Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T11448 | Target Info | |||
| Target Name | Adrenergic receptor alpha-2A (ADRA2A) | ||||
| Synonyms |
Alpha-2AAR; Alpha-2A adrenoreceptor; Alpha-2A adrenoceptor; Alpha-2A adrenergic receptor; Alpha-2 adrenergic receptor subtype C10; ADRAR; ADRA2R
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| Target Type | Successful Target | ||||
| Gene Name | ADRA2A | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 8 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
1-Isopentyl-4-(isopentylamino)-6-methylpyridine-2(1H)-one
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3814626; BDBM50179386; J3.553.469E
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| Activity |
Ki = 52000 nM
|
[1] | |||
| Compound Name |
1-Isobutyl-4-[[4-(trifluoromethyl)benzyl]amino]-6-methylpyridine-2(1H)-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3814535; BDBM50179382; J3.553.470I
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| Activity |
Ki = 58000 nM
|
[1] | |||
| Compound Name |
1H-Imidazol-5-yl(naphthalen-1-yl)methanol;hydrochloride
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL542155
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| Activity |
IC50 = 61900 nM
|
[2] | |||
| Compound Name |
1-Pentyl-4-(pentylamino)-6-methylpyridine-2(1H)-one
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3814593; BDBM50179383; J3.553.466K
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| Activity |
Ki = 62000 nM
|
[1] | |||
| Compound Name |
1-Pentyl-4-[(4-chlorobenzyl)amino]-6-methylpyridine-2(1H)-one
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3814521; BDBM50179385; J3.553.468G
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| Activity |
Ki = 80000 nM
|
[1] | |||
| Compound Name |
1-Isopentyl-4-(4-chlorobenzylamino)-6-methylpyridine-2(1H)-one
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3814259; BDBM50179388; J3.553.472E
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|
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| Activity |
Ki = 99000 nM
|
[1] | |||
| Compound Name |
1-Benzyl-4-(pentylamino)-6-methylpyridine-2(1H)-one
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3813724; BDBM50179389; J3.553.473C
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| Activity |
Ki = 110000 nM
|
[1] | |||
| Compound Name |
1-Benzyl-4-(isopentylamino)-6-methylpyridine-2(1H)-one
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3815157; BDBM50179390; J3.553.474A
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|
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| Activity |
Ki = 110000 nM
|
[1] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 3 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
2,2,2-Trifluoro-1-(1H-imidazol-5-yl)-1-naphthalen-1-ylethanol;hydrochloride
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL541302
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| Activity |
IC50 > 300000 nM
|
[2] | |||
| Compound Name |
5-[Methoxy(naphthalen-1-yl)methyl]-1H-imidazole;hydrochloride
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL553835
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|
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| Activity |
IC50 = 379800 nM
|
[2] | |||
| Compound Name |
1H-Imidazol-5-yl(naphthalen-1-yl)methanone;oxalic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL75022
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| Activity |
IC50 = 580400 nM
|
[2] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin. Bioorg Med Chem. 2016 Jul 15;24(14):3174-83. | ||||
| REF 2 | A structure-activity relationship study of benzylic modifications of 4-[1-(1-naphthyl)ethyl]-1H-imidazoles on alpha 1- and alpha 2-adrenergic recep... J Med Chem. 1994 Jul 22;37(15):2328-33. | ||||
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