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Literature summary extracted from

  • McCarthy, A.R.; Hartmann, R.W.; Abell, A.D.
    Evaluation of 4-substituted bicyclic pyridones as non-steroidal inhibitors of steroid 5alpha-reductase (2007), Bioorg. Med. Chem. Lett., 17, 3603-3607.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.3.1.22 1-methyl-5-(4-(2-phenylacetyl)phenyl)pyridin-2(1H)-one 61% inhibition of type 1 steroid 5alpha reductase at 0.01 mM Homo sapiens
1.3.1.22 2-(16-(acetylthio)hexadecanamido)ethyl 6-(2-(4-(1-methyl-6-oxo-1,6-dihydropyridin-3-yl)phenoxy)acetamido)hex-4-enoate 43% inhibition of type 1 steroid 5alpha reductase at 0.01 mM Homo sapiens
1.3.1.22 2-(2-(16-(acetylthio)hexadecanamido)ethoxy)ethyl 6-(2-(4-(1-methyl-6-oxo-1,6-dihydropyridin-3-yl)phenoxy)acetamido)hex-4-enoate 33% inhibition of type 1 steroid 5alpha reductase at 0.01 mM Homo sapiens
1.3.1.22 finasteride
-
 Homo sapiens
1.3.1.22 additional information no inhibition of type 2 steroid 5alpha reductase at 0.01 mM N,N-diisopropyl-2-(4-(1-methyl-6-oxo-1,6-dihydropyridin-3-yl)phenoxy)acetamide, N-allyl-2-(4-(1-methyl-6-oxo-1,6-dihydropyridin-3-yl)phenoxy)acetamide, N,N-diisopropyl-2-(4-(1-methyl-6-oxopiperidin-3-yl)phenoxy)acetamide, 1-methyl-5-(4-(2-phenylacetyl)phenyl)pyridin-2(1H)-one, N,N-diisopropyl-2-(4-(2-methyl-4-oxo-3,4-dihydropyridin-1(2H)-yl)phenoxy) acetamide, 2-(16-(acetylthio)hexadecanamido)ethyl 6-(2-(4-(1-methyl-6-oxo-1,6-dihydropyridin-3-yl)phenoxy)acetamido)hex-4-enoate, and 2-(2-(16-(acetylthio)hexadecanamido)ethoxy)ethyl 6-(2-(4-(1-methyl-6-oxo-1,6-dihydropyridin-3-yl)phenoxy)acetamido)hex-4-enoate Homo sapiens
1.3.1.22 N,N-diisopropyl-2-(4-(1-methyl-6-oxo-1,6-dihydropyridin-3-yl)phenoxy)acetamide 8% inhibition of type 1 steroid 5alpha reductase at 0.01 mM Homo sapiens
1.3.1.22 N,N-diisopropyl-2-(4-(1-methyl-6-oxopiperidin-3-yl)phenoxy)acetamide 6% inhibition of type 1 steroid 5alpha reductase at 0.01 mM Homo sapiens
1.3.1.22 N,N-diisopropyl-2-(4-(2-methyl-4-oxo-3,4-dihydropyridin-1(2H)-yl)phenoxy)acetamide 3% inhibition of type 1 steroid 5alpha reductase at 0.01 mM Homo sapiens
1.3.1.22 N-allyl-2-(4-(1-methyl-6-oxo-1,6-dihydropyridin-3-yl)phenoxy)acetamide 6% inhibition of type 1 steroid 5alpha reductase at 0.01 mM Homo sapiens
1.3.1.22 N-allyl-2-(4-(2-methyl-4-oxo-3,4-dihydropyridin-1(2H)-yl)phenoxy)acetamide 8% inhibition of type 1 steroid 5alpha reductase at 0.01 mM and 12% inhibition of type 2 steroid 5alpha reductase at 0.01 mM Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
1.3.1.22 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.3.1.22 HEK-293 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.3.1.22 testosterone + NADPH + H+
-
 Homo sapiens 5alpha-dihydrotestosterone + NADP+ + H+
-
 ir

Synonyms

EC Number Synonyms Comment Organism
1.3.1.22 steroid 5alpha-reductase
-
 Homo sapiens
1.3.1.22 type 1 SR
-
 Homo sapiens
1.3.1.22 type 1 steroid 5alpha reductase
-
 Homo sapiens
1.3.1.22 type 2 SR
-
 Homo sapiens
1.3.1.22 type 2 steroid 5alpha reductase
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
1.3.1.22 NADPH dependent Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.3.1.22 0.000025
-
 type 2 steroid 5alpha reductase inhibition Homo sapiens finasteride
1.3.1.22 0.000453
-
 type 1 steroid 5alpha reductase inhibition Homo sapiens finasteride