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Literature summary extracted from

  • Szécsi, M.; Ondré, D.; Tóth, I.; Magony, S.; Wölfling, J.; Schneider, G.; Julesz, J.
    Determination of rat 5alpha-reductase type 1 isozyme activity and its inhibition by novel steroidal oxazolines (2010), Acta Biol. Hung., 61, 274-281.
    View publication on PubMed

Application

EC Number Application Comment Organism
1.3.1.22 analysis radiosubstrate in vitro incubation method for the determination of 5alpha-reductase type 1 activity using rat liver microsomes as an enzyme source Rattus norvegicus

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.3.1.22 (5'S)-17beta-(2-chlorophenyl-4,5-dihydrooxazol-5-yl)androst-5-en-3-one
-
 Rattus norvegicus
1.3.1.22 (5'S)-17beta-(4-bromophenyl-4,5-dihydrooxazol-5-yl)androst-5-en-3-one
-
 Rattus norvegicus
1.3.1.22 finasteride
-
 Rattus norvegicus
1.3.99.5 (17beta)-17-[(5S)-2-(2-chlorophenyl)-4,5-dihydro-1,3-oxazol-5-yl]androst-4-en-3-one
-
 Rattus norvegicus
1.3.99.5 (17beta)-17-[(5S)-2-(4-bromophenyl)-4,5-dihydro-1,3-oxazol-5-yl]androst-4-en-3-one
-
 Rattus norvegicus
1.3.99.5 (17beta)-17-[(5S)-2-(4-chlorophenyl)-4,5-dihydro-1,3-oxazol-5-yl]androst-4-en-3-one
-
 Rattus norvegicus
1.3.99.5 (17beta)-17-[(5S)-2-(4-fluorophenyl)-4,5-dihydro-1,3-oxazol-5-yl]androst-4-en-3-one
-
 Rattus norvegicus
1.3.99.5 (17beta)-17-[(5S)-2-(4-nitrophenyl)-4,5-dihydro-1,3-oxazol-5-yl]androst-4-en-3-one
-
 Rattus norvegicus
1.3.99.5 (17beta)-17-[(5S)-2-phenyl-4,5-dihydro-1,3-oxazol-5-yl]androst-4-en-3-one
-
 Rattus norvegicus
1.3.99.5 finasteride
-
 Rattus norvegicus

Organism

EC Number Organism UniProt Comment Textmining
1.3.1.22 Rattus norvegicus
-
 type 1 enzyme
-
1.3.99.5 Rattus norvegicus
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.3.99.5 liver
-
 Rattus norvegicus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.3.99.5 testosterone + NADPH + H+
-
 Rattus norvegicus 5alpha-dihydrotestosterone + NADP+
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.3.99.5 5alpha-reductase type 1
-
 Rattus norvegicus
1.3.99.5 r5alphaR1
-
 Rattus norvegicus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.3.1.22 0.000008
-
 pH 7.3, 37°C Rattus norvegicus finasteride
1.3.1.22 0.00072
-
 pH 7.3, 37°C Rattus norvegicus (5'S)-17beta-(2-chlorophenyl-4,5-dihydrooxazol-5-yl)androst-5-en-3-one
1.3.1.22 0.00105
-
 pH 7.3, 37°C Rattus norvegicus (5'S)-17beta-(4-bromophenyl-4,5-dihydrooxazol-5-yl)androst-5-en-3-one
1.3.99.5 0.000008
-
 37°C Rattus norvegicus finasteride
1.3.99.5 0.00075
-
 37°C Rattus norvegicus (17beta)-17-[(5S)-2-(2-chlorophenyl)-4,5-dihydro-1,3-oxazol-5-yl]androst-4-en-3-one
1.3.99.5 0.00105
-
 37°C Rattus norvegicus (17beta)-17-[(5S)-2-(4-bromophenyl)-4,5-dihydro-1,3-oxazol-5-yl]androst-4-en-3-one
1.3.99.5 0.00109
-
 37°C Rattus norvegicus (17beta)-17-[(5S)-2-(4-chlorophenyl)-4,5-dihydro-1,3-oxazol-5-yl]androst-4-en-3-one
1.3.99.5 0.00118
-
 37°C Rattus norvegicus (17beta)-17-[(5S)-2-phenyl-4,5-dihydro-1,3-oxazol-5-yl]androst-4-en-3-one
1.3.99.5 0.00152
-
 37°C Rattus norvegicus (17beta)-17-[(5S)-2-(4-nitrophenyl)-4,5-dihydro-1,3-oxazol-5-yl]androst-4-en-3-one
1.3.99.5 0.00275
-
 37°C Rattus norvegicus (17beta)-17-[(5S)-2-(4-fluorophenyl)-4,5-dihydro-1,3-oxazol-5-yl]androst-4-en-3-one