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Literature summary for 1.1.1.188 extracted from

  • Liedtke, A.J.; Adeniji, A.O.; Chen, M.; Byrns, M.C.; Jin, Y.; Christianson, D.W.; Marnett, L.J.; Penning, T.M.
    Development of potent and selective indomethacin analogues for the inhibition of AKR1C3 (Type 5 17beta-hydroxysteroid dehydrogenase/prostaglandin F synthase) in castrate-resistant prostate cancer (2013), J. Med. Chem., 56, 2429-2446.
    View publication on PubMedView publication on EuropePMC
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Cloned(Commentary)

Cloned (Comment) Organism
-
 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2-(1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl)-N-((trifluoromethyl)sulfonyl)acetamide 257fold selectivity for isoform AKR1C3 over isoform AKR1C2 Homo sapiens
3-(1-(4-chlorobenzoyl)-3-ethyl-5-methoxy-1H-indol-2-yl)-propanoic acid 540fold selectivity for isoform AKR1C3 over isoform AKR1C2 Homo sapiens
3-(1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl)-propanoic acid 257fold selectivity for isoform AKR1C3 over isoform AKR1C2 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P42330 isoform AKR1C3
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00009
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 3-(1-(4-chlorobenzoyl)-3-ethyl-5-methoxy-1H-indol-2-yl)-propanoic acid
0.00021
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-(1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl )-N-((trifluoromethyl)sulfonyl)acetamide
0.00022
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 3-(1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl)-propanoic acid