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Literature summary for 1.3.1.22 extracted from

  • Picard, F.; Barassin, S.; Mokhtarian, A.; Hartmann, R.W.
    Synthesis and evaluation of 2'-substituted 4-(4'-carboxy- or 4'-carboxymethylbenzylidene)-N-acylpiperidines: highly potent and in vivo active steroid 5alpha-reductase type 2 inhibitors (2002), J. Med. Chem., 45, 3406-3417.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
4-(N-(diphenyl)acetyl-4-piperidinyloxy)benzoic acid pH 5.5, 37°C, BPH tissue, 50% inhibition at 0.0013 mM Homo sapiens
4-(N-(diphenyl)acetyl-4-piperidinyloxy)benzoic acid isoform 1, pH 6.6, 37°C, 62% inhibition at 0.01 mM, isoform 2, pH 5.5, 37°C, 58% inhibition at 0.01 mM Rattus norvegicus
4-(N-(diphenyl)carbamoyl-4-piperidinyloxy)benzoic acid pH 5.5, 37°C, DU145 cells, 10% inhibition at 0.01 mM, BPH tissue, 68% inhibition at 0.01 mM Homo sapiens
4-(N-(diphenyl)carbamoyl-4-piperidinyloxy)benzoic acid isoform 1, pH 6.6, 37°C, 53% inhibition at 0.01 mM, isoform 2, pH 5.5, 37°C, 50% inhibition at 0.01 mM Rattus norvegicus
4-(N-(tert-butyloxycarbonyl)-4-piperidinyloxy)benzoic acid pH 5.5, 37°C, DU145 cells, 2% inhibition at 0.01 mM, BPH tissue, 50% inhibition at 0.0078 mM Homo sapiens
4-(N-(tert-butyloxycarbonyl)-4-piperidinyloxy)benzoic acid isoform 1, pH 6.6, 37°C, 4% inhibition at 0.01 mM, isoform 2, pH 5.5, 37°C, 12% inhibition at 0.01 mM Rattus norvegicus
4-(N-adamantanoyl-4-piperidinyloxy)benzoic acid pH 5.5, 37°C, DU145 cells, 7% inhibition at 0.01 mM, BPH tissue, 50% inhibition at 0.00043 mM Homo sapiens
4-(N-adamantanoyl-4-piperidinyloxy)benzoic acid isoform 1, pH 6.6, 37°C, 18% inhibition at 0.01 mM, isoform 2, pH 5.5, 37°C, 21% inhibition at 0.01 mM Rattus norvegicus
N(dicyclohexyl)acetylpiperidine-4-(2-methoxybenzylidene-4-carboxylic acid) isoform 1, pH 6.6, 37°C, 55% inhibition at 0.01 mM, isoform 2, pH 5.5, 37°C, 43% inhibition at 0.01 mM Rattus norvegicus
N-(1-adamantanoyl)piperdine-4-(2-methoxybenzyliden-4-carboxylic acid) pH 5.5, 37°C, DU145 cells, 10% inhibition at 0.01 mM, BPH tissue, 50% inhibition at 0.0012 mM Homo sapiens
N-(1-adamantanoyl)piperdine-4-(2-methoxybenzyliden-4-carboxylic acid) isoform 1, pH 6.6, 37°C, 50% inhibition at 0.0011 mM, isoform 2, pH 5.5, 37°C, 50% inhibition at 0.0011 mM Rattus norvegicus
N-(1-adamantanoyl)piperidine-4-(2-fluorobenzylidene-4-carboxylic acid) pH 5.5, 37°C, DU145 cells, 20% inhibition at 0.01 mM, BPH tissue, 50% inhibition at 0.00021 mM Homo sapiens
N-(1-adamantanoyl)piperidine-4-(2-fluorobenzylidene-4-carboxylic acid) isoform 1, pH 6.6, 37°C, 52% inhibition at 0.01 mM, isoform 2, pH 5.5, 37°C, 51% inhibition at 0.01 mM Rattus norvegicus
N-(3,3-diphenyl)propanoylpiperidine-4-(benzylidene-4-carboxylic acid) pH 5.5, 37°C, DU145 cells, 8% inhibition at 0.01 mM, BPH tissue, 50% inhibition at 0.0011 mM Homo sapiens
N-(3,3-diphenyl)propanoylpiperidine-4-(benzylidene-4-carboxylic acid) isoform 1, pH 6.6, 37°C, 50% inhibition at 0.0016 mM, isoform 2, pH 5.5, 37°C, 50% inhibition at 0.00088 mM Rattus norvegicus
N-(dicyclohexyl)acetylpiperidine-4-(2-fluorobenzylidene-4-carboxylic acid) pH 5.5, 37°C, DU145 cells, 12% inhibition at 0.01 mM, BPH tissue, 50% inhibition at 0.000011 mM Homo sapiens
N-(dicyclohexyl)acetylpiperidine-4-(2-fluorobenzylidene-4-carboxylic acid) isoform 1, pH 6.6, 37°C, 50% inhibition at 0.0018 mM, isoform 2, pH 5.5, 37°C, 50% inhibition at 0.003 mM Rattus norvegicus
N-(dicyclohexyl)acetylpiperidine-4-(2-methoxybenzylidene-4-carboxylic acid) pH 5.5, 37°C, DU145 cells, 5% inhibition at 0.01 mM, BPH tissue, 50% inhibition at 0.00013 mM Homo sapiens
N-(dicyclohexyl)acetylpiperidine-4-(benzylidene-3-carboxylic acid) pH 5.5, 37°C, BPH tissue, 50% inhibition at 0.0007mM Homo sapiens
N-(dicyclohexyl)acetylpiperidine-4-(benzylidene-3-carboxylic acid) isoform 1, pH 6.6, 37°C, 35% inhibition at 0.01 mM, isoform 2, pH 5.5, 37°C, 25% inhibition at 0.01 mM Rattus norvegicus
N-(dicyclohexyl)acetylpiperidine-4-(benzylidene-4-acetic acid) pH 5.5, 37°C, DU145 cells, 6% inhibition at 0.01 mM, BPH tissue, 50% inhibition at 0.000006 mM Homo sapiens
N-(dicyclohexyl)acetylpiperidine-4-(benzylidene-4-acetic acid) isoform 1, pH 6.6, 37°C, 66% inhibition at 0.01 mM, isoform 2, pH 5.5, 37°C, 56% inhibition at 0.01 mM Rattus norvegicus
N-(dicyclohexyl)acetylpiperidine-4-(benzylidene-4-carboxylic acid) pH 5.5, 37°C, DU145 cells, 46% inhibition at 0.01 mM, BPH tissue, 50% inhibition at 0.00006 mM Homo sapiens
N-(dicyclohexyl)acetylpiperidine-4-(benzylidene-4-carboxylic acid) isoform 1, pH 6.6, 37°C, 51% inhibition at 0.01 mM, isoform 2, pH 5.5, 37°C, 50% inhibition at 0.00008 mM Rattus norvegicus
N-(diphenyl)acetylpiperidine-4-(2-fluorobenzylidene-4-carboxylic acid) pH 5.5, 37°C, DU145 cells, 2% inhibition at 0.01 mM, BPH tissue, 50% inhibition at 0.00041 mM Homo sapiens
N-(diphenyl)acetylpiperidine-4-(2-fluorobenzylidene-4-carboxylic acid) isoform 1, pH 6.6, 37°C, 50% inhibition at 0.0011 mM, isoform 2, pH 5.5, 37°C, 50% inhibition at 0.0011 mM Rattus norvegicus
N-(diphenyl)acetylpiperidine-4-(2-methoxybenzylidene-4-carboxylic acid) pH 5.5, 37°C, DU145 cells, 8% inhibition at 0.01 mM, BPH tissue, 50% inhibition at 0.0035 mM Homo sapiens
N-(diphenyl)acetylpiperidine-4-(2-methoxybenzylidene-4-carboxylic acid) isoform 1, pH 6.6, 37°C, 50% inhibition at 0.0019 mM, isoform 2, pH 5.5, 37°C, 50% inhibition at 0.00094 mM Rattus norvegicus
N-(diphenyl)acetylpiperidine-4-(benzylidene-3-carboxylic acid) pH 5.5, 37°C, DU145 cells, 6% inhibition at 0.01 mM, BPH tissue, 57% inhibition at 0.01 mM Homo sapiens
N-(diphenyl)acetylpiperidine-4-(benzylidene-3-carboxylic acid) isoform 1, pH 6.6, 37°C, 49% inhibition at 0.01 mM, isoform 2, pH 5.5, 37°C, 43% inhibition at 0.01 mM Rattus norvegicus
N-(diphenyl)acetylpiperidine-4-(benzylidene-4-acetic acid) pH 5.5, 37°C, BPH tissue, 50% inhibition at 0.000075 mM Homo sapiens
N-(diphenyl)acetylpiperidine-4-(benzylidene-4-acetic acid) isoform 1, pH 6.6, 37°C, 50% inhibition at 0.0045 mM, isoform 2, pH 5.5, 37°C, 63% inhibition at 0.01 mM Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Homo sapiens
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Rattus norvegicus
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Source Tissue

Source Tissue Comment Organism Textmining
prostate homogenate of Rattus norvegicus
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prostate prostate carcinoma DU145 cells or from benign prostatic hyperplasia patients, BPH Homo sapiens
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