Crystallization (Comment) | Organism |
---|---|
NADP+ and 2'-des-methyl-indomethacin is determined at a resolution of 1.8 A by molecular replacement. The cofactor binding cavity of AKR1C3 is not perturbed upon binding of the inhibitor | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(4-chlorophenyl)(5-methoxy-2-methyl-1H-indol-1-yl)methanone | - |
Homo sapiens | |
2'-des-methyl-indomethacin | the cofactor binding cavity of AKR1C3 is not perturbed upon binding of the inhibitor | Homo sapiens | |
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(2-methylbenzene-1-sulfonyl)acetamide | - |
Homo sapiens | |
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(4-cyanobenzene-1-sulfonyl)acetamide | - |
Homo sapiens | |
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(4-fluorobenzene-1-sulfonyl)acetamide | - |
Homo sapiens | |
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(4-methoxybenzene-1-sulfonyl)acetamide | - |
Homo sapiens | |
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(4-methylbenzene-1-sulfonyl)acetamide | - |
Homo sapiens | |
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(4-phenoxybenzene-1-sulfonyl)acetamide | - |
Homo sapiens | |
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(5-chlorothiophene-2-sulfonyl)acetamide | - |
Homo sapiens | |
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(methanesulfonyl)acetamide | - |
Homo sapiens | |
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(naphthalene-2-sulfonyl)acetamide | - |
Homo sapiens | |
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(trifluoromethanesulfonyl)acetamide | - |
Homo sapiens | |
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-[3-(trifluoromethyl)benzene-1-sulfonyl]acetamide | - |
Homo sapiens | |
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-[4-(propan-2-yl)benzene-1-sulfonyl]acetamide | - |
Homo sapiens | |
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-[4-(trifluoromethyl)benzene-1-sulfonyl]acetamide | - |
Homo sapiens | |
2-[1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]-N-(trifluoromethanesulfonyl)acetamide | - |
Homo sapiens | |
3-(3,4-dihydroisoquinolin-2(1H)-ylsulfonyl)benzoate | - |
Homo sapiens | |
3-(5-methoxy-2-methyl-1H-indol-3-yl)propanoic acid | - |
Homo sapiens | |
3-(phenylamino)benzoic acid | - |
Homo sapiens | |
3-[1-(4-chlorobenzoyl)-2-ethyl-5-methoxy-1H-indol-3-yl]propanoic acid | - |
Homo sapiens | |
3-[1-(4-chlorobenzoyl)-3-ethyl-5-methoxy-1H-indol-2-yl]propanoic acid | - |
Homo sapiens | |
3-[1-(4-chlorobenzoyl)-5-fluoro-2-methyl-1H-indol-3-yl]propanoic acid | - |
Homo sapiens | |
3-[1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]propanoic acid | - |
Homo sapiens | |
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid | - |
Homo sapiens | |
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-2-methylpropanoic acid | - |
Homo sapiens | |
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(2-methylbenzene-1-sulfonyl)propanamide | - |
Homo sapiens | |
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(4-methylbenzene-1-sulfonyl)propanamide | - |
Homo sapiens | |
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(5-chlorothiophene-2-sulfonyl)propanamide | - |
Homo sapiens | |
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(methanesulfonyl)-2-methylpropanamide | - |
Homo sapiens | |
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(methanesulfonyl)propanamide | - |
Homo sapiens | |
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(naphthalene-2-sulfonyl)propanamide | - |
Homo sapiens | |
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(trifluoromethanesulfonyl)propanamide | - |
Homo sapiens | |
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-[4-(propan-2-yl)benzene-1-sulfonyl]propanamide | - |
Homo sapiens | |
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-[4-(trifluoromethoxy)benzene-1-sulfonyl]propanamide | - |
Homo sapiens | |
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-[4-(trifluoromethyl)benzene-1-sulfonyl]propanamide | - |
Homo sapiens | |
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]propanoic acid | - |
Homo sapiens | |
4-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]butanoic acid | - |
Homo sapiens | |
5-methoxy-3-(2-oxobutyl)-1H-indole-1-carboxylic acid | - |
Homo sapiens | |
6-methoxy-9-[3-(trifluoromethyl)benzoyl]-2,3,4,9-tetrahydro-1H-carbazole-3-carboxylic acid | - |
Homo sapiens | |
9-(4-chlorobenzoyl)-6-methoxy-2,3,4,9-tetrahydro-1H-carbazole-2-carboxylic acid | - |
Homo sapiens | |
9-(4-chlorobenzoyl)-6-methoxy-2,3,4,9-tetrahydro-1H-carbazole-3-carboxylic acid | - |
Homo sapiens | |
9-(4-chlorobenzoyl)-N-(methanesulfonyl)-6-methoxy-2,3,4,9-tetrahydro-1H-carbazole-3-carboxamide | - |
Homo sapiens | |
baccharin | - |
Homo sapiens | |
indomethacin | - |
Homo sapiens | |
methyl 5-methoxy-3-(2-oxobutyl)-1H-indole-1-carboxylate | - |
Homo sapiens | |
methyl [1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]acetate | - |
Homo sapiens | |
methyl [1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]acetate | - |
Homo sapiens | |
methyl [5-methoxy-1-(4-methoxybenzoyl)-2-methyl-1H-indol-3-yl]acetate | - |
Homo sapiens | |
methyl [5-methoxy-2-methyl-1-(4-methylbenzoyl)-1H-indol-3-yl]acetate | - |
Homo sapiens | |
additional information | development of potent and selective indomethacin analogues for the inhibition of AKR1C3 in castrate-resistant prostate cancer, overview. Increasing the length of the aliphatic side chain of indomethacin from -ethyl to -propyl leads to a 2fold reduction in AKR1C3 potency, but the compound retained 257fold selectivity for AKR1C3 over AKR1C2 | Homo sapiens | |
N-(4-acetylbenzene-1-sulfonyl)-2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]acetamide | - |
Homo sapiens | |
N-(4-acetylbenzene-1-sulfonyl)-3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]propanamide | - |
Homo sapiens | |
N-(4-bromobenzene-1-sulfonyl)-2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]acetamide | - |
Homo sapiens | |
N-(4-chlorobenzoyl)-melatonin | - |
Homo sapiens | |
N-benzoylanthranilic acid | - |
Homo sapiens | |
N-[2,5-bis(trifluoromethyl)benzene-1-sulfonyl]-2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]acetamide | - |
Homo sapiens | |
thiazolidinedione | - |
Homo sapiens | |
[1-(4-chlorobenzoyl)-5-fluoro-1H-indol-3-yl]acetic acid | - |
Homo sapiens | |
[1-(4-chlorobenzoyl)-5-fluoro-2-methyl-1H-indol-3-yl]acetic acid | - |
Homo sapiens | |
[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]acetic acid | - |
Homo sapiens | |
[1-(4-chlorobenzoyl)-5-methoxy-2-propyl-1H-indol-3-yl]acetic acid | - |
Homo sapiens | |
[1-(4-fluorobenzoyl)-5-methoxy-1H-indol-3-yl]acetic acid | - |
Homo sapiens | |
[1-(4-fluorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]acetic acid | - |
Homo sapiens | |
[1-[4-(chloromethyl)benzoyl]-5-methoxy-2-methyl-1H-indol-3-yl]acetic acid | - |
Homo sapiens | |
[5-fluoro-2-methyl-1-[3-(trifluoromethyl)benzoyl]-1H-indol-3-yl]acetic acid | - |
Homo sapiens | |
[5-methoxy-1-(4-methoxybenzoyl)-2-methyl-1H-indol-3-yl]acetic acid | - |
Homo sapiens | |
[5-methoxy-1-[3-(trifluoromethyl)benzoyl]-1H-indol-3-yl]acetic acid | - |
Homo sapiens | |
[5-methoxy-1-[4-(trifluoromethyl)benzoyl]-1H-indol-3-yl]acetic acid | - |
Homo sapiens | |
[5-methoxy-2-methyl-1-(4-methylbenzoyl)-1H-indol-3-yl]acetic acid | - |
Homo sapiens | |
[5-methoxy-2-methyl-1-[3-(trifluoromethyl)benzoyl]-1H-indol-3-yl]acetic acid | - |
Homo sapiens | |
[5-methoxy-2-methyl-1-[4-(trifluoromethyl)benzoyl]-1H-indol-3-yl]acetic acid | - |
Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
testosterone + NAD+ | Homo sapiens | the enzyme shows LNCaP-AKR1C3 mediates formation of testosterone, conversion of 4-androstene-3,17-dione to testosterone | androstenedione + NADH + H+ | - |
r |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P42330 | - |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
LNCaP cell | - |
Homo sapiens | - |
prostate cancer cell | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
testosterone + NAD+ | - |
Homo sapiens | androstenedione + NADH + H+ | - |
r | |
testosterone + NAD+ | the enzyme shows LNCaP-AKR1C3 mediates formation of testosterone, conversion of 4-androstene-3,17-dione to testosterone | Homo sapiens | androstenedione + NADH + H+ | - |
r |
Synonyms | Comment | Organism |
---|---|---|
AKR1C3 | - |
Homo sapiens |
More | cf. EC 1.1.1.357 | Homo sapiens |
type 5 17beta-hydroxysteroid dehydrogenase/prostaglandin F synthase | - |
Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
NAD+ | - |
Homo sapiens | |
NADH | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00007 | - |
110 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 3-[1-(4-chlorobenzoyl)-3-ethyl-5-methoxy-1H-indol-2-yl]propanoic acid | |
0.00007 | - |
111 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | [1-(4-chlorobenzoyl)-5-methoxy-2-propyl-1H-indol-3-yl]acetic acid | |
0.00009 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 3-[1-(4-chlorobenzoyl)-3-ethyl-5-methoxy-1H-indol-2-yl]propanoic acid | |
0.0001 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | indomethacin | |
0.00012 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | [1-[4-(chloromethyl)benzoyl]-5-methoxy-2-methyl-1H-indol-3-yl]acetic acid | |
0.00012 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid | |
0.00013 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]propanoic acid | |
0.00014 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | [5-methoxy-1-(4-methoxybenzoyl)-2-methyl-1H-indol-3-yl]acetic acid | |
0.00015 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 3-[1-(4-chlorobenzoyl)-2-ethyl-5-methoxy-1H-indol-3-yl]propanoic acid | |
0.00015 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 4-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]butanoic acid | |
0.00016 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | [5-methoxy-2-methyl-1-(4-methylbenzoyl)-1H-indol-3-yl]acetic acid | |
0.00016 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 9-(4-chlorobenzoyl)-6-methoxy-2,3,4,9-tetrahydro-1H-carbazole-3-carboxylic acid | |
0.00021 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(trifluoromethanesulfonyl)acetamide | |
0.00022 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 3-[1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]propanoic acid | |
0.00025 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | [1-(4-chlorobenzoyl)-5-fluoro-2-methyl-1H-indol-3-yl]acetic acid | |
0.00027 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | [5-methoxy-2-methyl-1-[4-(trifluoromethyl)benzoyl]-1H-indol-3-yl]acetic acid | |
0.000279 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 6-methoxy-9-[3-(trifluoromethyl)benzoyl]-2,3,4,9-tetrahydro-1H-carbazole-3-carboxylic acid | |
0.00029 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 3-[1-(4-chlorobenzoyl)-5-fluoro-2-methyl-1H-indol-3-yl]propanoic acid | |
0.00029 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-2-methylpropanoic acid | |
0.00034 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(methanesulfonyl)propanamide | |
0.00034 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 9-(4-chlorobenzoyl)-6-methoxy-2,3,4,9-tetrahydro-1H-carbazole-2-carboxylic acid | |
0.0005 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | [1-(4-chlorobenzoyl)-5-fluoro-1H-indol-3-yl]acetic acid | |
0.00071 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | [1-(4-fluorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]acetic acid | |
0.00074 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 2-[1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]-N-(trifluoromethanesulfonyl)acetamide | |
0.00096 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | [1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]acetic acid | |
0.00108 | - |
110 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | [5-methoxy-1-[4-(trifluoromethyl)benzoyl]-1H-indol-3-yl]acetic acid | |
0.00111 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(4-cyanobenzene-1-sulfonyl)acetamide | |
0.00111 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-[4-(trifluoromethyl)benzene-1-sulfonyl]propanamide | |
0.00119 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(naphthalene-2-sulfonyl)acetamide | |
0.00144 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(trifluoromethanesulfonyl)propanamide | |
0.00194 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | N-[2,5-bis(trifluoromethyl)benzene-1-sulfonyl]-2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]acetamide | |
0.00207 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-[4-(trifluoromethyl)benzene-1-sulfonyl]acetamide | |
0.00209 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | N-(4-acetylbenzene-1-sulfonyl)-2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]acetamide | |
0.00223 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | [5-fluoro-2-methyl-1-[3-(trifluoromethyl)benzoyl]-1H-indol-3-yl]acetic acid | |
0.00224 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | methyl [5-methoxy-1-(4-methoxybenzoyl)-2-methyl-1H-indol-3-yl]acetate | |
0.0024 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 5-methoxy-3-(2-oxobutyl)-1H-indole-1-carboxylic acid | |
0.00244 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | [5-methoxy-2-methyl-1-[3-(trifluoromethyl)benzoyl]-1H-indol-3-yl]acetic acid | |
0.0025 | - |
110 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-[4-(trifluoromethoxy)benzene-1-sulfonyl]propanamide | |
0.00252 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(4-phenoxybenzene-1-sulfonyl)acetamide | |
0.00254 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(naphthalene-2-sulfonyl)propanamide | |
0.00265 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-[3-(trifluoromethyl)benzene-1-sulfonyl]acetamide | |
0.00265 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | N-(4-acetylbenzene-1-sulfonyl)-3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]propanamide | |
0.00311 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(4-methylbenzene-1-sulfonyl)propanamide | |
0.00325 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(2-methylbenzene-1-sulfonyl)propanamide | |
0.00356 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | (4-chlorophenyl)(5-methoxy-2-methyl-1H-indol-1-yl)methanone | |
0.00373 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(5-chlorothiophene-2-sulfonyl)acetamide | |
0.00397 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | N-(4-bromobenzene-1-sulfonyl)-2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]acetamide | |
0.00469 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-[4-(propan-2-yl)benzene-1-sulfonyl]propanamide | |
0.00496 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | [1-(4-fluorobenzoyl)-5-methoxy-1H-indol-3-yl]acetic acid | |
0.00507 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 9-(4-chlorobenzoyl)-N-(methanesulfonyl)-6-methoxy-2,3,4,9-tetrahydro-1H-carbazole-3-carboxamide | |
0.00521 | - |
111 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | [5-methoxy-1-[3-(trifluoromethyl)benzoyl]-1H-indol-3-yl]acetic acid | |
0.00553 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(methanesulfonyl)-2-methylpropanamide | |
0.00564 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | methyl [1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]acetate | |
0.0058 | - |
111 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(4-methoxybenzene-1-sulfonyl)acetamide | |
0.00634 | - |
110 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-[4-(propan-2-yl)benzene-1-sulfonyl]acetamide | |
0.00754 | - |
110 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | methyl [5-methoxy-2-methyl-1-(4-methylbenzoyl)-1H-indol-3-yl]acetate | |
0.00759 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | methyl [5-methoxy-1-(4-methoxybenzoyl)-2-methyl-1H-indol-3-yl]acetate | |
0.00786 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(4-fluorobenzene-1-sulfonyl)acetamide | |
0.00882 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(2-methylbenzene-1-sulfonyl)acetamide | |
0.01134 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | methyl [1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]acetate | |
0.012 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(methanesulfonyl)acetamide | |
0.0124 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(4-methylbenzene-1-sulfonyl)acetamide | |
0.01571 | - |
111 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | methyl [5-methoxy-2-methyl-1-(4-methylbenzoyl)-1H-indol-3-yl]acetate | |
0.02278 | - |
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | methyl 5-methoxy-3-(2-oxobutyl)-1H-indole-1-carboxylate | |
0.1 | - |
above, 100 mM Tris-HCl buffer, 37°C, pH not specified in the publication | Homo sapiens | 3-(5-methoxy-2-methyl-1H-indol-3-yl)propanoic acid |
General Information | Comment | Organism |
---|---|---|
additional information | the structure of the AKR1C3-NADP+ complex is solved by molecular replacement, overview | Homo sapiens |
physiological function | AKR1C3 catalyzes the conversion of the weak androgen precursors 4-androstene-3,17-dione and 5alpha-androstane-3,17-dione to the potent androgens testosterone and 5alpha-dihydrotestosterone (DHT), respectively, and is one of the most highly upregulated genes in castrate-resistant prostate cancer, CRPC | Homo sapiens |