Application | Comment | Organism |
---|---|---|
drug development | regioisomeric 17beta-N-phenylpyrazolyl steroid derivatives have weak inhibitory effect on 17alpha-hydroxylase/C17,20-lyase | Rattus norvegicus |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
17beta-(1-p-chlorophenyl-3-pyrazolyl)androst-4-en-3-one | 91% relative conversion at 0.05 mM | Rattus norvegicus | |
17beta-(1-p-chlorophenyl-3-pyrazolyl)androst-5-en-3beta-ol | 74% relative conversion at 0.05 mM | Rattus norvegicus | |
17beta-(1-p-chlorophenyl-5-pyrazolyl)androst-4-en-3-one | 78% relative conversion at 0.05 mM | Rattus norvegicus | |
17beta-(1-p-chlorophenyl-5-pyrazolyl)androst-5-en-3beta-ol | - |
Rattus norvegicus | |
17beta-(1-p-cyanophenyl-3-pyrazolyl)androst-4-en-3-one | 34% relative conversion at 0.05 mM | Rattus norvegicus | |
17beta-(1-p-cyanophenyl-3-pyrazolyl)androst-5-en-3beta-ol | - |
Rattus norvegicus | |
17beta-(1-p-cyanophenyl-5-pyrazolyl)androst-4-en-3-one | 69% relative conversio at 0.05 mMn | Rattus norvegicus | |
17beta-(1-p-cyanophenyl-5-pyrazolyl)androst-5-en-3beta-ol | - |
Rattus norvegicus | |
17beta-(1-p-methoxyphenyl-3-pyrazolyl)androst-4-en-3-one | 54% relative conversion at 0.05 mM | Rattus norvegicus | |
17beta-(1-p-methoxyphenyl-3-pyrazolyl)androst-5-en-3beta-ol | 95% relative conversion at 0.05 mM | Rattus norvegicus | |
17beta-(1-p-methoxyphenyl-5-pyrazolyl)androst-4-en-3-one | 91% relative conversion at 0.05 mM | Rattus norvegicus | |
17beta-(1-p-methoxyphenyl-5-pyrazolyl)androst-5-en-3beta-ol | - |
Rattus norvegicus | |
17beta-(1-p-tolyl-3-pyrazolyl)androst-4-en-3-one | 92% relative conversion at 0.05 mM | Rattus norvegicus | |
17beta-(1-p-tolyl-5-pyrazolyl)androst-4-en-3-one | 86% relative conversion at 0.05 mM | Rattus norvegicus | |
17beta-(1-p-tolyl-5-pyrazolyl)androst-5-en-3beta-ol | 89% relative conversion at 0.05 mM | Rattus norvegicus | |
17beta-(1-p-tolylphenyl-3-pyrazolyl)androst-5-en-3beta- | - |
Rattus norvegicus | |
17beta-(1-p-tolylphenyl-3-pyrazolyl)androst-5-en-3beta-ol | 93% relative conversion at 0.05 mM | Rattus norvegicus | |
17beta-(1-p-tolylphenyl-5-pyrazolyl)androst-5-en-3beta- | - |
Rattus norvegicus | |
17beta-(1-phenyl-3-pyrazolyl)androst-4-en-3-one | 86% relative conversion at 0.05 mM | Rattus norvegicus | |
17beta-(1-phenyl-3-pyrazolyl)androst-5-en-3beta-ol | 65% relative conversion at 0.05 mM | Rattus norvegicus | |
17beta-(1-phenyl-5-pyrazolyl)androst-4-en-3-one | 87% relative conversion at 0.05 mM | Rattus norvegicus | |
17beta-(1-phenyl-5-pyrazolyl)androst-5-en-3beta-ol | 92% relative conversion at 0.05 mM | Rattus norvegicus | |
ketoconazole | - |
Rattus norvegicus | |
additional information | C17,20-lyase activity is not inhibited by 0.05 mM 17beta-(1-p-chlorophenyl-3-pyrazolyl)androst-5-en-3beta-ol, 17beta-(1-p-cyanophenyl-3-pyrazolyl)androst-5-en-3beta-ol, 17beta-(1-p-cyanophenyl-5-pyrazolyl)androst-5-en-3beta-ol and 17beta-(1-p-methoxyphenyl-5-pyrazolyl)androst-5-en-3beta-ol; inhibitory effects of synthesized 3beta-hydroxy-17beta-exo-heterocyclic steroids and the corresponding DELTA4-3-ketosteroids on the testicular C17,20-lyase activity are analyzed by an in vitro radioligand incubation technique, overview | Rattus norvegicus |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Rattus norvegicus | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
testis | - |
Rattus norvegicus | - |
Synonyms | Comment | Organism |
---|---|---|
17alpha-hydroxylase/C(17,20)-lyase | - |
Rattus norvegicus |
17alpha-hydroxylase/C17,20-lyase | - |
Rattus norvegicus |
P45017alpha | - |
Rattus norvegicus |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00035 | - |
- |
Rattus norvegicus | ketoconazole | |
0.022 | - |
- |
Rattus norvegicus | 17beta-(1-p-cyanophenyl-3-pyrazolyl)androst-4-en-3-one | |
0.022 | - |
pH and temperature not specified in the publication | Rattus norvegicus | 17beta-(1-p-cyanophenyl-3-pyrazolyl)androst-4-en-3-one | |
0.059 | - |
- |
Rattus norvegicus | 17beta-(1-p-methoxyphenyl-3-pyrazolyl)androst-4-en-3-one | |
0.059 | - |
pH and temperature not specified in the publication | Rattus norvegicus | 17beta-(1-phenyl-5-pyrazolyl)androst-4-en-3-one |