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Literature summary for 3.5.1.2 extracted from

  • Shukla, K.; Ferraris, D.V.; Thomas, A.G.; Stathis, M.; Duvall, B.; Delahanty, G.; Alt, J.; Rais, R.; Rojas, C.; Gao, P.; Xiang, Y.; Dang, C.V.; Slusher, B.S.; Tsukamoto, T.
    Design, synthesis, and pharmacological evaluation of bis-2-(5-phenylacetamido-1,2,4-thiadiazol-2-yl)ethyl sulfide (BPTES) analogs as glutaminase inhibitors (2012), J. Med. Chem., 55, 10551-10563.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.5.1.2

Inhibitors

Inhibitors Comment Organism Structure
(2S)-2-amino-6-imino-5-oxohexanoic acid
-
 Homo sapiens
5,5'-(sulfanediyldiethane-2,1-diyl)bis(1,3,4-thiadiazol-2-amine)
-
 Homo sapiens
5-[3-bromo-4-(dimethylamino)phenyl]-2,2-dimethyl-2,3,5,6-tetrahydrobenzo[a]phenanthridin-4(1H)-one
-
 Homo sapiens
5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]-N-[2-(4-phenylpiperidin-1-yl)ethyl]pentanamide
-
 Homo sapiens
5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]-N-[2-(piperidin-1-yl)ethyl]pentanamide
-
 Homo sapiens
5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]-N-[2-(pyrrolidin-1-yl)ethyl]pentanamide
-
 Homo sapiens
5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]-N-[4-(trifluoromethyl)benzyl]pentanamide
-
 Homo sapiens
bis-2-(5-phenylacetamido-1,2,4-thiadiazol-2-yl)ethyl sulfide
-
 Homo sapiens
N,N'-[sulfanediylbis(ethane-2,1-diyl-1,3,4-thiadiazole-5,2-diyl)]bis(2-phenylacetamide)
-
 Homo sapiens
N-(2-aminoethyl)-5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]pentanamide
-
 Homo sapiens
N-(5-[2-[2-(5-amino-[1,3,4]thiadiazol-2-yl)-ethylsulfanyl]-ethyl]-[1,3,4]thiadiazol-2-yl)-2-phenyl-acetamide
-
 Homo sapiens
N-benzyl-5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]pentanamide
-
 Homo sapiens
N-methyl-5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]-N-[2-(pyrrolidin-1-yl)ethyl]pentanamide
-
 Homo sapiens
N-tert-butyl-5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]pentanamide
-
 Homo sapiens
N-tert-butyl-N-methyl-5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]pentanamide
-
 Homo sapiens
N-[2-(1-methylpyrrolidin-2-yl)ethyl]-5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]pentanamide
-
 Homo sapiens
N-[2-(4-hydroxypiperidin-1-yl)ethyl]-5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]pentanamide
-
 Homo sapiens
N-[2-(diethylamino)ethyl]-5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]pentanamide
-
 Homo sapiens
N-[4-(dimethylamino)benzyl]-5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]pentanamide
-
 Homo sapiens
N-[4-[4-(5-amino-1,3,4-thiadiazol-2-yl)butyl]-1,3-thiazol-2-yl]-2-phenylacetamide
-
 Homo sapiens
N-[5-(2-[[2-(5-amino-1,3,4-thiadiazol-2-yl)ethyl]sulfinyl]ethyl)-1,3,4-thiadiazol-2-yl]-2-phenylacetamide
-
 Homo sapiens
N-[5-[2-(5-amino-1,3,4-thiadiazol-2-yl)ethyl]-1,3,4-thiadiazol-2-yl]-2-phenylacetamide
-
 Homo sapiens
N-[5-[4-(5-amino-1,3,4-thiadiazol-2-yl)butyl]-1,3,4-thiadiazol-2-yl]-2-(4-fluorophenyl)acetamide
-
 Homo sapiens
N-[5-[4-(5-amino-1,3,4-thiadiazol-2-yl)butyl]-1,3,4-thiadiazol-2-yl]-2-(4-methylphenyl)acetamide
-
 Homo sapiens
N-[5-[4-(5-amino-1,3,4-thiadiazol-2-yl)butyl]-1,3,4-thiadiazol-2-yl]-2-cyclohexylacetamide
-
 Homo sapiens
N-[5-[4-(5-amino-1,3,4-thiadiazol-2-yl)butyl]-1,3,4-thiadiazol-2-yl]-2-phenylacetamide
-
 Homo sapiens
N-[5-[4-(5-amino-1,3,4-thiadiazol-2-yl)butyl]-1,3,4-thiadiazol-2-yl]-2-phenylpropanamide
-
 Homo sapiens
N-[5-[4-(5-amino-1,3,4-thiadiazol-2-yl)butyl]-1,3,4-thiadiazol-2-yl]-3-phenylpropanamide
-
 Homo sapiens
N-[5-[4-(5-amino-1,3,4-thiadiazol-2-yl)butyl]-1,3,4-thiadiazol-2-yl]benzamide
-
 Homo sapiens
N-[5-[4-(5-amino-1,3,4-thiadiazol-2-yl)butyl]-1,3-thiazol-2-yl]-2-phenylacetamide
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
L-glutamine + H2O Homo sapiens
-
 L-glutamate + NH3
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens O94925
-
-

Source Tissue

Source Tissue Comment Organism Textmining
kidney
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
L-glutamine + H2O
-
 Homo sapiens L-glutamate + NH3
-
 ?

Synonyms

Synonyms Comment Organism
GLS
-
 Homo sapiens
KGA
-
 Homo sapiens
kidney-type glutaminase
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0014
-
 in 45 mM phosphate buffer (pH 8.2), at 22°C Homo sapiens 5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]-N-[2-(4-phenylpiperidin-1-yl)ethyl]pentanamide
0.0019
-
 in 45 mM phosphate buffer (pH 8.2), at 22°C Homo sapiens N-[5-[4-(5-amino-1,3,4-thiadiazol-2-yl)butyl]-1,3,4-thiadiazol-2-yl]-2-phenylacetamide
0.0026
-
 in 45 mM phosphate buffer (pH 8.2), at 22°C Homo sapiens N-[5-[4-(5-amino-1,3,4-thiadiazol-2-yl)butyl]-1,3,4-thiadiazol-2-yl]-2-(4-fluorophenyl)acetamide
0.0027
-
 in 45 mM phosphate buffer (pH 8.2), at 22°C Homo sapiens N-(5-[2-[2-(5-amino-[1,3,4]thiadiazol-2-yl)-ethylsulfanyl]-ethyl]-[1,3,4]thiadiazol-2-yl)-2-phenyl-acetamide
0.0033
-
 in 45 mM phosphate buffer (pH 8.2), at 22°C Homo sapiens N,N'-[sulfanediylbis(ethane-2,1-diyl-1,3,4-thiadiazole-5,2-diyl)]bis(2-phenylacetamide)
0.0038
-
 in 45 mM phosphate buffer (pH 8.2), at 22°C Homo sapiens N-[2-(4-hydroxypiperidin-1-yl)ethyl]-5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]pentanamide
0.0045
-
 in 45 mM phosphate buffer (pH 8.2), at 22°C Homo sapiens N-[5-[4-(5-amino-1,3,4-thiadiazol-2-yl)butyl]-1,3,4-thiadiazol-2-yl]-2-(4-methylphenyl)acetamide
0.0046
-
 in 45 mM phosphate buffer (pH 8.2), at 22°C Homo sapiens 5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]-N-[2-(pyrrolidin-1-yl)ethyl]pentanamide
0.0052
-
 in 45 mM phosphate buffer (pH 8.2), at 22°C Homo sapiens N-tert-butyl-N-methyl-5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]pentanamide
0.0072
-
 in 45 mM phosphate buffer (pH 8.2), at 22°C Homo sapiens N-[5-[4-(5-amino-1,3,4-thiadiazol-2-yl)butyl]-1,3,4-thiadiazol-2-yl]benzamide
0.0081
-
 in 45 mM phosphate buffer (pH 8.2), at 22°C Homo sapiens N-[2-(1-methylpyrrolidin-2-yl)ethyl]-5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]pentanamide
0.01
-
 IC50 above 0.1 mM, in 45 mM phosphate buffer (pH 8.2), at 22°C Homo sapiens 5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]-N-[2-(piperidin-1-yl)ethyl]pentanamide
0.011
-
 in 45 mM phosphate buffer (pH 8.2), at 22°C Homo sapiens N-tert-butyl-5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]pentanamide
0.012
-
 in 45 mM phosphate buffer (pH 8.2), at 22°C Homo sapiens N-[5-[4-(5-amino-1,3,4-thiadiazol-2-yl)butyl]-1,3,4-thiadiazol-2-yl]-2-phenylpropanamide
0.015
-
 in 45 mM phosphate buffer (pH 8.2), at 22°C Homo sapiens N-[5-[2-(5-amino-1,3,4-thiadiazol-2-yl)ethyl]-1,3,4-thiadiazol-2-yl]-2-phenylacetamide
0.022
-
 in 45 mM phosphate buffer (pH 8.2), at 22°C Homo sapiens N-[5-[4-(5-amino-1,3,4-thiadiazol-2-yl)butyl]-1,3,4-thiadiazol-2-yl]-2-cyclohexylacetamide
0.026
-
 in 45 mM phosphate buffer (pH 8.2), at 22°C Homo sapiens N-[2-(diethylamino)ethyl]-5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]pentanamide
0.048
-
 in 45 mM phosphate buffer (pH 8.2), at 22°C Homo sapiens N-[4-(dimethylamino)benzyl]-5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]pentanamide
0.061
-
 in 45 mM phosphate buffer (pH 8.2), at 22°C Homo sapiens N-[5-(2-[[2-(5-amino-1,3,4-thiadiazol-2-yl)ethyl]sulfinyl]ethyl)-1,3,4-thiadiazol-2-yl]-2-phenylacetamide
0.1
-
 IC50 above 0.1 mM, in 45 mM phosphate buffer (pH 8.2), at 22°C Homo sapiens 5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]-N-[4-(trifluoromethyl)benzyl]pentanamide
0.1
-
 IC50 above 0.1 mM, in 45 mM phosphate buffer (pH 8.2), at 22°C Homo sapiens N-(2-aminoethyl)-5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]pentanamide
0.1
-
 IC50 above 0.1 mM, in 45 mM phosphate buffer (pH 8.2), at 22°C Homo sapiens N-benzyl-5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]pentanamide
0.1
-
 IC50 above 0.1 mM, in 45 mM phosphate buffer (pH 8.2), at 22°C Homo sapiens N-methyl-5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]-N-[2-(pyrrolidin-1-yl)ethyl]pentanamide
0.1
-
 IC50 above 0.1 mM, in 45 mM phosphate buffer (pH 8.2), at 22°C Homo sapiens N-[4-[4-(5-amino-1,3,4-thiadiazol-2-yl)butyl]-1,3-thiazol-2-yl]-2-phenylacetamide
0.1
-
 IC50 above 0.1 mM, in 45 mM phosphate buffer (pH 8.2), at 22°C Homo sapiens N-[5-[4-(5-amino-1,3,4-thiadiazol-2-yl)butyl]-1,3,4-thiadiazol-2-yl]-3-phenylpropanamide
0.1
-
 IC50 above 0.1 mM, in 45 mM phosphate buffer (pH 8.2), at 22°C Homo sapiens N-[5-[4-(5-amino-1,3,4-thiadiazol-2-yl)butyl]-1,3-thiazol-2-yl]-2-phenylacetamide
0.1
-
 in 45 mM phosphate buffer (pH 8.2), at 22°C Homo sapiens 5,5'-(sulfanediyldiethane-2,1-diyl)bis(1,3,4-thiadiazol-2-amine)