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Literature summary for 2.3.1.97 extracted from

  • Bayliss, T.; Robinson, D.A.; Smith, V.C.; Brand, S.; McElroy, S.P.; Torrie, L.S.; Mpamhanga, C.; Norval, S.; Stojanovski, L.; Brenk, R.; Frearson, J.A.; Read, K.D.; Gilbert, I.H.; Wyatt, P.G.
    Design and synthesis of brain penetrant trypanocidal N-myristoyltransferase inhibitors (2017), J. Med. Chem., 60, 9790-9806 .
    View publication on PubMedView publication on EuropePMC
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Inhibitors

Inhibitors Comment Organism Structure
1-(4-(3,5-dichloro-4-((2-methylpyridin-3-yl)methoxy)phenyl)pyridin-2-yl)piperazine 3fold selectivity over human isoform NMT1 Trypanosoma brucei
1-(4-(3,5-dichloro-4-((2-phenylpyridin-3-yl)methoxy)phenyl)-pyridin-2-yl)piperazine 3fold selectivity over human isoform NMT1 Trypanosoma brucei
1-(4-(3,5-dichloro-4-(pyridin-2-ylmethoxy)phenyl)pyridin-2-yl)-piperazine 2fold selectivity over human isoform NMT1; 65fold selectivity over human isoform NMT1 Trypanosoma brucei
additional information development of inhibitors based on DDD85646 Trypanosoma brucei

Organism

Organism UniProt Comment Textmining
Trypanosoma brucei
-
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00002
-
 pH 7.4, 22°C Trypanosoma brucei 1-(4-(3,5-dichloro-4-(pyridin-2-ylmethoxy)phenyl)pyridin-2-yl)-piperazine
0.00008
-
 pH 7.4, 22°C Trypanosoma brucei 1-(4-(3,5-dichloro-4-((2-phenylpyridin-3-yl)methoxy)phenyl)-pyridin-2-yl)piperazine
0.0001
-
 pH 7.4, 22°C Trypanosoma brucei 1-(4-(3,5-dichloro-4-((2-methylpyridin-3-yl)methoxy)phenyl)pyridin-2-yl)piperazine
0.0001
-
 pH 7.4, 22°C Trypanosoma brucei 1-(4-(3,5-dichloro-4-(pyridin-2-ylmethoxy)phenyl)pyridin-2-yl)-piperazine