Application | Comment | Organism |
---|---|---|
medicine | inhibitors of the enzyme have potential as treatments for hormone dependent breast cancer | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
1-(3'-ethyl-4'-hydroxy-biphenyl-4-yl)-ethanone | 37°C, 0.01 mM, 51% inhibition, substrate: estradiol-17beta, 7beta-HSD type 2 | Homo sapiens | |
1-(3'-ethyl-4'-hydroxy-biphenyl-4-yl)-ethanone | 37°C, 0.01 mM, 73% inhibition, substrate: estrone, 7beta-HSD type 1 | Homo sapiens | |
1-(3'-ethyl-4'-hydroxy-biphenyl-4-yl)-ethanone | 73% inhibition at 0.001 mM | Homo sapiens | |
1-(3-ethyl-4'-hydroxy-biphenyl-4-yl)-ethanone | 37°C, 0.01 mM, 71% inhibition, substrate: estrone, 7beta-HSD type 1 | Homo sapiens | |
1-(3-ethyl-4'-hydroxy-biphenyl-4-yl)-ethanone | 71% inhibition at 0.001 mM | Homo sapiens | |
1-(4'-hydroxy-2'-methyl-biphenyl-4-yl)-ethanone | 89% inhibition at 0.001 mM | Homo sapiens | |
1-(4'-hydroxy-2'_methyl-biphenyl-4-yl)-ethanone | 37°C, 0.01 mM, 89% inhibition, substrate: estrone, 7beta-HSD type 1 | Homo sapiens | |
1-(4'-hydroxy-biphenyl-4-yl)-ethanone | 37°C, 01 mM, 97% inhibition, substrate: estrone, 7beta-HSD type 1; 97% inhibition at 0.001 mM | Homo sapiens | |
1-(6-hydroxy-9H-fluoren-2-yl)-ethanone | 37°C, 0.01 mM, 86% inhibition, substrate: estrone, 7beta-HSD type 1; 86% inhibition at 0.001 mM | Homo sapiens | |
2-[(16beta)-2-ethyl-3-hydroxy-17-oxoestra-1(10),2,4-trien-16-yl]-N-(pyridin-3-ylmethyl)acetamide | - |
Homo sapiens | |
2-[5-(3-ethyl-4-hydroxyphenyl)-1-oxo-indan-2-yl]-N-pyridin-3-ylmethyl-acetamide | 37°C, 0.001 mM, 39% inhibition, substrate: estrone, 7beta-HSD type 1; 39% inhibition at 0.001 mM | Homo sapiens | |
4-(3'-ethyl-4'-hydroxy-3-methyl-biphenyl)-4-oxo-N-pyridin-3-ylethyl-butyramide | 15% inhibition at 0.001 mM | Homo sapiens | |
4-(3'-ethyl-4'-hydroxy-3-methyl-biphenyl)-4-oxo-N-pyridin-3-ylmethyl-butyramide | 21% inhibition at 0.001 mM; 37°C, 0.001 mM, 21% inhibition, substrate: estrone,7beta-HSD type 1 | Homo sapiens | |
4-(3'-ethyl-4'-hydroxy-biphenyl)-2,2-dimethyl-4-oxo-N-pyridin-3-ylethyl-butyramide | 15% inhibition at 0.001 mM; 37°C, 0.001 mM, 15% inhibition, substrate: estrone, 7beta-HSD type 1 | Homo sapiens | |
4-(3'-ethyl-4'-hydroxy-biphenyl)-2,2-dimethyl-4-oxo-N-pyridin-3-ylmethyl-butyramide | 38% inhibition at 0.001 mM | Homo sapiens | |
4-(3'-ethyl-4'-hydroxy-biphenyl)-4-oxo-N-(2-hydroxyethyl)-butyramide | 23% inhibition at 0.001 mM; 37°C, 0.001 mM, 23% inhibition, substrate: estrone, 7beta-HSD type 1 | Homo sapiens | |
4-(3'-ethyl-4'-hydroxy-biphenyl)-4-oxo-N-pyridin-3-ylethyl-butyramide | 17% inhibition at 0.001 mM; 37°C, 0.001 mM, 17% inhibition, substrate: estrone, 7beta-HSD type 1 | Homo sapiens | |
4-(3'-ethyl-4'-hydroxy-biphenyl)-4-oxo-N-pyridin-3-ylmethyl-butyramide | 24% inhibition at 0.001 mM; 37°C, 0.001 mM, 24% inhibition, substrate: estrone, 7beta-HSD type 1; 37°C, 0.01 mM, 12% inhibition, substrate: estradiol-17beta, 7beta-HSD type 2 | Homo sapiens | |
4-(3'-ethyl-4'-methoxy-biphenyl)-2,2-dimethyl-4-oxo-N-pyridin-3-ylmethyl-butyramide | 17% inhibition at 0.001 mM; 37°C, 0.001 mM, 17% inhibition, substrate: estrone, 7beta-HSD type 1 | Homo sapiens | |
4-(3-ethyl-4-hydroxy-3-methyl-biphenyl)-4-oxo-N-pyridin-3-ylethyl-butyramide | 37°C, 0.001 mM, 15% inhibition, substrate: estrone, 7beta-HSD type 1 | Homo sapiens | |
4-(3-ethyl-4-hydroxy-biphenyl)-2,2-dimethyl-4-oxo-N-pyridin-3-ylmethyl-butyramide | 37°C, 0.001 mM, 38% inhibition, substrate: estrone, 7beta-HSD type 1 | Homo sapiens | |
5-(3-ethyl-4-hydroxyphenyl)-indan-1-one | 37°C, 0.01 mM, 48% inhibition, substrate: estradiol-17beta, 7beta-HSD type 2; 37°C, 0.01 mM, 86% inhibition, substrate: estrone, 7beta-HSD type 1; 86% inhibition at 0.001 mM | Homo sapiens | |
5-(3-fluoro-4-hydroxyphenyl)-indan-1-one | 37°C, 0.01 mM, 24% inhibition, substrate: estradiol-17beta, 7beta-HSD type 2; 37°C, 0.01 mM, 75% inhibition, substrate: estrone, 7beta-HSD type 1; 75% inhibition at 0.001 mM | Homo sapiens | |
5-(3-fluoro-4-methoxyphenyl)-indan-1-one | 37°C, 0.01 mM, 56% inhibition, substrate: estrone, 7beta-HSD type 1; 56% inhibition at 0.001 mM | Homo sapiens | |
5-(4-hydroxyphenyl)-indan-1-one | 37°C, 0.01 mM, 17% inhibition, substrate: estradiol-17beta, 7beta-HSD type 2; 37°C, 0.01 mM, 81% inhibition, substrate: estrone, 7beta-HSD type 1; 81% inhibition at 0.001 mM | Homo sapiens | |
6-(3-ethyl-4-hydroxyphenyl)-3,4-dihydro-2H-naphthalen-1-one | 37°C, 0.01 mM, 51% inhibition, substrate: estrone, 7beta-HSD type 1; 51% inhibition at 0.001 mM | Homo sapiens | |
6-(3-ethyl-4-methoxyphenyl)-3,4-dihydro-2H-naphthalen-1-one | 37°C, 0.01 mM, 71% inhibition, substrate: estrone, 7beta-HSD type 1; 71% inhibition at 0.001 mM | Homo sapiens | |
6-(4-hydroxy-phenyl)-3,4-dihydro-2H-naphthalen-1-one | 37°C, 0.01 mM, 89% inhibition, substrate: estrone, 7beta-HSD type 1; 89% inhibition at 0.001 mM | Homo sapiens | |
additional information | not inhibited by 1-(4'-methoxy-biphenyl-4-yl)-ethanone, 1-(4-benzo[1,3]dioxol-5-yl-phenyl)-ethanone, 1-(3'-ethyl-4'-methoxy-biphenyl-4-yl)-ethanone, 1-(4'-methoxy-2'-methyl-biphenyl-4-yl)-ethanone, 1-(4'-methoxy-2-methyl-biphenyl-4-yl)-ethanone, 1-(4'-hydroxy-2-methyl-biphenyl-4-yl)-ethanone, 1-(7-methoxy-9H-fluoren-2-yl)-ethanone, 5-(4-methoxyphenyl)-indan-1-one, 5-(3-ethyl-4-methoxyphenyl)-indan-1-one, 2,3-dihydro-5-phenylinden-1-one, 6-(4-methoxy-phenyl)-3,4-dihydro-2H-naphthalen-1-one, 4-(3'-ethyl-4'-hydroxy-biphenyl)-4-oxo-N-pyridin-2-ylmethyl-butyramide, 2-[5-(3-ethyl-4-hydroxyphenyl)-1-oxo-indan-2-yl]-N-pyridin-2-ylmethyl-acetamide, and 2-[5-(3-ethyl-4-hydroxyphenyl)-1-oxo-indan-2-yl]-N-(5-methyl-pyrazin-2-ylmethyl)-acetamide | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Homo sapiens | P14061 | - |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
breast cancer cell | - |
Homo sapiens | - |
T-47 cell | breast cancer cell, 7beta-HSD type 1 | Homo sapiens | - |
T-47D cell | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
estradiol-17beta + NAD(P)+ | 7beta-HSD type 2 | Homo sapiens | estrone + NAD(P)H + H+ | - |
? | |
estradiol-17beta + NADP+ | - |
Homo sapiens | estrone + NADPH + H+ | - |
? | |
estrone + NAD(P)H + H+ | 7beta-HSD type 1 | Homo sapiens | estradiol-17beta + NAD(P)+ | - |
? |
Synonyms | Comment | Organism |
---|---|---|
17beta-HSD type 2 | - |
Homo sapiens |
17beta-HSD1 | - |
Homo sapiens |
17beta-hydroxysteroid dehydrogenase type 1 | - |
Homo sapiens |
17beta-hydroxysteroid dehydrogenase type 2 | - |
Homo sapiens |
7beta-HSD type 1 | - |
Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
NADPH | preferentially reductive activity using NADPH as cofactor | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0017 | - |
- |
Homo sapiens | 5-(4-hydroxyphenyl)-indan-1-one | |
0.0018 | - |
- |
Homo sapiens | 4-(3-ethyl-4-hydroxy-biphenyl)-2,2-dimethyl-4-oxo-N-pyridin-3-ylmethyl-butyramide | |
0.0018 | - |
- |
Homo sapiens | 4-(3'-ethyl-4'-hydroxy-biphenyl)-2,2-dimethyl-4-oxo-N-pyridin-3-ylmethyl-butyramide | |
0.002 | - |
- |
Homo sapiens | 5-(3-ethyl-4-hydroxyphenyl)-indan-1-one | |
0.0029 | - |
- |
Homo sapiens | 5-(3-fluoro-4-hydroxyphenyl)-indan-1-one | |
0.0037 | - |
- |
Homo sapiens | 1-(4'-hydroxy-biphenyl-4-yl)-ethanone | |
0.0037 | - |
- |
Homo sapiens | 4-(3'-ethyl-4'-hydroxy-biphenyl)-4-oxo-N-pyridin-3-ylmethyl-butyramide | |
0.0037 | - |
- |
Homo sapiens | 1-(4'-hydroxy-2'_methyl-biphenyl-4-yl)-ethanone | |
0.0037 | - |
- |
Homo sapiens | 1-(4'-hydroxy-2'-methyl-biphenyl-4-yl)-ethanone | |
0.0047 | - |
- |
Homo sapiens | 2-[5-(3-ethyl-4-hydroxyphenyl)-1-oxo-indan-2-yl]-N-pyridin-3-ylmethyl-acetamide | |
0.0048 | - |
- |
Homo sapiens | 1-(6-hydroxy-9H-fluoren-2-yl)-ethanone | |
0.0054 | - |
- |
Homo sapiens | 1-(3'-ethyl-4'-hydroxy-biphenyl-4-yl)-ethanone | |
0.0083 | - |
- |
Homo sapiens | 6-(3-ethyl-4-methoxyphenyl)-3,4-dihydro-2H-naphthalen-1-one | |
0.0099 | - |
- |
Homo sapiens | 1-(3-ethyl-4'-hydroxy-biphenyl-4-yl)-ethanone | |
0.0156 | - |
- |
Homo sapiens | 6-(4-hydroxy-phenyl)-3,4-dihydro-2H-naphthalen-1-one |