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Literature summary for 1.1.1.64 extracted from

  • Adeniji, A.O.; Twenter, B.M.; Byrns, M.C.; Jin, Y.; Winkler, J.D.; Penning, T.M.
    Discovery of substituted 3-(phenylamino)benzoic acids as potent and selective inhibitors of type 5 17beta-hydroxysteroid dehydrogenase (AKR1C3) (2011), Bioorg. Med. Chem. Lett., 21, 1464-1468.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
3-[(4-nitrophenyl)amino]benzoic acid 94fold selectivity for the inhibition of isoform AKR1C3 over AKR1C2 Homo sapiens
3-[[4-(methoxymethyl)phenyl]amino]benzoic acid 360fold selectivity for the inhibition of isoform AKR1C3 over AKR1C2 Homo sapiens
3-[[4-(trifluoromethyl)phenyl]amino]benzoic acid 250fold selectivity for the inhibition of isoform AKR1C3 over AKR1C2 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P42330
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
(S)-tetralol + NADP+
-
Homo sapiens ? + NADPH
-
?

Synonyms

Synonyms Comment Organism
AKR1C3
-
Homo sapiens
type 5 beta-hydroxysteroid dehydrogenase
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000036
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 3-[(4-nitrophenyl)amino]benzoic acid
0.000054
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 3-[[4-(methoxymethyl)phenyl]amino]benzoic acid
0.000062
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 3-[[4-(trifluoromethyl)phenyl]amino]benzoic acid