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Literature summary for 2.1.1.63 extracted from
- MGMT inhibitors--The Trinity College-Paterson Institute experience, a chemists perception (2007), DNA Repair, 6, 1161-1169.
Application
| Application | Comment | Organism |
|---|---|---|
| medicine | MGMT can confer resistance to the cancer chemotherapeutic effects of the class of DNA damaging drugs, inactivation of MGMT is thus a practical approach to improving the efficacy of such agents | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 2-([2-amino-6-[(4-bromothiophen-2-yl)methoxy]-9H-purin-9-yl]methoxy)ethanol | - |
Homo sapiens |  |
| 4-[(4-bromothiophen-2-yl)methoxy]-1H-pyrazolo[3,4-d]pyrimidin-6-amine | - |
Homo sapiens | |
| 6-(1-benzofuran-2-ylmethoxy)-9H-purin-2-amine | - |
Homo sapiens | |
| 6-(4,5,6,7-tetrahydro-1-benzothiophen-2-ylmethoxy)-9H-purin-2-amine | - |
Homo sapiens | |
| 6-(naphtho[1,2-b]thiophen-2-ylmethoxy)-9H-purin-2-amine | - |
Homo sapiens | |
| 6-(naphtho[2,1-b]thiophen-2-ylmethoxy)-9H-purin-2-amine | - |
Homo sapiens | |
| 6-(phenanthro[9,10-b]thiophen-2-ylmethoxy)-9H-purin-2-amine | - |
Homo sapiens | |
| 6-[(1-methyl-4-nitro-1H-pyrrol-2-yl)methoxy]-9H-purin-2-amine | - |
Homo sapiens | |
| 6-[(4-bromothiophen-2-yl)methoxy]-9-(2-deoxy-beta-D-erythro-pentofuranosyl)-9H-purin-2-amine | - |
Homo sapiens | |
| 7-[(4-bromothiophen-2-yl)methoxy]-2,3-dihydro-1H-[1,2,3]triazolo[4,5-d]pyrimidin-5-amine | - |
Homo sapiens | |
| 9-beta-D-arabinofuranosyl-6-[(4-bromothiophen-2-yl)methoxy]-9H-purin-2-amine | - |
Homo sapiens | |
| O4-(4-bromothenylpterin) | - |
Homo sapiens | |
| O6-(1,2-thiazol-4-ylmethyl)guanine | - |
Homo sapiens | |
| O6-(1,3-oxazol-5-yl)guanine | - |
Homo sapiens | |
| O6-(1,3-thiazol-5-yl)guanine | - |
Homo sapiens | |
| O6-(1-benzofuran-2-ylmethyl)guanine | - |
Homo sapiens | |
| O6-(2-benzo[b]thienylmethyl)guanine | - |
Homo sapiens | |
| O6-(3-pyridyl)guanine | - |
Homo sapiens | |
| O6-(4-(2-chloropyridyl))guanine | - |
Homo sapiens | |
| O6-(4-bromothenyl)-8-oxaguanine | - |
Homo sapiens | |
| O6-(4-bromothenyl)-8-thiaguanine | - |
Homo sapiens | |
| O6-(4-bromothenyl)guanine | PaTrin, PaTrin-2, Lomeguatrib | Homo sapiens | |
| O6-(4-pyridyl)guanine | - |
Homo sapiens | |
| O6-benzylguanine | - |
Homo sapiens | |
| O6-furfurylguanine | - |
Homo sapiens | |
| O6-thenylguanine | original Patrin, became Patrin-1 | Homo sapiens | |
| O6-[(1-methyl-1H-imidazol-5-yl)methyl]guanine | - |
Homo sapiens | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| DNA (containing 6-O-methylguanine) + [protein]-L-cysteine | Homo sapiens | - |
DNA (without 6-O-methylguanine) + [protein]-S-methyl-L-cysteine | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| DNA (containing 6-O-methylguanine) + [protein]-L-cysteine | - |
Homo sapiens | DNA (without 6-O-methylguanine) + [protein]-S-methyl-L-cysteine | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| MGMT | - |
Homo sapiens |
| O6-alkylguanine-DNA alkyltransferase | - |
Homo sapiens |
| O6-methylguanine-DNA methyltransferase | - |
Homo sapiens |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.0000028 | - |
- |
Homo sapiens | O6-(4-bromothenyl)-8-thiaguanine | |
| 0.0000034 | - |
Patrin, PaTrin-2, Lomeguatrib | Homo sapiens | O6-(4-bromothenyl)guanine | |
| 0.000006 | - |
- |
Homo sapiens | 4-[(4-bromothiophen-2-yl)methoxy]-1H-pyrazolo[3,4-d]pyrimidin-6-amine | |
| 0.000018 | - |
- |
Homo sapiens | O6-thenylguanine | |
| 0.000022 | - |
- |
Homo sapiens | 6-(naphtho[1,2-b]thiophen-2-ylmethoxy)-9H-purin-2-amine | |
| 0.000025 | - |
- |
Homo sapiens | O4-(4-bromothenylpterin) | |
| 0.00003 | - |
- |
Homo sapiens | O6-(2-benzo[b]thienylmethyl)guanine | |
| 0.000033 | - |
- |
Homo sapiens | O6-(1,3-thiazol-5-yl)guanine | |
| 0.000035 | - |
- |
Homo sapiens | O6-(1-benzofuran-2-ylmethyl)guanine | |
| 0.00004 | - |
- |
Homo sapiens | O6-(4-(2-chloropyridyl))guanine | |
| 0.000045 | - |
- |
Homo sapiens | 7-[(4-bromothiophen-2-yl)methoxy]-2,3-dihydro-1H-[1,2,3]triazolo[4,5-d]pyrimidin-5-amine | |
| 0.00005 | - |
- |
Homo sapiens | 6-(naphtho[2,1-b]thiophen-2-ylmethoxy)-9H-purin-2-amine | |
| 0.00007 | - |
- |
Homo sapiens | O6-(1,2-thiazol-4-ylmethyl)guanine | |
| 0.00008 | - |
- |
Homo sapiens | 6-(1-benzofuran-2-ylmethoxy)-9H-purin-2-amine | |
| 0.000095 | - |
- |
Homo sapiens | 6-[(4-bromothiophen-2-yl)methoxy]-9-(2-deoxy-beta-D-erythro-pentofuranosyl)-9H-purin-2-amine | |
| 0.000115 | - |
- |
Homo sapiens | 9-beta-D-arabinofuranosyl-6-[(4-bromothiophen-2-yl)methoxy]-9H-purin-2-amine | |
| 0.00013 | - |
- |
Homo sapiens | O6-(4-pyridyl)guanine | |
| 0.0002 | - |
- |
Homo sapiens | O6-benzylguanine | |
| 0.00024 | - |
- |
Homo sapiens | O6-(4-bromothenyl)-8-oxaguanine | |
| 0.0003 | - |
- |
Homo sapiens | O6-furfurylguanine | |
| 0.00033 | - |
- |
Homo sapiens | 2-([2-amino-6-[(4-bromothiophen-2-yl)methoxy]-9H-purin-9-yl]methoxy)ethanol | |
| 0.00035 | - |
- |
Homo sapiens | O6-(1,3-oxazol-5-yl)guanine | |
| 0.00043 | - |
- |
Homo sapiens | O6-(3-pyridyl)guanine | |
| 0.00055 | - |
- |
Homo sapiens | 6-[(1-methyl-4-nitro-1H-pyrrol-2-yl)methoxy]-9H-purin-2-amine | |
| 0.0011 | - |
- |
Homo sapiens | 6-(phenanthro[9,10-b]thiophen-2-ylmethoxy)-9H-purin-2-amine | |
| 0.0085 | - |
- |
Homo sapiens | O6-[(1-methyl-1H-imidazol-5-yl)methyl]guanine | |
| 0.185 | - |
- |
Homo sapiens | 6-(4,5,6,7-tetrahydro-1-benzothiophen-2-ylmethoxy)-9H-purin-2-amine | |
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