homo sapiens 3'-[[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]sulfamoyl]biphenyl-4-carboxamide
2.7.1.74 0.00011
-
-
 Homo sapiens N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]-4'-methylbiphenyl-3-sulfonamide
2.7.1.74 0.00012
-
-
 Homo sapiens 5-Fluoro-2'-deoxycytidine
2.7.1.74 0.00012
-
-
 Homo sapiens N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]biphenyl-3-sulfonamide
2.7.1.74 0.00026
-
-
 Homo sapiens N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]biphenyl-3-carboxamide
2.7.1.74 0.00035
-
-
 Homo sapiens N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]-3-bromobenzenesulfonamide
2.7.1.74 0.00051
-
-
 Homo sapiens 4-(1-benzothiophen-2-yl)-6-[4-(2-oxo-2-pyrrolidin-1-ylethyl)piperazin-1-yl]pyrimidine
2.7.1.74 0.0019
-
-
 Homo sapiens N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]-3-bromobenzenesulfonamide
2.7.1.74 0.0027
-
-
 Homo sapiens N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]-4-bromobenzenesulfonamide
2.7.1.74 0.0032
-
-
 Homo sapiens N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]-4-nitrobenzenesulfonamide
2.7.1.74 0.0036
-
-
 Homo sapiens N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]benzenesulfonamide
2.7.1.74 0.0153
-
-
 Homo sapiens N-[(1S,3S)-3-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)cyclopentyl]-4'-formylbiphenyl-3-sulfonamide