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Literature summary for 2.7.10.1 extracted from
- Syntheses of 4-(indole-3-yl)quinazolines: a new class of epidermal growth factor receptor tyrosine kinase inhibitors (2008), Eur. J. Med. Chem., 43, 1478-1488.
Application
| Application | Comment | Organism |
|---|---|---|
| drug development | new substance class (4-(indole-3-yl)quinazolines) for the treatment of EGFR-dependent tumors, showing strong fluorescences. No connection between cytotoxicity and EGFR-TK inhibition | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 4-(5-bromoindole-3-yl)-6,7-dimethoxyquinazoline | relatively potent inhibitor of EGFR-TK activity | Homo sapiens |  |
| 4-(5-chloro-6-fluoro-indole-3-yl)-6,7-di-(2-methoxyethoxy)quinazoline | relatively potent inhibitor of EGFR-TK activity | Homo sapiens | |
| 4-(5-chloro-6-fluoroindole-3-yl)-6,7-dimethoxyquinazoline | relatively potent inhibitor of EGFR-TK activity, is a dual EGFR-TK and HER-2-TK inhibitor | Homo sapiens | |
| 4-(5-chloro-6-fluoroindole-3-yl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazoline | relatively potent inhibitor of EGFR-TK activity, is a dual EGFR-TK and HER-2-TK inhibitor | Homo sapiens | |
| 4-(6-fluoro-5-methylindole-3-yl)-6,7-dimethoxyquinazoline | relatively potent inhibitor of EGFR-TK activity | Homo sapiens | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| A-498 cell | - |
Homo sapiens | - |
| ACHN cell | - |
Homo sapiens | - |
| HT-29 cell | - |
Homo sapiens | - |
| IGROV-1 cell | - |
Homo sapiens | - |
| additional information | EKVX cell, HOP-92 cell, NCI-H322M cell, TK-10 cell and SNB-75 cell | Homo sapiens | - |
| PC-3 cell | - |
Homo sapiens | - |
| SKOV-3 cell | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| poly(Glu:Tyr) + ATP | - |
Homo sapiens | ADP + poly(Glu:Tyr) phosphate | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| EGFR tyrosine kinase | - |
Homo sapiens |
| EGFR-TK | - |
Homo sapiens |
| epidermal growth factor receptor tyrosine kinase | - |
Homo sapiens |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.000131 | - |
- |
Homo sapiens | 4-(5-bromoindole-3-yl)-6,7-dimethoxyquinazoline | |
| 0.000209 | - |
- |
Homo sapiens | 4-(5-chloro-6-fluoroindole-3-yl)-6,7-dimethoxyquinazoline | |
| 0.000333 | - |
- |
Homo sapiens | 4-(5-chloro-6-fluoroindole-3-yl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazoline | |
| 0.000472 | - |
- |
Homo sapiens | 4-(5-chloro-6-fluoro-indole-3-yl)-6,7-di-(2-methoxyethoxy)quinazoline | |
| 0.000533 | - |
- |
Homo sapiens | 4-(6-fluoro-5-methylindole-3-yl)-6,7-dimethoxyquinazoline | |
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