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Literature summary for 1.3.99.5 extracted from

  • Salem, O.I.; Frotscher, M.; Scherer, C.; Neugebauer, A.; Biemel, K.; Streiber, M.; Maas, R.; Hartmann, R.W.
    Novel 5alpha-reductase inhibitors: synthesis, structure-activity studies, and pharmacokinetic profile of phenoxybenzoylphenyl acetic acids (2006), J. Med. Chem., 49, 748-759.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(4-[4-(4-bromophenoxy)benzoyl]phenyl)acetic acid pH 5.5, 55% inhibition at 0.01 mM, pH 6.6, 59% inhibition at 0.01 mM Rattus norvegicus
3-[4-(4-phenoxybenzoyl)phenyl]acrylic acid pH 5.5, isoform 2, 50% inhibition at 0.00047 mM, not inhibitory to isoform 1 Homo sapiens
3-[4-(4-phenoxybenzoyl)phenyl]acrylic acid pH 5.5, 63% inhibition at 0.01 mM, pH 6.6, 61% inhibition at 0.01 mM Rattus norvegicus
4-(4-([2,6-bis(trifluoromethyl)benzyl]oxy)benzoyl)benzoic acid pH 5.5, 29% inhibition at 0.01 mM, pH 6.6, 69% inhibition at 0.01 mM Rattus norvegicus
4-(4-phenoxybenzoyl)benzoic acid pH 5.5, isoform 2, 50% inhibition at 0.000053 mM, not inhibitory to isoform 1 Homo sapiens
4-(4-phenoxybenzoyl)benzoic acid pH 5.5, 33% inhibition at 0.01 mM, pH 6.6, 53% inhibition at 0.01 mM Rattus norvegicus
4-(4-[[2,6-bis(trifluoromethyl)benzyl]oxy]benzoyl)benzoic acid pH 5.5, isoform 2, 50% inhibition at 0.000113 mM, isoform 1, 12% inhibition at 0.01 mM Homo sapiens
4-[3-(benzyloxy)benzoyl]benzoic acid pH 5.5, isoform 2, 50% inhibition at 0.000131 mM, not inhibitory to isoform 1 Homo sapiens
4-[3-(benzyloxy)benzoyl]benzoic acid pH 5.5, 55% inhibition at 0.01 mM, pH 6.6, 35% inhibition at 0.01 mM Rattus norvegicus
4-[4-(benzyloxy)benzoyl]benzoic acid pH 5.5, isoform 2, 50% inhibition at 0.000119 mM, not inhibitory to isoform 1 Homo sapiens
4-[4-(benzyloxy)benzoyl]benzoic acid pH 5.5, 0.01 mM, 45% inhibition at 0.01 mM, pH 6.6, 64% inhibition at 0.01 mM Rattus norvegicus
finasteride pH 5.5, isoform 2, 50% inhibition at 0.000005 mM, isoform 1, 50% inhibition at 0.051 mM Homo sapiens
finasteride pH 5.5, 50% inhibition at 0.000011 mM, pH 6.6, 50% inhibition at 0.00001 mM Rattus norvegicus
[3-fluoro-4-(4-phenoxybenzoyl)phenyl]acetic acid pH 5.5, isoform 2, 50% inhibition at 0.000045 mM, not inhibitory to isoform 1 Homo sapiens
[3-fluoro-4-(4-phenoxybenzoyl)phenyl]acetic acid pH 5.5, 73% inhibition at 0.01 mM, pH 6.6, 57% inhibition at 0.01 mM Rattus norvegicus
[3-methyl-4-(4-phenoxybenzoyl)phenyl]acetic acid pH 5.5, isoform 2, 50% inhibition at 0.000027 mM, not inhibitory to isoform 1 Homo sapiens
[3-methyl-4-(4-phenoxybenzoyl)phenyl]acetic acid pH 5.5, 78% inhibition at 0.01 mM, pH 6.6, 50% inhibition at 0.00145 mM Rattus norvegicus
[4-(4-phenoxybenzoyl)phenyl]acetic acid pH 5.5, isoform 2, 50% inhibition at 0.000023 mM, not inhibitory to isoform 1 Homo sapiens
[4-(4-phenoxybenzoyl)phenyl]acetic acid pH 5.5, 77% inhibition at 0.01 mM, pH 6.6, 42% inhibition at 0.01 mM Rattus norvegicus
[4-[4-(4-bromophenoxy)benzoyl]phenyl]acetic acid pH 5.5, isoform 2, 50% inhibition at 0.000005 mM, not inhibitory to isoform 1 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
isoforms 1 and 2
-
Rattus norvegicus
-
isoforms 1 and 2
-

Source Tissue

Source Tissue Comment Organism Textmining
prostate
-
Homo sapiens
-
prostate gland ventral prostate Rattus norvegicus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1-androstene-3,17-dione + acceptor
-
Homo sapiens 1,4-androstadiene-3,17-dione + reduced reduced acceptor
-
?
testosterone + reduced acceptor
-
Homo sapiens 5alpha-dihydrotestosterone + acceptor
-
?
testosterone + reduced acceptor
-
Rattus norvegicus 5alpha-dihydrotestosterone + acceptor
-
?