Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T58998 | Target Info | |||
| Target Name | Bromodomain and extraterminal domain protein (BET) | ||||
| Synonyms |
Bromodomain and Extra Terminal protein
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| Target Type | Clinical trial Target | ||||
| Gene Name | NO-GeName | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| Co-Target Name | Translocator protein (TSPO) | Successful Target | ||||
| UniProt ID | TSPO_HUMAN | |||||
| Gene Name | TSPO | |||||
| Synonyms |
Peripheral-type benzodiazepine receptor; Peripheral benzodiazepine receptor; PKBS; PBR; Mitochondrial benzodiazepine receptor; MBR; BZRP
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| Representative Drug(s) | Mivebresib | Drug Info | IC50 = 800 nM | [1] | ||
| Co-Target Name | Histone acetyltransferase p300 (EP300) | Literature-reported Target | ||||
| UniProt ID | EP300_HUMAN | |||||
| Gene Name | EP300 | |||||
| Synonyms |
p300 HAT; Protein propionyltransferase p300; P300; Histone crotonyltransferase p300; Histone butyryltransferase p300; E1Aassociated protein p300; E1A-associated protein p300
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| Representative Drug(s) | Mivebresib | Drug Info | IC50 = 63 nM | [2] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor. J Med Chem. 2017 Oct 26;60(20):8369-84. | ||||
| REF 2 | Discovery of 8-Methyl-pyrrolo[1,2- a]pyrazin-1(2 H)-one Derivatives as Highly Potent and Selective Bromodomain and Extra-Terminal (BET) Bromodomain Inhibitors. J Med Chem. 2020 Apr 23;63(8):3956-3975. | ||||
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