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Literature summary for 2.1.1.320 extracted from
- Discovery of new potent protein arginine methyltransferase 5 (PRMT5) inhibitors by assembly of key pharmacophores from known inhibitors (2018), Bioorg. Med. Chem. Lett., 28, 3693-3699 .
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 3-(3,4-dihydroisoquinolin-2(1H)-yl)-N-(3-fluorophenyl)propanamide | - |
Homo sapiens |  |
| 3-(3,4-dihydroisoquinolin-2(1H)-yl)-N-[3-(trifluoromethoxy)phenyl]propanamide | - |
Homo sapiens | |
| 3-(3,4-dihydroisoquinolin-2(1H)-yl)-N-[4-(trifluoromethyl)pyrimidin-2-yl]propanamide | - |
Homo sapiens | |
| methyl 2-[2-(3,4-dihydroisoquinolin-2(1H)-yl)acetamido]benzoate | - |
Homo sapiens | |
| methyl 2-[3-(3,4-dihydroisoquinolin-2(1H)-yl)propanamido]benzoate | - |
Homo sapiens | |
| methyl 2-[4-(3,4-dihydroisoquinolin-2(1H)-yl)butanamido]benzoate | - |
Homo sapiens | |
| N'-[3-(3,4-dihydroisoquinolin-2(1H)-yl)propanoyl]benzohydrazide | - |
Homo sapiens | |
| N-(2-cyanophenyl)-3-(3,4-dihydroisoquinolin-2(1H)-yl)propanamide | - |
Homo sapiens | |
| N-(3-acetylphenyl)-3-(3,4-dihydroisoquinolin-2(1H)-yl)propanamide | - |
Homo sapiens | |
| N-(3-bromo-2-cyanophenyl)-3-(3,4-dihydroisoquinolin-2(1H)-yl)propanamide | - |
Homo sapiens | |
| N-(3-bromophenyl)-3-(3,4-dihydroisoquinolin-2(1H)-yl)propanamide | - |
Homo sapiens | |
| N-(3-chlorophenyl)-3-(3,4-dihydroisoquinolin-2(1H)-yl)propanamide | - |
Homo sapiens | |
| N-[(2S)-3-(3,4-dihydro-2(1H)-isoquinolinyl)-2-hydroxypropyl]-6-(3-oxetanylamino)-4-pyrimidinecarboxamide | i.e. EPZ015666 | Homo sapiens | |
| S-adenosyl-L-homocysteine | - |
Homo sapiens | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 2 S-adenosyl-L-methionine + [SmD3 protein]-L-arginine | Homo sapiens | - |
2 S-adenosyl-L-homocysteine + [SmD3 protein]-Nomega,Nomega'-dimethyl-L-arginine | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | O14744 | - |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| KARPAS-422 cell | - |
Homo sapiens | - |
| MV4-11 cell | - |
Homo sapiens | - |
| Pfeiffer cell | - |
Homo sapiens | - |
| SU-DHL-4 cell | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 2 S-adenosyl-L-methionine + [SmD3 protein]-L-arginine | - |
Homo sapiens | 2 S-adenosyl-L-homocysteine + [SmD3 protein]-Nomega,Nomega'-dimethyl-L-arginine | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| PRMT5 | - |
Homo sapiens |
| protein arginine methyltransferase 5 | - |
Homo sapiens |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.000047 | - |
pH and temperature not specified in the publication | Homo sapiens | N-[(2S)-3-(3,4-dihydro-2(1H)-isoquinolinyl)-2-hydroxypropyl]-6-(3-oxetanylamino)-4-pyrimidinecarboxamide | |
| 0.00056 | - |
pH and temperature not specified in the publication | Homo sapiens | S-adenosyl-L-homocysteine | |
| 0.00271 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(3-bromo-2-cyanophenyl)-3-(3,4-dihydroisoquinolin-2(1H)-yl)propanamide | |
| 0.01812 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(3-bromophenyl)-3-(3,4-dihydroisoquinolin-2(1H)-yl)propanamide | |
| 0.02555 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(2-cyanophenyl)-3-(3,4-dihydroisoquinolin-2(1H)-yl)propanamide | |
| 0.03162 | - |
pH and temperature not specified in the publication | Homo sapiens | methyl 2-[3-(3,4-dihydroisoquinolin-2(1H)-yl)propanamido]benzoate | |
| 0.04213 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(3-chlorophenyl)-3-(3,4-dihydroisoquinolin-2(1H)-yl)propanamide | |
| 0.04587 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-(3,4-dihydroisoquinolin-2(1H)-yl)-N-(3-fluorophenyl)propanamide | |
| 0.05195 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(3-acetylphenyl)-3-(3,4-dihydroisoquinolin-2(1H)-yl)propanamide | |
| 0.06 | - |
pH and temperature not specified in the publication | Homo sapiens | methyl 2-[2-(3,4-dihydroisoquinolin-2(1H)-yl)acetamido]benzoate | |
| 0.06295 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-(3,4-dihydroisoquinolin-2(1H)-yl)-N-[3-(trifluoromethoxy)phenyl]propanamide | |
| 0.06987 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-(3,4-dihydroisoquinolin-2(1H)-yl)-N-[4-(trifluoromethyl)pyrimidin-2-yl]propanamide | |
| 0.07254 | - |
pH and temperature not specified in the publication | Homo sapiens | N'-[3-(3,4-dihydroisoquinolin-2(1H)-yl)propanoyl]benzohydrazide | |
| 0.08789 | - |
pH and temperature not specified in the publication | Homo sapiens | methyl 2-[4-(3,4-dihydroisoquinolin-2(1H)-yl)butanamido]benzoate | |
General Information
| General Information | Comment | Organism |
|---|---|---|
| drug target | the enzyme is a promising therapeutic target for human cancer | Homo sapiens |
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