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Literature summary for 3.1.1.8 extracted from

  • Chen, X.; Tikhonova, I.G.; Decker, M.
    Probing the mid-gorge of cholinesterases with spacer-modified bivalent quinazolinimines leads to highly potent and selective butyrylcholinesterase inhibitors (2011), Bioorg. Med. Chem., 19, 1222-1235.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(13E,13'Z)-N,N'-hexane-1,6-diylbis(6,7,8,9,10,11-hexahydro-13H-azocino[2,1-b]quinazolin-13-imine)
-
Equus caballus
(13Z,13'Z)-N,N'-heptane-1,7-diylbis(6,7,8,9,10,11-hexahydro-13H-azocino[2,1-b]quinazolin-13-imine)
-
Equus caballus
(9E,9'E)-N,N'-hexane-1,6-diylbis(2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-imine)
-
Equus caballus
(9E,9'Z)-N,N'-heptane-1,7-diylbis(2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-imine)
-
Equus caballus
(Z)-N1-methyl-N4-(8,9,10,11-tetrahydro-6H-azocino[2,1-b]quinazolin-13(7H)-ylidene)-N1-(3-((E)-8,9,10,11-tetrahydro-6H-azocino[2,1-b]quinazolin-13(7H)-ylideneamino)propyl)-butane-1,4-diamine
-
Equus caballus
2-acetamido-N-(4-(8,9,10,11-tetrahydro-6H-azocino-[2,1-b]quinazolin-13(7H)-ylideneamino)butyl)-N-(3-(8,9,10,-11-tetrahydro-6H-azocino[2,1-b]quinazolin-13(7H)-ylideneamino)propyl)acetamide
-
Equus caballus
3-methyl-N-(4-(8,9,10,11-tetrahydro-6H-azocino-[2,1-b]quinazolin-13(7H)-ylideneamino)butyl)-N-(3-(8,9,-10,11-tetrahydro-6H-azocino[2,1-b]quinazolin-13(7H)-ylideneamino)propyl)butanamide
-
Equus caballus
4-methyl-N-(4-(8,9,10,11-tetrahydro-6H-azocino-[2,1-b]quinazolin-13(7H)-ylideneamino)butyl)-N-(3-(8,9,-10,11-tetrahydro-6H-azocino[2,1-b]quinazolin-13(7H)-ylideneamino)propyl)pentanamide
-
Equus caballus
cymserine BChE selective inhibitor Equus caballus
galanthamine
-
Equus caballus
N,N-bis(3-(2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-ylideneamino)propyl) acetamide
-
Equus caballus
N,N-bis(3-(8,9,10,11-tetrahydro-6H-azocino[2,1-b]quinazolin-13(7H)-ylideneamino)propyl)acetamide
-
Equus caballus
N-(4-(2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-ylideneamino)butyl)-N-(3-(2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-ylideneamino)propyl) methacrylamide
-
Equus caballus
N-(4-(2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-ylideneamino)butyl)-N-(3-(2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-ylideneamino)propyl) propionamide
-
Equus caballus
N-(4-(2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-ylideneamino)butyl)-N-(3-(2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-ylideneamino)propyl)acetamide
-
Equus caballus
N-(4-(8,9,10,11-tetrahydro-6H-azocino[2,1-b]quinazolin-13(7H)-ylideneamino)butyl)-N-(3-(8,9,10,11-tetrahydro--6H-azocino[2,1-b]quinazolin-13(7H)-ylideneamino)propyl)-acetamide
-
Equus caballus
N-(4-(8,9,10,11-tetrahydro-6H-azocino[2,1-b]quinazolin-13(7H)-ylideneamino)butyl)-N-(3-(8,9,10,11-tetrahydro-6H-azocino[2,1-b]quinazolin-13(7H)-ylideneamino)propyl)-methacrylamide
-
Equus caballus
N-(4-(8,9,10,11-tetrahydro-6H-azocino[2,1-b]quinazolin-13(7H)-ylideneamino)butyl)-N-(3-(8,9,10,11-tetrahydro-6H-azocino[2,1-b]quinazolin-13(7H)-ylideneamino)propyl)-pentanamide
-
Equus caballus
N-(4-(8,9,10,11-tetrahydro-6H-azocino[2,1-b]quinazolin-13(7H)-ylideneamino)butyl)-N-(3-(8,9,10,11-tetrahydro-6H-azocino[2,1-b]quinazolin-13(7H)-ylideneamino)propyl)-pivalamide
-
Equus caballus
N-(4-(8,9,10,11-tetrahydro-6H-azocino[2,1-b]quinazolin-13(7H)-ylideneamino)butyl)-N-(3-(8,9,10,11-tetrahydro-6H-azocino[2,1-b]quinazolin-13(7H)-ylideneamino)propyl)-propionamide
-
Equus caballus
N1-(2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-ylidene)-N3-(3-(2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-ylideneamino)propyl)-N3-methylpropane-1,3-diamine
-
Equus caballus
N1-(2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-ylidene)-N4-(3-(2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-ylideneamino)propyl)-N4-methylbutane-1,4-diamine
-
Equus caballus
N1-methyl-N3-(8,9,10,11-tetrahydro-6H-azocino[2,1-b]quinazolin-13(7H)-ylidene)-N1-(3-(8,9,10,11-tetrahydro-6Hazocino[2,1-b]quinazolin-13(7H)-ylideneamino)propyl)propane-1,3-diamine
-
Equus caballus
tacrine
-
Equus caballus

Organism

Organism UniProt Comment Textmining
Equus caballus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
serum
-
Equus caballus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acetylthiocholine + H2O
-
Equus caballus thiocholine + acetate
-
?
benzoylcholine + H2O
-
Equus caballus choline + benzoate
-
?
butyrylthiocholine + H2O
-
Equus caballus thiocholine + butyrate
-
?

Synonyms

Synonyms Comment Organism
BChE
-
Equus caballus
butyrylcholinesterase
-
Equus caballus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000003
-
in 100 mM potassium dihydrogen phosphate buffer, pH 8.0, at 25°C Equus caballus 4-methyl-N-(4-(8,9,10,11-tetrahydro-6H-azocino-[2,1-b]quinazolin-13(7H)-ylideneamino)butyl)-N-(3-(8,9,-10,11-tetrahydro-6H-azocino[2,1-b]quinazolin-13(7H)-ylideneamino)propyl)pentanamide
0.000004
-
in 100 mM potassium dihydrogen phosphate buffer, pH 8.0, at 25°C Equus caballus N-(4-(2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-ylideneamino)butyl)-N-(3-(2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-ylideneamino)propyl)acetamide
0.0000048
-
pH and temperature not specified in the publication Equus caballus (9E,9'Z)-N,N'-heptane-1,7-diylbis(2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-imine)
0.0000059
-
in 100 mM potassium dihydrogen phosphate buffer, pH 8.0, at 25°C Equus caballus N-(4-(2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-ylideneamino)butyl)-N-(3-(2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-ylideneamino)propyl) propionamide
0.0000064
-
in 100 mM potassium dihydrogen phosphate buffer, pH 8.0, at 25°C Equus caballus tacrine
0.0000081
-
in 100 mM potassium dihydrogen phosphate buffer, pH 8.0, at 25°C Equus caballus 3-methyl-N-(4-(8,9,10,11-tetrahydro-6H-azocino-[2,1-b]quinazolin-13(7H)-ylideneamino)butyl)-N-(3-(8,9,-10,11-tetrahydro-6H-azocino[2,1-b]quinazolin-13(7H)-ylideneamino)propyl)butanamide
0.0000106
-
in 100 mM potassium dihydrogen phosphate buffer, pH 8.0, at 25°C Equus caballus N-(4-(2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-ylideneamino)butyl)-N-(3-(2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-ylideneamino)propyl) methacrylamide
0.0000129
-
in 100 mM potassium dihydrogen phosphate buffer, pH 8.0, at 25°C Equus caballus N-(4-(8,9,10,11-tetrahydro-6H-azocino[2,1-b]quinazolin-13(7H)-ylideneamino)butyl)-N-(3-(8,9,10,11-tetrahydro-6H-azocino[2,1-b]quinazolin-13(7H)-ylideneamino)propyl)-pentanamide
0.0000255
-
in 100 mM potassium dihydrogen phosphate buffer, pH 8.0, at 25°C Equus caballus N-(4-(8,9,10,11-tetrahydro-6H-azocino[2,1-b]quinazolin-13(7H)-ylideneamino)butyl)-N-(3-(8,9,10,11-tetrahydro-6H-azocino[2,1-b]quinazolin-13(7H)-ylideneamino)propyl)-pivalamide
0.000027
-
pH and temperature not specified in the publication Equus caballus (13E,13'Z)-N,N'-hexane-1,6-diylbis(6,7,8,9,10,11-hexahydro-13H-azocino[2,1-b]quinazolin-13-imine)
0.0000377
-
in 100 mM potassium dihydrogen phosphate buffer, pH 8.0, at 25°C Equus caballus N-(4-(8,9,10,11-tetrahydro-6H-azocino[2,1-b]quinazolin-13(7H)-ylideneamino)butyl)-N-(3-(8,9,10,11-tetrahydro-6H-azocino[2,1-b]quinazolin-13(7H)-ylideneamino)propyl)-methacrylamide
0.0000431
-
in 100 mM potassium dihydrogen phosphate buffer, pH 8.0, at 25°C Equus caballus N-(4-(8,9,10,11-tetrahydro-6H-azocino[2,1-b]quinazolin-13(7H)-ylideneamino)butyl)-N-(3-(8,9,10,11-tetrahydro--6H-azocino[2,1-b]quinazolin-13(7H)-ylideneamino)propyl)-acetamide
0.0000463
-
in 100 mM potassium dihydrogen phosphate buffer, pH 8.0, at 25°C Equus caballus N-(4-(8,9,10,11-tetrahydro-6H-azocino[2,1-b]quinazolin-13(7H)-ylideneamino)butyl)-N-(3-(8,9,10,11-tetrahydro-6H-azocino[2,1-b]quinazolin-13(7H)-ylideneamino)propyl)-propionamide
0.0000514
-
in 100 mM potassium dihydrogen phosphate buffer, pH 8.0, at 25°C Equus caballus (Z)-N1-methyl-N4-(8,9,10,11-tetrahydro-6H-azocino[2,1-b]quinazolin-13(7H)-ylidene)-N1-(3-((E)-8,9,10,11-tetrahydro-6H-azocino[2,1-b]quinazolin-13(7H)-ylideneamino)propyl)-butane-1,4-diamine
0.0000727
-
in 100 mM potassium dihydrogen phosphate buffer, pH 8.0, at 25°C Equus caballus N,N-bis(3-(8,9,10,11-tetrahydro-6H-azocino[2,1-b]quinazolin-13(7H)-ylideneamino)propyl)acetamide
0.000076
-
pH and temperature not specified in the publication Equus caballus (13Z,13'Z)-N,N'-heptane-1,7-diylbis(6,7,8,9,10,11-hexahydro-13H-azocino[2,1-b]quinazolin-13-imine)
0.0000813
-
in 100 mM potassium dihydrogen phosphate buffer, pH 8.0, at 25°C Equus caballus N1-(2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-ylidene)-N4-(3-(2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-ylideneamino)propyl)-N4-methylbutane-1,4-diamine
0.000088
-
pH and temperature not specified in the publication Equus caballus (9E,9'E)-N,N'-hexane-1,6-diylbis(2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-imine)
0.0001221
-
in 100 mM potassium dihydrogen phosphate buffer, pH 8.0, at 25°C Equus caballus 2-acetamido-N-(4-(8,9,10,11-tetrahydro-6H-azocino-[2,1-b]quinazolin-13(7H)-ylideneamino)butyl)-N-(3-(8,9,10,-11-tetrahydro-6H-azocino[2,1-b]quinazolin-13(7H)-ylideneamino)propyl)acetamide
0.000197
-
in 100 mM potassium dihydrogen phosphate buffer, pH 8.0, at 25°C Equus caballus N1-methyl-N3-(8,9,10,11-tetrahydro-6H-azocino[2,1-b]quinazolin-13(7H)-ylidene)-N1-(3-(8,9,10,11-tetrahydro-6Hazocino[2,1-b]quinazolin-13(7H)-ylideneamino)propyl)propane-1,3-diamine
0.000267
-
in 100 mM potassium dihydrogen phosphate buffer, pH 8.0, at 25°C Equus caballus N,N-bis(3-(2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-ylideneamino)propyl) acetamide
0.0005471
-
in 100 mM potassium dihydrogen phosphate buffer, pH 8.0, at 25°C Equus caballus N1-(2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-ylidene)-N3-(3-(2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-ylideneamino)propyl)-N3-methylpropane-1,3-diamine