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Literature summary extracted from

  • Fienberg, S.; Eyermann, C.J.; Arendse, L.; Basarab, G.S.; McPhail, J.; Burke, J.E.; Chibale, K.
    Structural Basis for Inhibitor Potency and Selectivity of Plasmodium falciparum Phosphatidylinositol 4-kinase Inhibitors (2020), ACS Infect. Dis., 6, 3048-3063 .
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.1.67 (1'R)-2'-acetyl-N-(2-fluorophenyl)-1'-(hydroxymethyl)-7'-methoxy-1',2',3',9'-tetrahydrospiro[piperidine-4,4'-pyrido[3,4-b]indole]-1-carboxamide BRD73842 Plasmodium falciparum
2.7.1.67 (1R)-3-[3-[8-(pyridin-4-yl)-1,5-naphthyridin-2-yl]benzene-1-sulfonyl]cyclopentan-1-ol
-
Plasmodium falciparum
2.7.1.67 (3-aminopyrrolidin-1-yl)(4-[5-amino-6-[6-(trifluoromethyl)pyridin-3-yl]pyrazin-2-yl]phenyl)methanone
-
Plasmodium falciparum
2.7.1.67 (4-[3-[4-(methanesulfonyl)phenyl]imidazo[1,2-b]pyridazin-6-yl]phenyl)(piperazin-1-yl)methanone
-
Plasmodium falciparum
2.7.1.67 (4-[5-amino-6-[4-(trifluoromethyl)phenyl]pyrazin-2-yl]phenyl)(3-hydroxypyrrolidin-1-yl)methanone
-
Plasmodium falciparum
2.7.1.67 (4-[5-amino-6-[4-(trifluoromethyl)phenyl]pyrazin-2-yl]phenyl)(piperazin-1-yl)methanone
-
Plasmodium falciparum
2.7.1.67 (4-[5-amino-6-[4-(trifluoromethyl)phenyl]pyrazin-2-yl]phenyl)[(3R)-3-hydroxypyrrolidin-1-yl]methanone
-
Plasmodium falciparum
2.7.1.67 (4-[5-amino-6-[4-(trifluoromethyl)phenyl]pyrazin-2-yl]phenyl)[(3S)-3-hydroxypyrrolidin-1-yl]methanone
-
Plasmodium falciparum
2.7.1.67 (4-[5-amino-6-[6-(trifluoromethyl)pyridin-3-yl]pyrazin-2-yl]phenyl)(piperazin-1-yl)methanone
-
Plasmodium falciparum
2.7.1.67 (4-[6-[3-(methanesulfonyl)phenyl]imidazo[1,2-b]pyridazin-3-yl]phenyl)(piperazin-1-yl)methanone
-
Plasmodium falciparum
2.7.1.67 2-ethoxy-6'-methoxy-5-[4-(methylsulfonyl)phenyl]-3,3'-bipyridine
-
Plasmodium falciparum
2.7.1.67 2-iodo-6'-methoxy-5-[4-(methylsulfonyl)phenyl]-3,3'-bipyridine
-
Plasmodium falciparum
2.7.1.67 2-[3-(phenylsulfanyl)phenyl]-8-(pyridin-4-yl)-1,5-naphthyridine
-
Plasmodium falciparum
2.7.1.67 2-[8-(pyridin-4-yl)-1,5-naphthyridin-2-yl]benzenesulfonamide
-
Plasmodium falciparum
2.7.1.67 2-[[7-(3,4-dimethoxyphenyl)quinoxalin-2-yl]amino]-N-methylacetamide BQR695 Plasmodium falciparum
2.7.1.67 3-(1-methyl-1H-benzimidazol-5-yl)-6-[3-(propane-2-sulfonyl)phenyl]imidazo[1,2-b]pyridazine
-
Plasmodium falciparum
2.7.1.67 3-(6-methoxypyridin-3-yl)-5-[4-(methylsulfonyl)-2-(trifluoromethyl)phenyl]pyrazin-2-amine
-
Plasmodium falciparum
2.7.1.67 3-(6-methoxypyridin-3-yl)-5-[4-(methylsulfonyl)phenyl]pyrazin-2-amine
-
Plasmodium falciparum
2.7.1.67 3-(6-methoxypyridin-3-yl)-5-[4-(trifluoromethoxy)phenyl]pyrazin-2-amine
-
Plasmodium falciparum
2.7.1.67 3-[4-(methylsulfonyl)phenyl]-6-[2-(trifluoromethyl)pyridin-4-yl]imidazo[1,2-b]pyridazine
-
Plasmodium falciparum
2.7.1.67 3-[4-(methylsulfonyl)phenyl]-6-[3-(trifluoromethyl)phenyl]imidazo[1,2-b]pyridazine
-
Plasmodium falciparum
2.7.1.67 3-[8-(4-methylpiperazin-1-yl)-1,5-naphthyridin-2-yl]benzenesulfonamide
-
Plasmodium falciparum
2.7.1.67 3-[8-(pyridin-4-yl)-1,5-naphthyridin-2-yl]benzenesulfonamide
-
Plasmodium falciparum
2.7.1.67 4-[5-amino-6-[6-(trifluoromethyl)pyridin-3-yl]pyrazin-2-yl]benzoic acid
-
Plasmodium falciparum
2.7.1.67 4-[8-(pyridin-4-yl)-1,5-naphthyridin-2-yl]benzenesulfonamide
-
Plasmodium falciparum
2.7.1.67 5-[4-(methylsulfonyl)phenyl]-3-[6-(trifluoromethyl)pyridin-3-yl]pyrazin-2-amine
-
Plasmodium falciparum
2.7.1.67 5-[4-(methylsulfonyl)phenyl]-6'-(trifluoromethyl)-3,3'-bipyridin-2-amine MMV390048 Plasmodium falciparum
2.7.1.67 6-(3-methylphenyl)-3-(6-methylpyridin-3-yl)imidazo[1,2-b]pyridazine
-
Plasmodium falciparum
2.7.1.67 6-[3-(methylsulfonyl)phenyl]-3-[4-(methylsulfonyl)phenyl]imidazo[1,2-a]pyridine
-
Plasmodium falciparum
2.7.1.67 6-[3-(methylsulfonyl)phenyl]-3-[4-(methylsulfonyl)phenyl]imidazo[1,2-a]pyrimidine
-
Plasmodium falciparum
2.7.1.67 6-[3-(methylsulfonyl)phenyl]-3-[4-(methylsulfonyl)phenyl]imidazo[1,2-b]pyridazine
-
Plasmodium falciparum
2.7.1.67 6-[4-(cyclopropylsulfonyl)phenyl]-3-[4-(methylsulfonyl)phenyl]imidazo[1,2-b]pyridazine
-
Plasmodium falciparum
2.7.1.67 N-(4-chlorophenyl)-N-methyl-3-[4-(methylcarbamoyl)phenyl]imidazo[1,2-a]pyrazine-6-carboxamide KDU691 Plasmodium falciparum
2.7.1.67 N-(4-cyanophenyl)-N-methyl-3-[4-(trifluoromethyl)phenyl]imidazo[1,2-a]pyrazine-6-carboxamide KAI407 Plasmodium falciparum
2.7.1.67 N-cyclopropyl-8-(pyridin-4-yl)-1,5-naphthyridin-2-amine
-
Plasmodium falciparum
2.7.1.67 N-[3-[8-(pyridin-4-yl)-1,5-naphthyridin-2-yl]phenyl]methanesulfonamide
-
Plasmodium falciparum
2.7.1.67 [(3R)-3-aminopyrrolidin-1-yl](4-[5-amino-6-[4-(trifluoromethyl)phenyl]pyrazin-2-yl]phenyl)methanone
-
Plasmodium falciparum
2.7.1.67 [(3S)-3-aminopyrrolidin-1-yl](4-[5-amino-6-[4-(trifluoromethyl)phenyl]pyrazin-2-yl]phenyl)methanone
-
Plasmodium falciparum

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.1.67 ATP + 1-phosphatidyl-1D-myo-inositol Plasmodium falciparum
-
ADP + 1-phosphatidyl-1D-myo-inositol 4-phosphate
-
?

Organism

EC Number Organism UniProt Comment Textmining
2.7.1.67 Plasmodium falciparum
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.1.67 ATP + 1-phosphatidyl-1D-myo-inositol
-
Plasmodium falciparum ADP + 1-phosphatidyl-1D-myo-inositol 4-phosphate
-
?

Synonyms

EC Number Synonyms Comment Organism
2.7.1.67 phosphatidylinositol 4-kinase
-
Plasmodium falciparum
2.7.1.67 PI4K
-
Plasmodium falciparum

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.1.67 0.0000015
-
pH and temperature not specified in the publication Plasmodium falciparum N-(4-chlorophenyl)-N-methyl-3-[4-(methylcarbamoyl)phenyl]imidazo[1,2-a]pyrazine-6-carboxamide
2.7.1.67 0.0000034
-
pH and temperature not specified in the publication Plasmodium falciparum 5-[4-(methylsulfonyl)phenyl]-6'-(trifluoromethyl)-3,3'-bipyridin-2-amine
2.7.1.67 0.0000035
-
pH and temperature not specified in the publication Plasmodium falciparum 2-[[7-(3,4-dimethoxyphenyl)quinoxalin-2-yl]amino]-N-methylacetamide
2.7.1.67 0.000021
-
pH and temperature not specified in the publication Plasmodium falciparum (1'R)-2'-acetyl-N-(2-fluorophenyl)-1'-(hydroxymethyl)-7'-methoxy-1',2',3',9'-tetrahydrospiro[piperidine-4,4'-pyrido[3,4-b]indole]-1-carboxamide
2.7.1.67 0.000023
-
pH and temperature not specified in the publication Plasmodium falciparum (4-[5-amino-6-[4-(trifluoromethyl)phenyl]pyrazin-2-yl]phenyl)(piperazin-1-yl)methanone
2.7.1.67 0.00012
-
pH and temperature not specified in the publication Plasmodium falciparum N-(4-cyanophenyl)-N-methyl-3-[4-(trifluoromethyl)phenyl]imidazo[1,2-a]pyrazine-6-carboxamide