Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 1.3.1.22 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
Search for more literature for 1.3.1.22

Inhibitors

Inhibitors Comment Organism Structure
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
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
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
finasteride
-
 Homo sapiens
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
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
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
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
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
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

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HEK-293 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

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

Synonyms

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

Cofactor

Cofactor Comment Organism Structure
NADPH dependent Homo sapiens

IC50 Value

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