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Literature summary extracted from

  • Manz, T.D.; Sivakumaren, S.C.; Yasgar, A.; Hall, M.D.; Davis, M.I.; Seo, H.S.; Card, J.D.; Ficarro, S.B.; Shim, H.; Marto, J.A.; Dhe-Paganon, S.; Sasaki, A.T.; Boxer, M.B.; Simeonov, A.; Cantley, L.C.; Shen, M.; Zhang, T.; Ferguson, F.M.; Gray, N.S.
    Structure-activity relationship study of covalent pan-phosphatidylinositol 5-phosphate 4-kinase inhibitors (2020), ACS Med. Chem. Lett., 11, 346-352 .
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.1.149 (2E)-4-(dimethylamino)-N-[1-[(3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)acetyl]piperidin-4-yl]but-2-enamide
-
 Homo sapiens
2.7.1.149 (2Z)-2-(1H-indol-3-yl)-3-(isoquinolin-5-yl)prop-2-enenitrile
-
 Homo sapiens
2.7.1.149 3-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)benzamide
-
 Homo sapiens
2.7.1.149 4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
-
 Homo sapiens
2.7.1.149 4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)benzamide
-
 Homo sapiens
2.7.1.149 4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)cyclohexane-1-carboxamide
-
 Homo sapiens
2.7.1.149 4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(2-methyl-2H-benzimidazol-5-yl)pyrimidin-4-yl]amino]phenyl)benzamide
-
 Homo sapiens
2.7.1.149 4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(4-methylanilino)pyrimidin-4-yl]amino]phenyl)benzamide
-
 Homo sapiens
2.7.1.149 4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[7-(4-methylphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]phenyl)benzamide
-
 Homo sapiens
2.7.1.149 4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(4-methyl-3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)benzamide
-
 Homo sapiens
2.7.1.149 4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(5-[[6-(1H-indol-3-yl)pyrimidin-4-yl]amino]-2-methylphenyl)benzamide
-
 Homo sapiens
2.7.1.149 4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-[(3-[[6-(1H-indol-3-yl)pyrimidin-4-yl]amino]phenyl)methyl]benzamide
-
 Homo sapiens
2.7.1.149 5-[3-(methylsulfonyl)phenyl]-4-[(1-methyl-1H-tetrazol-5-yl)sulfanyl]thieno[2,3-d]pyrimidine
-
 Homo sapiens
2.7.1.149 N-(3-[[6-([1,1'-biphenyl]-3-yl)pyrimidin-4-yl]amino]phenyl)-4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]benzamide
-
 Homo sapiens
2.7.1.149 N-[3-([6-[([1,1'-biphenyl]-3-yl)amino]pyrimidin-4-yl]amino)phenyl]-4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]benzamide
-
 Homo sapiens
2.7.1.149 N-[3-([6-[([1,1'-biphenyl]-4-yl)amino]pyrimidin-4-yl]amino)phenyl]-4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]benzamide
-
 Homo sapiens
2.7.1.149 NIH-12848
-
 Homo sapiens
2.7.1.149 THZ-P1-2
-
 Homo sapiens
2.7.1.149 tyrphostin AG 538
-
 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
-
-
-

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 PI5P4Kalpha isoform Homo sapiens
2.7.1.149 PI5P4Kbeta isoform Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.7.1.149 0.0013
-
 4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(4-methylanilino)pyrimidin-4-yl]amino]phenyl)benzamide isoform PI5P4Kalpha, at pH 7.5 and 37°C Homo sapiens
2.7.1.149 0.0013
-
 N-[3-([6-[([1,1'-biphenyl]-4-yl)amino]pyrimidin-4-yl]amino)phenyl]-4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]benzamide isoform PI5P4Kalpha, at pH 7.5 and 37°C Homo sapiens
2.7.1.149 0.00134
-
 4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[7-(4-methylphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]phenyl)benzamide isoform PI5P4Kalpha, at pH 7.5 and 37°C Homo sapiens
2.7.1.149 0.0019
-
 (2Z)-2-(1H-indol-3-yl)-3-(isoquinolin-5-yl)prop-2-enenitrile isoform PI5P4Kalpha, at pH 7.5 and 37°C Homo sapiens
2.7.1.149 0.00199
-
 4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)benzamide isoform PI5P4Kalpha, at pH 7.5 and 37°C Homo sapiens
2.7.1.149 0.002
-
 4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)cyclohexane-1-carboxamide isoform PI5P4Kalpha, at pH 7.5 and 37°C Homo sapiens
2.7.1.149 0.0021
-
 3-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)benzamide isoform PI5P4Kalpha, at pH 7.5 and 37°C Homo sapiens
2.7.1.149 0.0021
-
 4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)benzamide isoform PI5P4Kalpha, at pH 7.5 and 37°C Homo sapiens
2.7.1.149 0.0026
-
 (2E)-4-(dimethylamino)-N-[1-[(3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)acetyl]piperidin-4-yl]but-2-enamide isoform PI5P4Kalpha, at pH 7.5 and 37°C Homo sapiens
2.7.1.149 0.0035
-
 4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(2-methyl-2H-benzimidazol-5-yl)pyrimidin-4-yl]amino]phenyl)benzamide isoform PI5P4Kalpha, at pH 7.5 and 37°C Homo sapiens
2.7.1.149 0.0038
-
 4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide isoform PI5P4Kbeta, at pH 7.5 and 37°C Homo sapiens
2.7.1.149 0.0052
-
 4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-[(3-[[6-(1H-indol-3-yl)pyrimidin-4-yl]amino]phenyl)methyl]benzamide isoform PI5P4Kalpha, at pH 7.5 and 37°C Homo sapiens
2.7.1.149 0.0053
-
 4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(5-[[6-(1H-indol-3-yl)pyrimidin-4-yl]amino]-2-methylphenyl)benzamide isoform PI5P4Kalpha, at pH 7.5 and 37°C Homo sapiens
2.7.1.149 0.0062
-
 4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(4-methylanilino)pyrimidin-4-yl]amino]phenyl)benzamide isoform PI5P4Kbeta, at pH 7.5 and 37°C Homo sapiens
2.7.1.149 0.0063
-
 N-[3-([6-[([1,1'-biphenyl]-4-yl)amino]pyrimidin-4-yl]amino)phenyl]-4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]benzamide isoform PI5P4Kbeta, at pH 7.5 and 37°C Homo sapiens
2.7.1.149 0.0065
-
 4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(4-methyl-3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)benzamide isoform PI5P4Kalpha, at pH 7.5 and 37°C Homo sapiens
2.7.1.149 0.0089
-
 3-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)benzamide isoform PI5P4Kbeta, at pH 7.5 and 37°C Homo sapiens
2.7.1.149 0.0099
-
 4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[7-(4-methylphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]phenyl)benzamide isoform PI5P4Kbeta, at pH 7.5 and 37°C Homo sapiens
2.7.1.149 0.0101
-
 (2E)-4-(dimethylamino)-N-[1-[(3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)acetyl]piperidin-4-yl]but-2-enamide isoform PI5P4Kbeta, at pH 7.5 and 37°C Homo sapiens
2.7.1.149 0.0109
-
 4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)benzamide isoform PI5P4Kbeta, at pH 7.5 and 37°C Homo sapiens
2.7.1.149 0.0158
-
 4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(2-methyl-2H-benzimidazol-5-yl)pyrimidin-4-yl]amino]phenyl)benzamide isoform PI5P4Kbeta, at pH 7.5 and 37°C Homo sapiens
2.7.1.149 0.0174
-
 N-(3-[[6-([1,1'-biphenyl]-3-yl)pyrimidin-4-yl]amino]phenyl)-4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]benzamide isoform PI5P4Kalpha, at pH 7.5 and 37°C Homo sapiens
2.7.1.149 0.0193
-
 N-[3-([6-[([1,1'-biphenyl]-3-yl)amino]pyrimidin-4-yl]amino)phenyl]-4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]benzamide isoform PI5P4Kalpha, at pH 7.5 and 37°C Homo sapiens
2.7.1.149 0.0205
-
 4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(4-methyl-3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)benzamide isoform PI5P4Kbeta, at pH 7.5 and 37°C Homo sapiens
2.7.1.149 0.0245
-
 N-[3-([6-[([1,1'-biphenyl]-3-yl)amino]pyrimidin-4-yl]amino)phenyl]-4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]benzamide isoform PI5P4Kbeta, at pH 7.5 and 37°C Homo sapiens
2.7.1.149 0.0298
-
 4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-[(3-[[6-(1H-indol-3-yl)pyrimidin-4-yl]amino]phenyl)methyl]benzamide isoform PI5P4Kbeta, at pH 7.5 and 37°C Homo sapiens
2.7.1.149 0.0304
-
 N-(3-[[6-([1,1'-biphenyl]-3-yl)pyrimidin-4-yl]amino]phenyl)-4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]benzamide isoform PI5P4Kbeta, at pH 7.5 and 37°C Homo sapiens
2.7.1.149 0.0318
-
 4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)cyclohexane-1-carboxamide isoform PI5P4Kbeta, at pH 7.5 and 37°C Homo sapiens
2.7.1.149 0.0336
-
 4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(5-[[6-(1H-indol-3-yl)pyrimidin-4-yl]amino]-2-methylphenyl)benzamide isoform PI5P4Kbeta, at pH 7.5 and 37°C Homo sapiens
2.7.1.149 0.0356
-
 4-[[(2E)-4-(dimethylamino)but-2-enoyl]amino]-N-(3-[[6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidin-4-yl]amino]phenyl)benzamide isoform PI5P4Kbeta, at pH 7.5 and 37°C Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.1.149 0.00095
-
 isoform PI5P4Kalpha, at pH 7.5 and 37°C Homo sapiens THZ-P1-2
2.7.1.149 0.0059
-
 isoform PI5P4Kbeta, at pH 7.5 and °C Homo sapiens THZ-P1-2