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Literature summary for 1.1.1.62 extracted from

  • Allan, G.M.; Bubert, C.; Vicker, N.; Smith, A.; Tutill, H.J.; Purohit, A.; Reed, M.J.; Potter, B.V.
    Novel, potent inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (2006), Mol. Cell. Endocrinol., 248, 204-207.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(6aS)-2-hydroxy-6a-methyl-N-(2-pyridin-3-ylethyl)-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazole-9-carboxamide 0.01 mM, 99% inhibition, IC50: 0.0003 mM Homo sapiens
(6aS)-2-hydroxy-6a-methyl-N-(pyridin-2-ylmethyl)-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazole-9-carboxamide 0.01 mM, 93% inhibition, IC50: 0.00088 mM Homo sapiens
(6aS)-2-hydroxy-6a-methyl-N-(pyridin-3-ylmethyl)-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazole-9-carboxamide 0.01 mM, 92% inhibition, IC50: 0.00078 mM Homo sapiens
(6aS)-2-hydroxy-6a-methyl-N-[(1-methyl-1H-pyrrol-2-yl)methyl]-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazole-9-carboxamide 0.01 mM, 90% inhibition, IC50: 0.0023 mM Homo sapiens
(6aS)-2-hydroxy-6a-methyl-N-[(5-methylpyrazin-2-yl)methyl]-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazole-9-carboxamide 0.01 mM, 80% inhibition Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P14061
-
-

Source Tissue

Source Tissue Comment Organism Textmining
T47D cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
estrone + NAD(P)H + H+
-
Homo sapiens estradiol + NAD(P)+
-
?

Synonyms

Synonyms Comment Organism
17beta-hydroxysteroid dehydrogenase type 1
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0003
-
0.01 mM, 99% inhibition, IC50: 0.0003 mM Homo sapiens (6aS)-2-hydroxy-6a-methyl-N-(2-pyridin-3-ylethyl)-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazole-9-carboxamide
0.00078
-
0.01 mM, 92% inhibition, IC50: 0.00078 mM Homo sapiens (6aS)-2-hydroxy-6a-methyl-N-(pyridin-3-ylmethyl)-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazole-9-carboxamide
0.00088
-
0.01 mM, 93% inhibition, IC50: 0.00088 mM Homo sapiens (6aS)-2-hydroxy-6a-methyl-N-(pyridin-2-ylmethyl)-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazole-9-carboxamide
0.0023
-
0.01 mM, 90% inhibition, IC50: 0.0023 mM Homo sapiens (6aS)-2-hydroxy-6a-methyl-N-[(1-methyl-1H-pyrrol-2-yl)methyl]-4b,5,6,6a,8,10,10a,10b,11,12-decahydronaphtho[2',1':4,5]indeno[1,2-c]pyrazole-9-carboxamide