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Literature summary for 2.7.1.67 extracted from

  • Sala, M.; Koegler, M.; Plackova, P.; Mejdrova, I.; Hrebabecky, H.; Prochazkova, E.; Strunin, D.; Lee, G.; Birkus, G.; Weber, J.; Mertlikova-Kaiserova, H.; Nencka, R.
    Purine analogs as phosphatidylinositol 4-kinase IIIbeta inhibitors (2016), Bioorg. Med. Chem. Lett., 26, 2706-2712 .
    View publication on PubMed
Search for more literature for 2.7.1.67

Activating Compound

Activating Compound Comment Organism Structure
4-[9-(3,4-dimethoxyphenyl)-2-methyl-6-[[2-(morpholin-4-yl)ethyl]amino]-9H-purin-8-yl]benzaldehyde 138% residual activity at 0.01 mM Homo sapiens
4-[9-(3,4-dimethoxyphenyl)-2-methyl-6-[[2-(morpholin-4-yl)ethyl]amino]-9H-purin-8-yl]phenol 125% residual activity at 0.01 mM Homo sapiens
9-(3,4-dimethoxyphenyl)-2,8-dimethyl-N-[2-(morpholin-4-yl)ethyl]-9H-purin-6-amine 126% residual activity at 0.01 mM Homo sapiens
9-(3,4-dimethoxyphenyl)-2-methyl-N-[2-(morpholin-4-yl)ethyl]-8-(4-phenoxyphenyl)-9H-purin-6-amine 112% activity at 0.01 mM Homo sapiens
[4-[9-(3,4-dimethoxyphenyl)-2-methyl-6-[[2-(morpholin-4-yl)ethyl]amino]-9H-purin-8-yl]phenyl]methanol 103% residual activity at 0.01 mM Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1-[3-[9-(3,4-dimethoxyphenyl)-8-methyl-6-[[2-(morpholin-4-yl)ethyl]amino]-9H-purin-2-yl]phenyl]-2-methylpropan-1-one 16% residual activity at 0.01 mM Homo sapiens
2-(3-chlorophenyl)-9-(3,4-dimethoxyphenyl)-8-methyl-N-[2-(morpholin-4-yl)ethyl]-9H-purin-6-amine 67% residual activity at 0.01 mM Homo sapiens
3-(3,4-dimethoxyphenyl)-2,5-dimethyl-N-[2-(morpholin-4-yl)ethyl]pyrazolo[1,5-a]pyrimidin-7-amine
-
 Homo sapiens
3-(3,4-dimethoxyphenyl)-5-methyl-N-[2-(morpholin-4-yl)ethyl]-3H-[1,2,3]triazolo[4,5-d]pyrimidin-7-amine 31% residual activity at 0.01 mM Homo sapiens
3-(3,4-dimethoxyphenyl)-N-[2-(morpholin-4-yl)ethyl]-3H-[1,2,3]triazolo[4,5-d]pyrimidin-7-amine 41% residual activity at 0.01 mM Homo sapiens
4-[9-(3,4-dimethoxyphenyl)-2-methyl-6-[[2-(morpholin-4-yl)ethyl]amino]-9H-purin-8-yl]benzonitrile 97% residual activity at 0.01 mM Homo sapiens
4-[9-(3,4-dimethoxyphenyl)-8-methyl-6-[[2-(morpholin-4-yl)ethyl]amino]-9H-purin-2-yl]benzonitrile 97% residual activity at 0.01 mM Homo sapiens
4-[9-(3,4-dimethoxyphenyl)-8-methyl-6-[[2-(morpholin-4-yl)ethyl]amino]-9H-purin-2-yl]phenol 18% residual activity at 0.01 mM Homo sapiens
7-(3,4-dimethoxyphenyl)-N-[2-(morpholin-4-yl)ethyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine 74% residual activity at 0.01 mM Homo sapiens
8-(cyclohex-3-en-1-yl)-9-(3,4-dimethoxyphenyl)-2-methyl-N-[2-(morpholin-4-yl)ethyl]-9H-purin-6-amine 75% residual activity at 0.01 mM Homo sapiens
8-bromo-9-(3,4-dimethoxyphenyl)-2-methyl-N-[2-(morpholin-4-yl)ethyl]-9H-purin-6-amine 17% residual activity at 0.01 mM Homo sapiens
8-cyclohexyl-9-(3,4-dimethoxyphenyl)-2-methyl-N-[2-(morpholin-4-yl)ethyl]-9H-purin-6-amine 79% residual activity at 0.01 mM Homo sapiens
9-(3,4-dimethoxyphenyl)-2,8-dimethyl-N-[2-(morpholin-4-yl)ethyl]-5,9-dihydro-4H-purin-6-amine 14% residual activity at 0.01 mM Homo sapiens
9-(3,4-dimethoxyphenyl)-2-(4-fluorophenyl)-8-methyl-N-[2-(morpholin-4-yl)ethyl]-9H-purin-6-amine 66% residual activity at 0.01 mM Homo sapiens
9-(3,4-dimethoxyphenyl)-2-ethynyl-8-methyl-N-[2-(morpholin-4-yl)ethyl]-9H-purin-6-amine 18% residual activity at 0.01 mM Homo sapiens
9-(3,4-dimethoxyphenyl)-2-iodo-8-methyl-N-[2-(morpholin-4-yl)ethyl]-9H-purin-6-amine 33% residual activity at 0.01 mM Homo sapiens
9-(3,4-dimethoxyphenyl)-2-methoxy-8-methyl-N-[2-(morpholin-4-yl)ethyl]-9H-purin-6-amine 15% residual activity at 0.01 mM Homo sapiens
9-(3,4-dimethoxyphenyl)-2-methyl-N-[2-(morpholin-4-yl)ethyl]-8-(3-phenylprop-1-yn-1-yl)-9H-purin-6-amine 96% residual activity at 0.01 mM Homo sapiens
9-(3,4-dimethoxyphenyl)-2-methyl-N-[2-(morpholin-4-yl)ethyl]-8-(propan-2-yl)-9H-purin-6-amine 65% residual activity at 0.01 mM Homo sapiens
9-(3,4-dimethoxyphenyl)-2-methyl-N-[2-(morpholin-4-yl)ethyl]-8-(thiophen-3-yl)-9H-purin-6-amine 94% residual activity at 0.01 mM Homo sapiens
9-(3,4-dimethoxyphenyl)-2-methyl-N-[2-(morpholin-4-yl)ethyl]-8-(trifluoromethyl)-9H-purin-6-amine 99% residual activity at 0.01 mM Homo sapiens
9-(3,4-dimethoxyphenyl)-2-methyl-N-[2-(morpholin-4-yl)ethyl]-9H-purin-6-amine 26% residual activity at 0.01 mM Homo sapiens
9-(3,4-dimethoxyphenyl)-8-(4-fluorophenyl)-2-methyl-N-[2-(morpholin-4-yl)ethyl]-9H-purin-6-amine 78% residual activity at 0.01 mM Homo sapiens
9-(3,4-dimethoxyphenyl)-8-iodo-2-methyl-N-[2-(morpholin-4-yl)ethyl]-9H-purin-6-amine 38% residual activity at 0.01 mM Homo sapiens
9-(3,4-dimethoxyphenyl)-8-methoxy-2-methyl-N-[2-(morpholin-4-yl)ethyl]-9H-purin-6-amine 86% residual activity at 0.01 mM Homo sapiens
9-(3,4-dimethoxyphenyl)-8-methyl-6-[[2-(morpholin-4-yl)ethyl]amino]-9H-purine-2-carbonitrile 24% residual activity at 0.01 mM Homo sapiens
9-(3,4-dimethoxyphenyl)-8-methyl-N-[2-(morpholin-4-yl)ethyl]-2-(3-phenylprop-1-yn-1-yl)-9H-purin-6-amine 58% residual activity at 0.01 mM Homo sapiens
9-(3,4-dimethoxyphenyl)-8-methyl-N-[2-(morpholin-4-yl)ethyl]-2-(pyridin-3-yl)-9H-purin-6-amine 36% residual activity at 0.01 mM Homo sapiens
9-(3,4-dimethoxyphenyl)-8-methyl-N-[2-(morpholin-4-yl)ethyl]-2-(thiophen-3-yl)-9H-purin-6-amine 46% residual activity at 0.01 mM Homo sapiens
9-(3,4-dimethoxyphenyl)-8-methyl-N-[2-(morpholin-4-yl)ethyl]-9H-purin-6-amine 13% residual activity at 0.01 mM Homo sapiens
9-(3,4-dimethoxyphenyl)-8-methyl-N6-[2-(morpholin-4-yl)ethyl]-9H-purine-2,6-diamine 25% residual activity at 0.01 mM Homo sapiens
N-[3-[9-(3,4-dimethoxyphenyl)-8-methyl-6-[[2-(morpholin-4-yl)ethyl]amino]-9H-purin-2-yl]phenyl]acetamide 14% residual activity at 0.01 mM Homo sapiens
PIK93
-
 Homo sapiens
T-00127-HEV1
-
 Homo sapiens
[9-(3,4-dimethoxyphenyl)-2-methyl-6-[[2-(morpholin-4-yl)ethyl]amino]-9H-purin-8-yl]methanol 62% residual activity at 0.01 mM 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 Homo sapiens
-
 ADP + 1-phosphatidyl-1D-myo-inositol 4-phosphate
-
 ?

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
-
 Homo sapiens ADP + 1-phosphatidyl-1D-myo-inositol 4-phosphate
-
 ?

Synonyms

Synonyms Comment Organism
phosphatidylinositol 4-kinase IIIbeta
-
 Homo sapiens
PI 4-kinase
-
 Homo sapiens
PI4K IIIbeta
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00091
-
 isoform PI4K IIIbeta, pH and temperature not specified in the publication Homo sapiens 9-(3,4-dimethoxyphenyl)-2,8-dimethyl-N-[2-(morpholin-4-yl)ethyl]-5,9-dihydro-4H-purin-6-amine
0.00109
-
 isoform PI4K IIIbeta, pH and temperature not specified in the publication Homo sapiens 1-[3-[9-(3,4-dimethoxyphenyl)-8-methyl-6-[[2-(morpholin-4-yl)ethyl]amino]-9H-purin-2-yl]phenyl]-2-methylpropan-1-one
0.00144
-
 isoform PI4K IIIbeta, pH and temperature not specified in the publication Homo sapiens 9-(3,4-dimethoxyphenyl)-8-methyl-N6-[2-(morpholin-4-yl)ethyl]-9H-purine-2,6-diamine
0.00161
-
 isoform PI4K IIIbeta, pH and temperature not specified in the publication Homo sapiens 9-(3,4-dimethoxyphenyl)-8-methyl-N-[2-(morpholin-4-yl)ethyl]-9H-purin-6-amine
0.00191
-
 isoform PI4K IIIbeta, pH and temperature not specified in the publication Homo sapiens 9-(3,4-dimethoxyphenyl)-2-ethynyl-8-methyl-N-[2-(morpholin-4-yl)ethyl]-9H-purin-6-amine
0.00207
-
 isoform PI4K IIIbeta, pH and temperature not specified in the publication Homo sapiens 9-(3,4-dimethoxyphenyl)-8-methyl-6-[[2-(morpholin-4-yl)ethyl]amino]-9H-purine-2-carbonitrile
0.00214
-
 isoform PI4K IIIbeta, pH and temperature not specified in the publication Homo sapiens N-[3-[9-(3,4-dimethoxyphenyl)-8-methyl-6-[[2-(morpholin-4-yl)ethyl]amino]-9H-purin-2-yl]phenyl]acetamide
0.00237
-
 isoform PI4K IIIbeta, pH and temperature not specified in the publication Homo sapiens 4-[9-(3,4-dimethoxyphenyl)-8-methyl-6-[[2-(morpholin-4-yl)ethyl]amino]-9H-purin-2-yl]phenol
0.00299
-
 isoform PI4K IIIbeta, pH and temperature not specified in the publication Homo sapiens 9-(3,4-dimethoxyphenyl)-2-methoxy-8-methyl-N-[2-(morpholin-4-yl)ethyl]-9H-purin-6-amine
0.0052
-
 isoform PI4K IIIbeta, pH and temperature not specified in the publication Homo sapiens 8-bromo-9-(3,4-dimethoxyphenyl)-2-methyl-N-[2-(morpholin-4-yl)ethyl]-9H-purin-6-amine