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Literature summary for 2.7.1.149 extracted from

  • Davis, M.I.; Sasaki, A.T.; Shen, M.; Emerling, B.M.; Thorne, N.; Michael, S.; Pragani, R.; Boxer, M.; Sumita, K.; Takeuchi, K.; Auld, D.S.; Li, Z.; Cantley, L.C.; Simeonov, A.
    A homogeneous, high-throughput assay for phosphatidylinositol 5-phosphate 4-kinase with a novel, rapid substrate preparation (2013), PLoS ONE, 8, e54127.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
(2E)-2-(3,4-dihydroxybenzoyl)-3-(3,4-dihydroxyphenyl)prop-2-enenitrile
-
Homo sapiens
(2E)-2-(3,4-dihydroxybenzoyl)-3-(4-hydroxy-3-iodo-5-methoxyphenyl)prop-2-enenitrile
-
Homo sapiens
(3E)-5-amino-3-[(2Z)-1-cyano-2-(3H-indol-3-ylidene)ethylidene]-2,3-dihydro-1H-pyrazole-4-carbonitrile
-
Homo sapiens
(3Z)-2-amino-4-(3,4,5-trihydroxyphenyl)buta-1,3-diene-1,1,3-tricarbonitrile
-
Homo sapiens
additional information high-throughput inhibitor screening method, counterscreen assay and ATP competition assay, overview Homo sapiens
tyrphostin ATP-competitive inhibitors, i.e. tyrosine phosphorylation inhibitors, of isozyme PI5P4Kalpha Homo sapiens
tyrphostin 23
-
Homo sapiens
tyrphostin 47
-
Homo sapiens
tyrphostin AG 1478
-
Homo sapiens
tyrphostin AG 490
-
Homo sapiens
tyrphostin AG 494
-
Homo sapiens
tyrphostin AG 537
-
Homo sapiens
tyrphostin AG 555
-
Homo sapiens
tyrphostin AG 698
-
Homo sapiens
tyrphostin AG 808
-
Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ required Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
phosphatidylinositol 5-phosphate 4-kinase
-
Homo sapiens
PI5P 4-kinase
-
Homo sapiens
PI5P4K
-
Homo sapiens
PI5P4Kalpha
-
Homo sapiens
type II kinase
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
22
-
assay at room temperature Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.001
-
pH 7.4, 22°C, isozyme PI5P4Kalpha Homo sapiens tyrphostin
0.002
-
pH 7.4, 22°C, isozyme PI5P4Kalpha Homo sapiens (2E)-2-(3,4-dihydroxybenzoyl)-3-(4-hydroxy-3-iodo-5-methoxyphenyl)prop-2-enenitrile
0.005
-
pH 7.4, 22°C, isozyme PI5P4Kalpha Homo sapiens (3Z)-2-amino-4-(3,4,5-trihydroxyphenyl)buta-1,3-diene-1,1,3-tricarbonitrile
0.013
-
pH 7.4, 22°C, isozyme PI5P4Kalpha Homo sapiens (3E)-5-amino-3-[(2Z)-1-cyano-2-(3H-indol-3-ylidene)ethylidene]-2,3-dihydro-1H-pyrazole-4-carbonitrile
0.014
-
pH 7.4, 22°C, isozyme PI5P4Kalpha Homo sapiens (2E)-2-(3,4-dihydroxybenzoyl)-3-(3,4-dihydroxyphenyl)prop-2-enenitrile
0.018
-
pH 7.4, 22°C, isozyme PI5P4Kalpha Homo sapiens tyrphostin AG 808
0.02
-
pH 7.4, 22°C, isozyme PI5P4Kalpha Homo sapiens tyrphostin 47
0.032
-
pH 7.4, 22°C, isozyme PI5P4Kalpha Homo sapiens tyrphostin AG 537
0.045
-
pH 7.4, 22°C, isozyme PI5P4Kalpha Homo sapiens tyrphostin 23
0.05
-
pH 7.4, 22°C, isozyme PI5P4Kalpha Homo sapiens tyrphostin AG 698
0.055
-
pH 7.4, 22°C, isozyme PI5P4Kalpha Homo sapiens tyrphostin AG 555
0.089
-
pH 7.4, 22°C, isozyme PI5P4Kalpha Homo sapiens tyrphostin AG 494
0.089
-
pH 7.4, 22°C, isozyme PI5P4Kalpha Homo sapiens tyrphostin AG 490
0.1
-
pH 7.4, 22°C, isozyme PI5P4Kalpha Homo sapiens tyrphostin AG 1478