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Literature summary for 2.3.1.20 extracted from

  • Mougenot, P.; Namane, C.; Fett, E.; Camy, F.; Dadji-Faihun, R.; Langot, G.; Monseau, C.; Onofri, B.; Pacquet, F.; Pascal, C.; Crespin, O.; Ben-Hassine, M.; Ragot, J.L.; Van-Pham, T.; Philippo, C.; Chatelain-Egger, F.; Peron, P.; Le Bail, J.C.; Guillot, E.; Chamiot-Clerc, P.; Chabanaud, M.A.; Pruniaux, M.-P.; Schmidt, F.; Venier, O.; Nicolai, E.; Viviani, F.
    Thiadiazoles as new inhibitors of diacylglycerol acyltransferase type 1 (2012), Bioorg. Med. Chem. Lett., 22, 2497-2502.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expression in Sf9 cell Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(trans-4-(4-[(5-benzyl-1,3,4-thiadiazol-2-yl)carbamoyl]phenyl)cyclohexyl)acetic acid inhibitor displays good metabolic stability and high intestinal permeability values Homo sapiens
(trans-4-(4-[(5-cyclopentylethyl-1,3,4-thiadiazol-2-yl)carbamoyl]phenyl)cyclohexyl)acetic acid
-
Homo sapiens
(trans-4-(4-[(5-cyclopentylmethyl-1,3,4-thiadiazol-2-yl)carbamoyl]phenyl)cyclohexyl)acetic acid
-
Homo sapiens
(trans-4-(4-[(5-[1-fluorobenzyl]-1,3,4-thiadiazol-2-yl)carbamoyl]phenyl)cyclohexyl)acetic acid inhibitor displays good metabolic stability and high intestinal permeability values Homo sapiens
(trans-4-(4-[(5-[2-chlorobenzyl]-1,3,4-thiadiazol-2-yl)carbamoyl]phenyl)cyclohexyl)acetic acid inhibitor displays good metabolic stability and high intestinal permeability values Homo sapiens
(trans-4-(4-[(5-[2-fluorobenzyl]-1,3,4-thiadiazol-2-yl)carbamoyl]phenyl)cyclohexyl)acetic acid inhibitor displays good metabolic stability and high intestinal permeability values Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Synonyms

Synonyms Comment Organism
DGAT1
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000019
-
pH not specified in the publication, 25°C Homo sapiens (trans-4-(4-[(5-cyclopentylethyl-1,3,4-thiadiazol-2-yl)carbamoyl]phenyl)cyclohexyl)acetic acid
0.000024
-
pH not specified in the publication, 25°C Homo sapiens (trans-4-(4-[(5-cyclopentylmethyl-1,3,4-thiadiazol-2-yl)carbamoyl]phenyl)cyclohexyl)acetic acid
0.00003
-
pH not specified in the publication, 25°C Homo sapiens (trans-4-(4-[(5-[2-fluorobenzyl]-1,3,4-thiadiazol-2-yl)carbamoyl]phenyl)cyclohexyl)acetic acid
0.00003
-
pH not specified in the publication, 25°C Homo sapiens (trans-4-(4-[(5-[2-chlorobenzyl]-1,3,4-thiadiazol-2-yl)carbamoyl]phenyl)cyclohexyl)acetic acid
0.000045
-
pH not specified in the publication, 25°C Homo sapiens (trans-4-(4-[(5-[1-fluorobenzyl]-1,3,4-thiadiazol-2-yl)carbamoyl]phenyl)cyclohexyl)acetic acid
0.00036
-
pH not specified in the publication, 25°C Homo sapiens (trans-4-(4-[(5-benzyl-1,3,4-thiadiazol-2-yl)carbamoyl]phenyl)cyclohexyl)acetic acid