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Literature summary for 1.3.5.2 extracted from

  • Bedingfield, P.T.; Cowen, D.; Acklam, P.; Cunningham, F.; Parsons, M.R.; McConkey, G.A.; Fishwick, C.W.; Johnson, A.P.
    Factors influencing the specificity of inhibitor binding to the human and malaria parasite dihydroorotate dehydrogenases (2012), J. Med. Chem., 55, 5841-5850.
    View publication on PubMed
Search for more literature for 1.3.5.2

Crystallization (Commentary)

Crystallization (Comment) Organism
in complex with inhibitors 2-[(2,5-dichlorophenyl)sulfanyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol and 2-[(2,5-dichlorophenyl)sulfanyl]-5-ethyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol. bindung induces a structural change in the N-terminal helix. Comparison with binding to Plasmodium falciparum enzyme Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2-[(2,5-dichlorophenyl)sulfanyl]-5-ethyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol compound has therapeutically relevant activity against human enzyme Homo sapiens
2-[(2,5-dichlorophenyl)sulfanyl]-5-ethyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol no specific inhibition of Plasmodium enzyme, good inhibitor of human enzyme Plasmodium falciparum
2-[(2,5-dichlorophenyl)sulfanyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol compound has therapeutically relevant activity against human enzyme Homo sapiens
2-[(2,5-dichlorophenyl)sulfanyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol no specific inhibition of Plasmodium enzyme, good inhibitor of human enzyme Plasmodium falciparum
2-[(3,4-dichlorophenyl)sulfanyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol compound is less active with human enzyme but good inhibitor of Plasmodium falciparum enzyme Homo sapiens
2-[(3,4-dichlorophenyl)sulfanyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol
-
 Plasmodium falciparum
2-[(4-chlorophenyl)sulfanyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol compound is less active with human enzyme but good inhibitor of Plasmodium falciparum enzyme Homo sapiens
2-[(4-chlorophenyl)sulfanyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol
-
 Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Homo sapiens Q02127
-
-
Plasmodium falciparum
-
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000013
-
 or above, pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-[(2,5-dichlorophenyl)sulfanyl]-5-ethyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol
0.000051
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-[(2,5-dichlorophenyl)sulfanyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol
0.001
-
 pH not specified in the publication, temperature not specified in the publication Plasmodium falciparum 2-[(4-chlorophenyl)sulfanyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol
0.0019
-
 pH not specified in the publication, temperature not specified in the publication Plasmodium falciparum 2-[(3,4-dichlorophenyl)sulfanyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol
0.0065
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-[(3,4-dichlorophenyl)sulfanyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol
0.011
-
 pH not specified in the publication, temperature not specified in the publication Plasmodium falciparum 2-[(2,5-dichlorophenyl)sulfanyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol
0.039
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-[(4-chlorophenyl)sulfanyl]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol
0.1
-
 or above, pH not specified in the publication, temperature not specified in the publication Plasmodium falciparum 2-[(2,5-dichlorophenyl)sulfanyl]-5-ethyl[1,2,4]triazolo[1,5-a]pyrimidin-7-ol