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Literature summary for 1.4.3.4 extracted from

  • Van der Walt, E.M.; Milczek, E.M.; Malan, S.F.; Edmondson, D.E.; Castagnoli, N.; Bergh, J.J.; Petzer, J.P.
    Inhibition of monoamine oxidase by (E)-styrylisatin analogues (2009), Bioorg. Med. Chem. Lett., 19, 2509-2513.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 1.4.3.4

Protein Variants

Protein Variants Comment Organism
I199A mutant of MAO-B, shows reduced inhibition by (E)-5-styrylisatin and (E)-6-styrylisatin compared to wild-type MAO-B Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(E)-5-(3-chlorostyryl)isatin
-
 Homo sapiens
(E)-5-(3-fluorostyryl)isatin
-
 Homo sapiens
(E)-5-styrylisatin
-
 Homo sapiens
(E)-6-styrylisatin
-
 Homo sapiens
(E)-8-(3-chlorostyryl)caffeine a specific reversible inhibitor of MAO-B Homo sapiens
isatin
-
 Homo sapiens
additional information synthesis and inhibhitory potencies of (E)-styrylisatin analogues on the enzyme, overview. No inhibition of MAO-A by (E)-8-(3-chlorostyryl)caffeine; synthesis and inhibhitory potencies of (E)-styrylisatin analogues on the enzyme, overview. The (E)-5-styrylisatin analogue binds more tightly than the (E)-6 analogue although the latter exhibits the highest MAO-B selectivity Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P21397
-
-
Homo sapiens P27338
-
-

Synonyms

Synonyms Comment Organism
MAO-A
-
 Homo sapiens
MAO-B
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00031
-
 (E)-5-styrylisatin inhibition of MAO-B Homo sapiens
0.00056
-
 (E)-5-(3-fluorostyryl)isatin inhibition of MAO-B Homo sapiens
0.0006
-
 (E)-6-styrylisatin inhibition of MAO-B Homo sapiens
0.00078
-
 (E)-5-styrylisatin inhibition of MAO-A Homo sapiens
0.0011
-
 (E)-5-styrylisatin inhibition of MAO-B mutant I199A Homo sapiens
0.0014
-
 (E)-5-(3-chlorostyryl)isatin inhibition of MAO-B Homo sapiens
0.0015
-
 isatin inhibition of MAO-A Homo sapiens
0.0022
-
 (E)-6-styrylisatin inhibition of MAO-A Homo sapiens
0.0022
-
 (E)-5-(3-fluorostyryl)isatin inhibition of MAO-B mutant I199A Homo sapiens
0.003
-
 isatin inhibition of MAO-B Homo sapiens
0.0045
-
 (E)-6-styrylisatin inhibition of MAO-B mutant I199A Homo sapiens
0.0056
-
 (E)-5-(3-chlorostyryl)isatin inhibition of MAO-A Homo sapiens
0.012
-
 isatin inhibition of MAO-B mutant I199A Homo sapiens
0.0125
-
 (E)-5-(3-chlorostyryl)isatin inhibition of MAO-B mutant I199A Homo sapiens
0.022
-
 (E)-5-(3-fluorostyryl)isatin inhibition of MAO-A Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000207
-
-
 Homo sapiens (E)-5-(3-chlorostyryl)isatin
0.0000301
-
-
 Homo sapiens (E)-6-styrylisatin
0.0000417
-
-
 Homo sapiens (E)-5-styrylisatin
0.000444
-
-
 Homo sapiens (E)-5-(3-fluorostyryl)isatin
0.008566
-
 inhibition of MAO-B Homo sapiens isatin