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Literature summary for 1.14.99.1 extracted from
- Novel N-substituted 5-aminosalicylamides as dual inhibitors of cyclooxygenase and 5-lipoxygenase enzymes Synthesis, biological evaluation and docking study (2018), Bioorg. Chem., 78, 80-93 .
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 5-amino-2-hydroxy-N-(propan-2-yl)benzamide | 5-aminosalicylic acid derivative, additionally inhibits lipoxygenase Lox-5. 7.6fold selectivity for isoform Cox-2 over Cox-1 | Homo sapiens | |
| 5-amino-2-hydroxy-N-(propan-2-yl)benzamide | 5-aminosalicylic acid derivative, additionally inhibits lipoxygenase Lox-5. 7.6fold selectivity for isoform Cox-2 over Cox-1 | Ovis aries | |
| 5-amino-N-cyclohexyl-2-hydroxybenzamide | 5-aminosalicylic acid derivative, additionally inhibits lipoxygenase Lox-5. 44fold selectivity for isoform Cox-2 over Cox-1 | Homo sapiens | |
| 5-amino-N-cyclohexyl-2-hydroxybenzamide | 5-aminosalicylic acid derivative, additionally inhibits lipoxygenase Lox-5. 44fold selectivity for isoform Cox-2 over Cox-1 | Ovis aries | |
| 5-amino-N-hexyl-2-hydroxybenzamide | 5-aminosalicylic acid derivative, additionally inhibits lipoxygenase Lox-5. 44fold selectivity for isoform Cox-2 over Cox-1 | Homo sapiens | |
| 5-amino-N-hexyl-2-hydroxybenzamide | 5-aminosalicylic acid derivative, additionally inhibits lipoxygenase Lox-5. 44fold selectivity for isoform Cox-2 over Cox-1 | Ovis aries | |
| 5-[[(2,5-dihydroxyphenyl)methyl]amino]-2-hydroxy-N-(4-methylphenyl)benzamide | 5-aminosalicylic acid derivative, additionally inhibits lipoxygenase Lox-5. 29.7fold selectivity for isoform Cox-2 over Cox-1 | Homo sapiens | |
| 5-[[(2,5-dihydroxyphenyl)methyl]amino]-2-hydroxy-N-(4-methylphenyl)benzamide | 5-aminosalicylic acid derivative, additionally inhibits lipoxygenase Lox-5. 29.7fold selectivity for isoform Cox-2 over Cox-1 | Ovis aries | |
| indomethacin | - |
Homo sapiens |  |
| indomethacin | - |
Ovis aries | |
| N-butyl-5-[[(2,5-dihydroxyphenyl)methyl]amino]-2-hydroxybenzamide | 5-aminosalicylic acid derivative, additionally inhibits lipoxygenase Lox-5. 135fold selectivity for isoform Cox-2 over Cox-1 | Homo sapiens | |
| N-butyl-5-[[(2,5-dihydroxyphenyl)methyl]amino]-2-hydroxybenzamide | 5-aminosalicylic acid derivative, additionally inhibits lipoxygenase Lox-5. 135fold selectivity for isoform Cox-2 over Cox-1 | Ovis aries | |
| N-cyclohexyl-5-[(E)-[(2,5-dihydroxyphenyl)methylidene]amino]-2-hydroxybenzamide | 5-aminosalicylic acid derivative, additionally inhibits lipoxygenase Lox-5. 120fold selectivity for isoform Cox-2 over Cox-1 | Homo sapiens | |
| N-cyclohexyl-5-[(E)-[(2,5-dihydroxyphenyl)methylidene]amino]-2-hydroxybenzamide | 5-aminosalicylic acid derivative, additionally inhibits lipoxygenase Lox-5. 120fold selectivity for isoform Cox-2 over Cox-1 | Ovis aries | |
| N-cyclohexyl-5-[[(2,5-dihydroxyphenyl)methyl]amino]-2-hydroxybenzamide | 5-aminosalicylic acid derivative, additionally inhibits lipoxygenase Lox-5. 114fold selectivity for isoform Cox-2 over Cox-1 | Homo sapiens | |
| N-cyclohexyl-5-[[(2,5-dihydroxyphenyl)methyl]amino]-2-hydroxybenzamide | 5-aminosalicylic acid derivative, additionally inhibits lipoxygenase Lox-5. 114fold selectivity for isoform Cox-2 over Cox-1 | Ovis aries | |
| N-hexyl-5-[[(2,5-dihydroxyphenyl)methyl]amino]-2-hydroxybenzamide | 5-aminosalicylic acid derivative, additionally inhibits lipoxygenase Lox-5. 145fold selectivity for isoform Cox-2 over Cox-1 | Homo sapiens | |
| N-hexyl-5-[[(2,5-dihydroxyphenyl)methyl]amino]-2-hydroxybenzamide | 5-aminosalicylic acid derivative, additionally inhibits lipoxygenase Lox-5. 145fold selectivity for isoform Cox-2 over Cox-1 | Ovis aries |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
| Ovis aries | - |
- |
- |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| COX-1 | - |
Ovis aries |
| COX-2 | - |
Homo sapiens |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.000041 | - |
pH 7.4, temperature not specified in the publication | Ovis aries | indomethacin | |
| 0.0001 | - |
pH 7.4, temperature not specified in the publication | Homo sapiens | N-butyl-5-[[(2,5-dihydroxyphenyl)methyl]amino]-2-hydroxybenzamide | |
| 0.0001 | - |
pH 7.4, temperature not specified in the publication | Homo sapiens | N-hexyl-5-[[(2,5-dihydroxyphenyl)methyl]amino]-2-hydroxybenzamide | |
| 0.00011 | - |
pH 7.4, temperature not specified in the publication | Homo sapiens | N-cyclohexyl-5-[(E)-[(2,5-dihydroxyphenyl)methylidene]amino]-2-hydroxybenzamide | |
| 0.00011 | - |
pH 7.4, temperature not specified in the publication | Homo sapiens | N-cyclohexyl-5-[[(2,5-dihydroxyphenyl)methyl]amino]-2-hydroxybenzamide | |
| 0.00019 | - |
pH 7.4, temperature not specified in the publication | Homo sapiens | 5-amino-N-cyclohexyl-2-hydroxybenzamide | |
| 0.00022 | - |
pH 7.4, temperature not specified in the publication | Homo sapiens | 5-amino-N-hexyl-2-hydroxybenzamide | |
| 0.00033 | - |
pH 7.4, temperature not specified in the publication | Homo sapiens | 5-[[(2,5-dihydroxyphenyl)methyl]amino]-2-hydroxy-N-(4-methylphenyl)benzamide | |
| 0.00039 | - |
pH 7.4, temperature not specified in the publication | Homo sapiens | 5-amino-2-hydroxy-N-(propan-2-yl)benzamide | |
| 0.00051 | - |
pH 7.4, temperature not specified in the publication | Homo sapiens | indomethacin | |
| 0.00298 | - |
pH 7.4, temperature not specified in the publication | Ovis aries | 5-amino-2-hydroxy-N-(propan-2-yl)benzamide | |
| 0.0083 | - |
pH 7.4, temperature not specified in the publication | Ovis aries | 5-amino-N-cyclohexyl-2-hydroxybenzamide | |
| 0.0097 | - |
pH 7.4, temperature not specified in the publication | Ovis aries | 5-amino-N-hexyl-2-hydroxybenzamide | |
| 0.0098 | - |
pH 7.4, temperature not specified in the publication | Ovis aries | 5-[[(2,5-dihydroxyphenyl)methyl]amino]-2-hydroxy-N-(4-methylphenyl)benzamide | |
| 0.0126 | - |
pH 7.4, temperature not specified in the publication | Ovis aries | N-cyclohexyl-5-[[(2,5-dihydroxyphenyl)methyl]amino]-2-hydroxybenzamide | |
| 0.0132 | - |
pH 7.4, temperature not specified in the publication | Ovis aries | N-cyclohexyl-5-[(E)-[(2,5-dihydroxyphenyl)methylidene]amino]-2-hydroxybenzamide | |
| 0.0135 | - |
pH 7.4, temperature not specified in the publication | Ovis aries | N-butyl-5-[[(2,5-dihydroxyphenyl)methyl]amino]-2-hydroxybenzamide | |
| 0.0145 | - |
pH 7.4, temperature not specified in the publication | Ovis aries | N-hexyl-5-[[(2,5-dihydroxyphenyl)methyl]amino]-2-hydroxybenzamide |
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