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Literature summary extracted from

  • Manz, T.D.; Sivakumaren, S.C.; Ferguson, F.M.; Zhang, T.; Yasgar, A.; Seo, H.S.; Ficarro, S.B.; Card, J.D.; Shim, H.; Miduturu, C.V.; Simeonov, A.; Shen, M.; Marto, J.A.; Dhe-Paganon, S.; Hall, M.D.; Cantley, L.C.; Gray, N.S.
    Discovery and structure-activity relationship study of (Z)-5-methylenethiazolidin-4-one derivatives as potent and selective pan-phosphatidylinositol 5-phosphate 4-kinase inhibitors (2020), J. Med. Chem., 63, 4880-4895 .
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.7.1.149
-
 Homo sapiens

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
2.7.1.149 isoform PI5P4Kalpha in complex with inhibitor CVM-05-002, sitting drop vapor diffusion method, using 2 M NH4 (pH 6.5) Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.1.149 (E)-N-(4-(5-((2,5-dioxopyrrolidin-3-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
-
 Homo sapiens
2.7.1.149 (Z)-1-(4-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)-3-methylurea
-
 Homo sapiens
2.7.1.149 (Z)-2-imino-5-((5-(4-(methylsulfonyl)phenyl)pyridin-3-yl)methylene)thiazolidin-4-one
-
 Homo sapiens
2.7.1.149 (Z)-2-imino-5-((5-(4-(trifluoromethoxy)phenyl)pyridin-3-yl)methylene)thiazolidin-4-one
-
 Homo sapiens
2.7.1.149 (Z)-2-imino-5-((5-(4-(trifluoromethyl)phenyl)pyridin-3-yl)methylene)thiazolidin-4-one
-
 Homo sapiens
2.7.1.149 (Z)-2-imino-5-((5-(4-methoxynaphthalen-1-yl)pyridin-3-yl)methylene)thiazolidin-4-one
-
 Homo sapiens
2.7.1.149 (Z)-4-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)-N-methylbenzenesulfonamide
-
 Homo sapiens
2.7.1.149 (Z)-5-((5-(4-(dimethylamino)phenyl)pyridin-3-yl)methylene)-2-iminothiazolidin-4-one
-
 Homo sapiens
2.7.1.149 (Z)-5-((5-(4-fluorophenyl)pyridin-3-yl)methylene)-2-iminothiazolidin-4-one
-
 Homo sapiens
2.7.1.149 (Z)-N-(3-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)acetamide
-
 Homo sapiens
2.7.1.149 (Z)-N-(4-(2-amino-5-((2-imino-4-oxothiazolidin-5-ylidene)-methyl)pyridin-3-yl)phenyl)methanesulfonamide
-
 Homo sapiens
2.7.1.149 (Z)-N-(4-(5-((2,4-dioxo-oxazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
-
 Homo sapiens
2.7.1.149 (Z)-N-(4-(5-((2,4-dioxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
-
 Homo sapiens
2.7.1.149 (Z)-N-(4-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)acetamide
-
 Homo sapiens
2.7.1.149 (Z)-N-(4-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide i.e. CVM-05-002, potent and selective inhibitor for isoform PI5P4Kalpha Homo sapiens
2.7.1.149 (Z)-N-(4-(6-amino-5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
-
 Homo sapiens
2.7.1.149 N-(3-((5-(4-(methylsulfonamido)phenyl)pyridin-3-yl)amino)phenyl)acetamide
-
 Homo sapiens
2.7.1.149 N-(3-((5-(4-(Mmthylsulfonamido)phenyl)pyridin-3-yl)oxy)phenyl)acetamide
-
 Homo sapiens
2.7.1.149 N-(3-(5-(4-(methylsulfonamido)phenyl)pyridin-3-yl)phenyl)acetamide
-
 Homo sapiens
2.7.1.149 N-(4-(5-(1H-indol-4-yl)pyridin-3-yl)phenyl)methanesulfonamide
-
 Homo sapiens
2.7.1.149 N-(4-(5-(2-oxoindolin-4yl)pyridin-3-yl)phenyl)methanesulfonamide
-
 Homo sapiens
2.7.1.149 N-(4-(5-(4-(3-methylureido)phenyl)pyridin-3-yl)phenyl)methanesulfonamide
-
 Homo sapiens
2.7.1.149 N-(5-(5-(1H-indol-4-yl)pyridin-3-yl)phenyl)methanesulfonamide
-
 Homo sapiens
2.7.1.149 N-(6-(5-(1H-indol-4-yl)pyridin-3-yl)phenyl)methanesulfonamide
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.1.149 ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate Homo sapiens
-
 ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.1.149 Homo sapiens
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.7.1.149
-
 Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.1.149 HEK-293T cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.1.149 ATP + 1-phosphatidyl-1D-myo-inositol 5-phosphate
-
 Homo sapiens ADP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.1.149 pan-phosphatidylinositol 5-phosphate 4-kinase
-
 Homo sapiens
2.7.1.149 pan-PI5P4K
-
 Homo sapiens
2.7.1.149 PI5P4Kalpha isoform Homo sapiens
2.7.1.149 PI5P4Kbeta isoform Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.1.149 0.00013
-
 isoform PI5P4Kalpha, at pH 7.4 and 25°C Homo sapiens (Z)-N-(4-(5-((2,4-dioxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
2.7.1.149 0.00027
-
 isoform PI5P4Kalpha, at pH 7.4 and 25°C Homo sapiens (Z)-N-(4-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
2.7.1.149 0.00066
-
 isoform PI5P4Kalpha, at pH 7.4 and 25°C Homo sapiens (Z)-N-(4-(2-amino-5-((2-imino-4-oxothiazolidin-5-ylidene)-methyl)pyridin-3-yl)phenyl)methanesulfonamide
2.7.1.149 0.0014
-
 isoform PI5P4Kalpha, at pH 7.4 and 25°C Homo sapiens (Z)-4-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)-N-methylbenzenesulfonamide
2.7.1.149 0.0017
-
 isoform PI5P4Kbeta, at pH 7.4 and 25°C Homo sapiens (Z)-N-(4-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
2.7.1.149 0.0018
-
 isoform PI5P4Kalpha, at pH 7.4 and 25°C Homo sapiens (Z)-1-(4-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)-3-methylurea
2.7.1.149 0.0019
-
 isoform PI5P4Kbeta, at pH 7.4 and 25°C Homo sapiens (Z)-N-(4-(5-((2,4-dioxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
2.7.1.149 0.002
-
 isoform PI5P4Kalpha, at pH 7.4 and 25°C Homo sapiens N-(4-(5-(1H-indol-4-yl)pyridin-3-yl)phenyl)methanesulfonamide
2.7.1.149 0.0021
-
 isoform PI5P4Kalpha, at pH 7.4 and 25°C Homo sapiens N-(5-(5-(1H-indol-4-yl)pyridin-3-yl)phenyl)methanesulfonamide
2.7.1.149 0.0027
-
 isoform PI5P4Kbeta, at pH 7.4 and 25°C Homo sapiens (Z)-N-(4-(2-amino-5-((2-imino-4-oxothiazolidin-5-ylidene)-methyl)pyridin-3-yl)phenyl)methanesulfonamide
2.7.1.149 0.0032
-
 isoform PI5P4Kalpha, at pH 7.4 and 25°C Homo sapiens N-(6-(5-(1H-indol-4-yl)pyridin-3-yl)phenyl)methanesulfonamide
2.7.1.149 0.0037
-
 isoform PI5P4Kalpha, at pH 7.4 and 25°C Homo sapiens N-(4-(5-(4-(3-methylureido)phenyl)pyridin-3-yl)phenyl)methanesulfonamide
2.7.1.149 0.0039
-
 isoform PI5P4Kalpha, at pH 7.4 and 25°C Homo sapiens (Z)-2-imino-5-((5-(4-methoxynaphthalen-1-yl)pyridin-3-yl)methylene)thiazolidin-4-one
2.7.1.149 0.004
-
 isoform PI5P4Kalpha, at pH 7.4 and 25°C Homo sapiens (Z)-N-(4-(6-amino-5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
2.7.1.149 0.0043
-
 isoform PI5P4Kbeta, at pH 7.4 and 25°C Homo sapiens (Z)-4-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)-N-methylbenzenesulfonamide
2.7.1.149 0.0053
-
 isoform PI5P4Kalpha, at pH 7.4 and 25°C Homo sapiens N-(3-(5-(4-(methylsulfonamido)phenyl)pyridin-3-yl)phenyl)acetamide
2.7.1.149 0.0061
-
 isoform PI5P4Kalpha, at pH 7.4 and 25°C Homo sapiens (E)-N-(4-(5-((2,5-dioxopyrrolidin-3-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
2.7.1.149 0.0086
-
 isoform PI5P4Kbeta, at pH 7.4 and 25°C Homo sapiens (Z)-1-(4-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)-3-methylurea
2.7.1.149 0.0088
-
 isoform PI5P4Kalpha, at pH 7.4 and 25°C Homo sapiens (Z)-5-((5-(4-(dimethylamino)phenyl)pyridin-3-yl)methylene)-2-iminothiazolidin-4-one
2.7.1.149 0.0089
-
 isoform PI5P4Kalpha, at pH 7.4 and 25°C Homo sapiens N-(4-(5-(2-oxoindolin-4yl)pyridin-3-yl)phenyl)methanesulfonamide
2.7.1.149 0.009
-
 isoform PI5P4Kalpha, at pH 7.4 and 25°C Homo sapiens N-(3-((5-(4-(Mmthylsulfonamido)phenyl)pyridin-3-yl)oxy)phenyl)acetamide
2.7.1.149 0.0094
-
 isoform PI5P4Kbeta, at pH 7.4 and 25°C Homo sapiens N-(4-(5-(1H-indol-4-yl)pyridin-3-yl)phenyl)methanesulfonamide
2.7.1.149 0.011
-
 isoform PI5P4Kalpha, at pH 7.4 and 25°C Homo sapiens (Z)-2-imino-5-((5-(4-(trifluoromethoxy)phenyl)pyridin-3-yl)methylene)thiazolidin-4-one
2.7.1.149 0.011
-
 isoform PI5P4Kalpha, at pH 7.4 and 25°C Homo sapiens (Z)-N-(3-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)acetamide
2.7.1.149 0.011
-
 isoform PI5P4Kalpha, at pH 7.4 and 25°C Homo sapiens (Z)-N-(4-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)acetamide
2.7.1.149 0.014
-
 isoform PI5P4Kalpha, at pH 7.4 and 25°C Homo sapiens N-(3-((5-(4-(methylsulfonamido)phenyl)pyridin-3-yl)amino)phenyl)acetamide
2.7.1.149 0.015
-
 isoform PI5P4Kbeta, at pH 7.4 and 25°C Homo sapiens N-(4-(5-(2-oxoindolin-4yl)pyridin-3-yl)phenyl)methanesulfonamide
2.7.1.149 0.021
-
 isoform PI5P4Kalpha, at pH 7.4 and 25°C Homo sapiens (Z)-N-(4-(5-((2,4-dioxo-oxazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
2.7.1.149 0.022
-
 isoform PI5P4Kbeta, at pH 7.4 and 25°C Homo sapiens N-(5-(5-(1H-indol-4-yl)pyridin-3-yl)phenyl)methanesulfonamide
2.7.1.149 0.025
-
 isoform PI5P4Kbeta, at pH 7.4 and 25°C Homo sapiens (Z)-N-(4-(6-amino-5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
2.7.1.149 0.025
-
 isoform PI5P4Kbeta, at pH 7.4 and 25°C Homo sapiens N-(3-((5-(4-(Mmthylsulfonamido)phenyl)pyridin-3-yl)oxy)phenyl)acetamide
2.7.1.149 0.026
-
 isoform PI5P4Kbeta, at pH 7.4 and 25°C Homo sapiens (Z)-2-imino-5-((5-(4-(trifluoromethyl)phenyl)pyridin-3-yl)methylene)thiazolidin-4-one
2.7.1.149 0.027
-
 isoform PI5P4Kbeta, at pH 7.4 and 25°C Homo sapiens (E)-N-(4-(5-((2,5-dioxopyrrolidin-3-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
2.7.1.149 0.028
-
 isoform PI5P4Kbeta, at pH 7.4 and 25°C Homo sapiens (Z)-5-((5-(4-fluorophenyl)pyridin-3-yl)methylene)-2-iminothiazolidin-4-one
2.7.1.149 0.029
-
 isoform PI5P4Kbeta, at pH 7.4 and 25°C Homo sapiens N-(6-(5-(1H-indol-4-yl)pyridin-3-yl)phenyl)methanesulfonamide
2.7.1.149 0.035
-
 isoform PI5P4Kalpha, at pH 7.4 and 25°C Homo sapiens (Z)-2-imino-5-((5-(4-(methylsulfonyl)phenyl)pyridin-3-yl)methylene)thiazolidin-4-one
2.7.1.149 0.036
-
 isoform PI5P4Kbeta, at pH 7.4 and 25°C Homo sapiens N-(3-(5-(4-(methylsulfonamido)phenyl)pyridin-3-yl)phenyl)acetamide
2.7.1.149 0.043
-
 isoform PI5P4Kbeta, at pH 7.4 and 25°C Homo sapiens N-(4-(5-(4-(3-methylureido)phenyl)pyridin-3-yl)phenyl)methanesulfonamide
2.7.1.149 0.045
-
 isoform PI5P4Kbeta, at pH 7.4 and 25°C Homo sapiens N-(3-((5-(4-(methylsulfonamido)phenyl)pyridin-3-yl)amino)phenyl)acetamide
2.7.1.149 0.05
-
 IC50 above 0.05 mM, isoform PI5P4Kalpha, at pH 7.4 and 25°C Homo sapiens (Z)-2-imino-5-((5-(4-(trifluoromethyl)phenyl)pyridin-3-yl)methylene)thiazolidin-4-one
2.7.1.149 0.05
-
 IC50 above 0.05 mM, isoform PI5P4Kalpha, at pH 7.4 and 25°C Homo sapiens (Z)-5-((5-(4-fluorophenyl)pyridin-3-yl)methylene)-2-iminothiazolidin-4-one
2.7.1.149 0.05
-
 IC50 above 0.05 mM, isoform PI5P4Kbeta, at pH 7.4 and 25°C Homo sapiens (Z)-2-imino-5-((5-(4-(methylsulfonyl)phenyl)pyridin-3-yl)methylene)thiazolidin-4-one
2.7.1.149 0.05
-
 IC50 above 0.05 mM, isoform PI5P4Kbeta, at pH 7.4 and 25°C Homo sapiens (Z)-2-imino-5-((5-(4-(trifluoromethoxy)phenyl)pyridin-3-yl)methylene)thiazolidin-4-one
2.7.1.149 0.05
-
 IC50 above 0.05 mM, isoform PI5P4Kbeta, at pH 7.4 and 25°C Homo sapiens (Z)-2-imino-5-((5-(4-methoxynaphthalen-1-yl)pyridin-3-yl)methylene)thiazolidin-4-one
2.7.1.149 0.05
-
 IC50 above 0.05 mM, isoform PI5P4Kbeta, at pH 7.4 and 25°C Homo sapiens (Z)-5-((5-(4-(dimethylamino)phenyl)pyridin-3-yl)methylene)-2-iminothiazolidin-4-one
2.7.1.149 0.05
-
 IC50 above 0.05 mM, isoform PI5P4Kbeta, at pH 7.4 and 25°C Homo sapiens (Z)-N-(3-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)acetamide
2.7.1.149 0.05
-
 IC50 above 0.05 mM, isoform PI5P4Kbeta, at pH 7.4 and 25°C Homo sapiens (Z)-N-(4-(5-((2,4-dioxo-oxazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)methanesulfonamide
2.7.1.149 0.05
-
 IC50 above 0.05 mM, isoform PI5P4Kbeta, at pH 7.4 and 25°C Homo sapiens (Z)-N-(4-(5-((2-imino-4-oxothiazolidin-5-ylidene)methyl)pyridin-3-yl)phenyl)acetamide