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Literature summary for 1.1.1.62 extracted from

  • Fischer, D.S.; Allan, G.M.; Bubert, C.; Vicker, N.; Smith, A.; Tutill, H.J.; Purohit, A.; Wood, L.; Packham, G.; Mahon, M.F.; Reed, M.J.; Potter, B.V.
    E-ring modified steroids as novel potent inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (2005), J. Med. Chem., 48, 5749-5770.
    View publication on PubMed
Search for more literature for 1.1.1.62

Inhibitors

Inhibitors Comment Organism Structure
3-hydroxy-1,3,5(10)-triene-[17,16-c]-(5'-carboxylic acid)-pyrazole 0.01 mM: 32% inhibition Homo sapiens
3-hydroxy-1,3,5(10)-triene-[17,16-c]-(5'-hydroxymethyl)-pyrazole 0.01 mM: 94% inhibition, IC50: 0.00095 mM Homo sapiens
3-hydroxy-1,3,5(10)-triene-[17,16-c]-[5'-(carboxylic acid ethyl ester)]-pyrazole 0.01 mM: 94% inhibition, IC50: 0.00185 mM Homo sapiens
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(1'-isobutyl)-pyrazole 0.01 mM: 77% inhibition Homo sapiens
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(1'-methoxyethyl)-pyrazole 0.01 mM: 95% inhibition, IC50: 0.00053 mM Homo sapiens
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(1'-methyl acetate)-pyrazole 0.01 mM: 95% inhibition, IC50: 0.00092 mM Homo sapiens
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(1'-methyl)-pyrazole 0.01 mM: 94% inhibition, IC50: 0.00275 mM Homo sapiens
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(1'-propionitrile)-pyrazole 0.01 mM: 95% inhibition, IC50: 0.00073 mM Homo sapiens
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(2'-isobutyl)-pyrazole 0.01 mM: 70% inhibition Homo sapiens
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(2'-methoxy-ethyl)-pyrazole 0.01 mM: 83% inhibition Homo sapiens
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(2'-methyl acetate)-pyrazole 0.01 mM: 79% inhibition Homo sapiens
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(2'-methyl)-pyrazole 0.01 mM: 43% inhibition Homo sapiens
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(5'-ethylme-thylcarbamoyl)-pyrazole 0.01 mM: 88% inhibition Homo sapiens
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(5'-isopropylcarbamoyl)-pyrazole 0.01 mM: 57% inhibition Homo sapiens
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(5'-methyl)-pyrazole 0.01 mM: 75% inhibition Homo sapiens
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(5'-methyl-carbamoyl)-pyrazole 0.01 mM: 62% inhibition Homo sapiens
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-[5'-(1''-methylpiperazin-4''-ylmethyl)carbamoyl]-pyrazole 0.01 mM: 50% inhibition Homo sapiens
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-[5'-(1'-methylpyrrol-2''-ylmethyl)carbamoyl]-pyrazole 0.01 mM: 89% inhibition, IC50: 0.0023 mM Homo sapiens
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-[5'-(5''-methylpyrazin-2''-ylmethyl)carbamoyl]-pyrazole 0.01 mM: 80% inhibition Homo sapiens
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-[5'-(pyridin-2''-ylmethyl)carbamoyl]-pyrazole 0.01 mM: 93% inhibition, IC50: 0.00088 mM Homo sapiens
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-[5'-(pyridin-3''-ylethyl)carbamoyl]-pyrazole 0.01 mM: 99% inhibition, IC50: 0.0003 mM Homo sapiens
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-[5'-(pyridin-3''-ylmethyl)carbamoyl]-pyrazole 0.01 mM: 92% inhibition, IC50: 0.00078 mM Homo sapiens
3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-[5'-(tetrahydrofuran-2''-ylmethyl)carbamoyl]-pyrazole 0.01 mM: 87% inhibition Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
T-47D cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
estrone + NADPH + H+
-
 Homo sapiens estradiol-17beta + NADP+
-
 ?

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 3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-[5'-(pyridin-3''-ylethyl)carbamoyl]-pyrazole
0.00053
-
 0.01 mM: 95% inhibition, IC50: 0.00053 mM Homo sapiens 3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(1'-methoxyethyl)-pyrazole
0.00073
-
 0.01 mM: 95% inhibition, IC50: 0.00073 mM Homo sapiens 3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(1'-propionitrile)-pyrazole
0.00078
-
 0.01 mM: 92% inhibition, IC50: 0.00078 mM Homo sapiens 3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-[5'-(pyridin-3''-ylmethyl)carbamoyl]-pyrazole
0.00088
-
 0.01 mM: 93% inhibition, IC50: 0.00088 mM Homo sapiens 3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-[5'-(pyridin-2''-ylmethyl)carbamoyl]-pyrazole
0.00092
-
 0.01 mM: 95% inhibition, IC50: 0.00092 mM Homo sapiens 3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(1'-methyl acetate)-pyrazole
0.00095
-
 0.01 mM: 94% inhibition, IC50: 0.00095 mM Homo sapiens 3-hydroxy-1,3,5(10)-triene-[17,16-c]-(5'-hydroxymethyl)-pyrazole
0.00185
-
 0.01 mM: 94% inhibition, IC50: 0.00185 mM Homo sapiens 3-hydroxy-1,3,5(10)-triene-[17,16-c]-[5'-(carboxylic acid ethyl ester)]-pyrazole
0.0023
-
 0.01 mM: 89% inhibition, IC50: 0.0023 mM Homo sapiens 3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-[5'-(1'-methylpyrrol-2''-ylmethyl)carbamoyl]-pyrazole
0.00275
-
 0.01 mM: 94% inhibition, IC50: 0.00275 mM Homo sapiens 3-hydroxy-estra-1,3,5(10)-triene-[17,16-c]-(1'-methyl)-pyrazole