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Literature summary for 3.4.24.69 extracted from

  • Opsenica, I.; Tot, M.; Gomba, L.; Nuss, J.; Sciotti, R.; Bavari, S.; Burnett, J.; Solaja, B.
    4-amino-7-chloroquinolines: Probing ligand efficiency provides botulinum neurotoxin serotype a light chain inhibitors with significant antiprotozoal activity (2013), J. Med. Chem., 56, 5860-5871.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.24.69

Inhibitors

Inhibitors Comment Organism Structure
(3alpha,5beta,7alpha,12alpha,17alpha)-24-([2-[(7-chloroquinolin-4-yl)amino]ethyl]amino)cholane-3,7,12-triyl triacetate 90% inhibition at 0.02 mM Clostridium botulinum
bis-aminoquinoline 60% inhibition at 0.02 mM Clostridium botulinum
Chloroquinone 7% inhibition at 0.02 mM Clostridium botulinum
mefloquine 28% inhibition at 0.02 mM Clostridium botulinum
additional information not inhibited by artemisin Clostridium botulinum
N-(4-bromobenzyl)-N'-(7-chloroquinolin-4-yl)ethane-1,2-diamine 69% inhibition at 0.02 mM Clostridium botulinum
N-(4-bromobenzyl)-N'-(7-chloroquinolin-4-yl)propane-1,3-diamine 68% inhibition at 0.02 mM Clostridium botulinum
N-(4-tert-butylbenzyl)-N'-(7-chloroquinolin-4-yl)ethane-1,2-diamine 47% inhibition at 0.02 mM Clostridium botulinum
N-(4-tert-butylbenzyl)-N'-(7-chloroquinolin-4-yl)propane-1,3-diamine 50.28% inhibition at 0.02 mM Clostridium botulinum
N-(7-chloroquinolin-4-yl)-N'-(4-fluorobenzyl)ethane-1,2-diamine 68% inhibition at 0.02 mM Clostridium botulinum
N-(7-chloroquinolin-4-yl)-N'-(4-fluorobenzyl)propane-1,3-diamine 50.09% inhibition at 0.02 mM Clostridium botulinum
N-(7-chloroquinolin-4-yl)-N'-(4-methoxybenzyl)ethane-1,2-diamine 18% inhibition at 0.02 mM Clostridium botulinum
N-(7-chloroquinolin-4-yl)-N'-(4-methoxybenzyl)propane-1,3-diamine 14% inhibition at 0.02 mM Clostridium botulinum
N-(7-chloroquinolin-4-yl)-N'-(pyridin-3-ylmethyl)ethane-1,2-diamine 25% inhibition at 0.02 mM Clostridium botulinum
N-(7-chloroquinolin-4-yl)-N'-(pyridin-3-ylmethyl)propane-1,3-diamine 39.89% inhibition at 0.02 mM Clostridium botulinum
N-(7-chloroquinolin-4-yl)-N'-(pyridin-4-ylmethyl)ethane-1,2-diamine 24% inhibition at 0.02 mM Clostridium botulinum
N-(7-chloroquinolin-4-yl)-N'-(pyridin-4-ylmethyl)propane-1,3-diamine 42.29% inhibition at 0.02 mM Clostridium botulinum
N-(7-chloroquinolin-4-yl)-N'-adamantylethane-1,2-diamine 51.4% inhibition at 0.02 mM Clostridium botulinum
N-(7-chloroquinolin-4-yl)-N'-[(4-methoxypyridin-3-yl)methyl]ethane-1,2-diamine 19% inhibition at 0.02 mM Clostridium botulinum
N-(7-chloroquinolin-4-yl)-N'-[(4-methoxypyridin-3-yl)methyl]propane-1,3-diamine 43.25% inhibition at 0.02 mM Clostridium botulinum
N-benzyl-N'-(7-chloroquinolin-4-yl)ethane-1,2-diamine 52% inhibition at 0.02 mM Clostridium botulinum
N-benzyl-N'-(7-chloroquinolin-4-yl)propane-1,3-diamine 51.83% inhibition at 0.02 mM Clostridium botulinum
N-[(4-chloropyridin-3-yl)methyl]-N'-(7-chloroquinolin-4-yl)ethane-1,2-diamine 23% inhibition at 0.02 mM Clostridium botulinum
N-[(4-chloropyridin-3-yl)methyl]-N'-(7-chloroquinolin-4-yl)propane-1,3-diamine 35.87% inhibition at 0.02 mM Clostridium botulinum

Metals/Ions

Metals/Ions Comment Organism Structure
Zn2+ zinc metalloprotease Clostridium botulinum

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
50000
-
 1 * 100000 + 1 * 50000, SDS-PAGE Clostridium botulinum
100000
-
 1 * 100000 + 1 * 50000, SDS-PAGE Clostridium botulinum

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
SNAP-25 + H2O Clostridium botulinum
-
 ?
-
 ?
synaptobrevin + H2O Clostridium botulinum
-
 ?
-
 ?
Syntaxin + H2O Clostridium botulinum
-
 ?
-
 ?

Organism

Organism UniProt Comment Textmining
Clostridium botulinum P10845
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
SNAP-25 + H2O
-
 Clostridium botulinum ?
-
 ?
synaptobrevin + H2O
-
 Clostridium botulinum ?
-
 ?
Syntaxin + H2O
-
 Clostridium botulinum ?
-
 ?

Subunits

Subunits Comment Organism
heterodimer 1 * 100000 + 1 * 50000, SDS-PAGE Clostridium botulinum

Synonyms

Synonyms Comment Organism
BoNT/A LC
-
 Clostridium botulinum
botulinum neurotoxin serotype A light chain
-
 Clostridium botulinum

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.01
-
 pH and temperature not specified in the publication Clostridium botulinum (3alpha,5beta,7alpha,12alpha,17alpha)-24-([2-[(7-chloroquinolin-4-yl)amino]ethyl]amino)cholane-3,7,12-triyl triacetate
0.0113
-
 at pH 7.3 and 37°C Clostridium botulinum bis-aminoquinoline
0.0189
-
 pH and temperature not specified in the publication Clostridium botulinum N-(7-chloroquinolin-4-yl)-N'-adamantylethane-1,2-diamine