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Literature summary extracted from

  • Voss, M.D.; Czechtizky, W.; Li, Z.; Rudolph, C.; Petry, S.; Brummerhop, H.; Langer, T.; Schiffer, A.; Schaefer, H.L.
    Discovery and pharmacological characterization of a novel small molecule inhibitor of phosphatidylinositol-5-phosphate 4-kinase, type II, beta (2014), Biochem. Biophys. Res. Commun., 449, 327-331.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.7.1.149 expressed in Escherichia coli BL21(DE3/pLysS) cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.1.149 2,4-diamino-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
 Homo sapiens
2.7.1.149 3-(trifluoromethyl)phenyl 4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)pyrimidine-5-carboxylate
-
 Homo sapiens
2.7.1.149 4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)-N-(3-phenoxyphenyl)pyrimidine-5-carboxamide
-
 Homo sapiens
2.7.1.149 4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)-N-methyl-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
 Homo sapiens
2.7.1.149 4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)-N-[3-(2,2,2-trifluoroethoxy)phenyl]pyrimidine-5-carboxamide
-
 Homo sapiens
2.7.1.149 4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)-N-[4-methyl-3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
 Homo sapiens
2.7.1.149 4-amino-2-(benzylamino)-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
 Homo sapiens
2.7.1.149 4-amino-2-(dimethylamino)-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
 Homo sapiens
2.7.1.149 4-amino-2-(methylsulfanyl)-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
 Homo sapiens
2.7.1.149 4-amino-2-(piperidin-1-yl)-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
 Homo sapiens
2.7.1.149 4-amino-2-hydroxy-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
 Homo sapiens
2.7.1.149 4-amino-2-methoxy-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
 Homo sapiens
2.7.1.149 4-amino-2-[(2,2-dimethylpropyl)amino]-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
 Homo sapiens
2.7.1.149 4-amino-2-[(tert-butylcarbamoyl)amino]-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
 Homo sapiens
2.7.1.149 4-amino-2-[[(1-methyl-1H-pyrazol-5-yl)methyl]amino]-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
 Homo sapiens
2.7.1.149 4-amino-N-(1,3-benzothiazol-5-yl)-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)pyrimidine-5-carboxamide
-
 Homo sapiens
2.7.1.149 4-amino-N-(1-benzothiophen-5-yl)-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)pyrimidine-5-carboxamide
-
 Homo sapiens
2.7.1.149 4-amino-N-[3-(trifluoromethyl)phenyl]-2-(3,4,4-trimethyl-2-oxoimidazolidin-1-yl)pyrimidine-5-carboxamide
-
 Homo sapiens
2.7.1.149 4-amino-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
 Homo sapiens
2.7.1.149 SAR088
-
 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 P78356
-
-

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 phosphatidylinositol-5-phosphate 4-kinase, type II, beta isoform Homo sapiens
2.7.1.149 PIP5K2B
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.1.149 0.0038
-
 at pH 7.4 and 26°C Homo sapiens SAR088
2.7.1.149 0.0041
-
 at pH 7.4 and 26°C Homo sapiens 4-amino-2-[[(1-methyl-1H-pyrazol-5-yl)methyl]amino]-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
2.7.1.149 0.0054
-
 at pH 7.4 and 26°C Homo sapiens 4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)-N-(3-phenoxyphenyl)pyrimidine-5-carboxamide
2.7.1.149 0.008
-
 at pH 7.4 and 26°C Homo sapiens 4-amino-2-[(2,2-dimethylpropyl)amino]-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
2.7.1.149 0.0081
-
 at pH 7.4 and 26°C Homo sapiens 4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)-N-[3-(2,2,2-trifluoroethoxy)phenyl]pyrimidine-5-carboxamide
2.7.1.149 0.013
-
 at pH 7.4 and 26°C Homo sapiens 4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)-N-[4-methyl-3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
2.7.1.149 0.013
-
 at pH 7.4 and 26°C Homo sapiens 4-amino-N-(1-benzothiophen-5-yl)-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)pyrimidine-5-carboxamide
2.7.1.149 0.025
-
 at pH 7.4 and 26°C Homo sapiens 4-amino-N-(1,3-benzothiazol-5-yl)-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)pyrimidine-5-carboxamide
2.7.1.149 0.025
-
 at pH 7.4 and 26°C Homo sapiens 4-amino-2-(benzylamino)-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
2.7.1.149 0.03
-
 IC50 above 0.03 mM, at pH 7.4 and 26°C Homo sapiens 3-(trifluoromethyl)phenyl 4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)pyrimidine-5-carboxylate
2.7.1.149 0.03
-
 IC50 above 0.03 mM, at pH 7.4 and 26°C Homo sapiens 4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)-N-methyl-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
2.7.1.149 0.03
-
 IC50 above 0.03 mM, at pH 7.4 and 26°C Homo sapiens 2,4-diamino-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
2.7.1.149 0.03
-
 IC50 above 0.03 mM, at pH 7.4 and 26°C Homo sapiens 4-amino-2-(dimethylamino)-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
2.7.1.149 0.03
-
 IC50 above 0.03 mM, at pH 7.4 and 26°C Homo sapiens 4-amino-2-[(tert-butylcarbamoyl)amino]-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
2.7.1.149 0.03
-
 IC50 above 0.03 mM, at pH 7.4 and 26°C Homo sapiens 4-amino-N-[3-(trifluoromethyl)phenyl]-2-(3,4,4-trimethyl-2-oxoimidazolidin-1-yl)pyrimidine-5-carboxamide
2.7.1.149 0.03
-
 IC50 above 0.03 mM, at pH 7.4 and 26°C Homo sapiens 4-amino-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
2.7.1.149 0.03
-
 IC50 above 0.03 mM, at pH 7.4 and 26°C Homo sapiens 4-amino-2-hydroxy-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
2.7.1.149 0.03
-
 IC50 above 0.03 mM, at pH 7.4 and 26°C Homo sapiens 4-amino-2-methoxy-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
2.7.1.149 0.03
-
 IC50 above 0.03 mM, at pH 7.4 and 26°C Homo sapiens 4-amino-2-(piperidin-1-yl)-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
2.7.1.149 0.03
-
 IC50 above 0.03 mM, at pH 7.4 and 26°C Homo sapiens 4-amino-2-(methylsulfanyl)-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide

General Information

EC Number General Information Comment Organism
2.7.1.149 physiological function the enzyme isoform PIP5K2B is linked to the pathogenesis of obesity, insulin resistance and diabetes Homo sapiens