Co-Target(s) Information
Target General Information | Top | ||||
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Target ID | T01777 | Target Info | |||
Target Name | Adrenergic receptor alpha-2C (ADRA2C) | ||||
Synonyms |
Subtype C4; Alpha-2CAR; Alpha-2C adrenoreceptor; Alpha-2C adrenoceptor; Alpha-2C adrenergic receptor; Alpha-2 adrenergic receptor subtype C4; ADRA2RL2; ADRA2L2
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Target Type | Successful Target | ||||
Gene Name | ADRA2C | ||||
Biochemical Class | GPCR rhodopsin | ||||
UniProt ID |
Co-Targets of This Target | Top | |||||
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Co-Target Name | Adrenergic receptor alpha-2A (ADRA2A) | Successful Target | ||||
UniProt ID | ADA2A_HUMAN | |||||
Gene Name | 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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Representative Drug(s) | Brimonidine | Drug Info | EC50 = 0.6166 nM | Click to Show More | [1] | |
2 | Rilmenidine | Drug Info | Ki = 36.31 nM | [4] | ||
3 | MOXONIDINE | Drug Info | Ki = 150 nM | [5] | ||
Co-Target Name | 5-HT 1D receptor (HTR1D) | Successful Target | ||||
UniProt ID | 5HT1D_HUMAN | |||||
Gene Name | HTR1D | |||||
Synonyms |
Serotonin receptor 1D; Serotonin 1D alpha receptor; HTRL; HTR1DA; 5HT1D; 5-hydroxytryptamine receptor 1D; 5-HT1D receptor; 5-HT1D; 5-HT-1D-alpha; 5-HT-1D
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Representative Drug(s) | Xylometazoline | Drug Info | Ki = 0.7 nM | [2] | ||
Co-Target Name | 5-HT 1B receptor (HTR1B) | Successful Target | ||||
UniProt ID | 5HT1B_HUMAN | |||||
Gene Name | HTR1B | |||||
Synonyms |
Serotonin receptor 1B; Serotonin 1D beta receptor; S12; HTR1DB; 5-hydroxytryptamine receptor 1B; 5-HT1B receptor; 5-HT1B; 5-HT-1D-beta; 5-HT-1B
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Representative Drug(s) | Xylometazoline | Drug Info | Ki = 13 nM | [3] | ||
Co-Target Name | Adrenergic receptor alpha-2B (ADRA2B) | Successful Target | ||||
UniProt ID | ADA2B_HUMAN | |||||
Gene Name | ADRA2B | |||||
Synonyms |
Subtype C2; Alpha-2BAR; Alpha-2B adrenoreceptor; Alpha-2B adrenoceptor; Alpha-2B adrenergic receptor; Alpha-2 adrenergic receptor subtype C2; ADRA2RL1; ADRA2L1
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Representative Drug(s) | Brimonidine | Drug Info | Ki = 34.67 nM | Click to Show More | [1] | |
2 | Rilmenidine | Drug Info | Ki = 42.66 nM | [4] | ||
Co-Target Name | Adrenergic receptor alpha-1A (ADRA1A) | Successful Target | ||||
UniProt ID | ADA1A_HUMAN | |||||
Gene Name | ADRA1A | |||||
Synonyms |
Alpha-adrenergic receptor 1c; Alpha-1C adrenergic receptor; Alpha-1A adrenoreceptor; Alpha-1A adrenoceptor; Alpha-1A adrenergic receptor; Alpha adrenergic receptor 1c; Alpha 1A-adrenoreceptor; Alpha 1A-adrenoceptor; ADRA1C
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Representative Drug(s) | Xylometazoline | Drug Info | Ki = 91 nM | [3] | ||
Co-Target Name | Adrenergic receptor alpha-1D (ADRA1D) | Successful Target | ||||
UniProt ID | ADA1D_HUMAN | |||||
Gene Name | ADRA1D | |||||
Synonyms |
Alpha-adrenergic receptor 1a; Alpha-1D adrenoreceptor; Alpha-1D adrenoceptor; Alpha-1D adrenergic receptor; Alpha adrenergic receptor 1a; Alpha 1D-adrenoreceptor; Alpha 1D-adrenoceptor; ADRA1A
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Representative Drug(s) | Brimonidine | Drug Info | Ki = 933.25 nM | [1] | ||
Co-Target Name | Imidazoline receptor 1 (IR1) | Literature-reported Target | ||||
UniProt ID | NISCH_HUMAN | |||||
Gene Name | NISCH | |||||
Synonyms |
hIRAS; KIAA0975; Imidazoline-1 receptor candidate protein; Imidazoline-1 receptor; Imidazoline receptor antisera-selected protein; IRAS; IR1; I1R candidate protein; I-1 receptor candidate protein; I-1
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Representative Drug(s) | MOXONIDINE | Drug Info | IC50 = 3.548 nM | Click to Show More | [6] | |
2 | Rilmenidine | Drug Info | Ki = 59.16 nM | [7] |
References | Top | ||||
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REF 1 | Pharmacological evaluation of UK-14,304 analogs at cloned human alpha adrenergic receptors. Bioorg Med Chem Lett. 1995 Oct 5;5(19):2255-8. | ||||
REF 2 | Benzylimidazolines as h5-HT1B/1D serotonin receptor ligands: a structure-affinity investigation. J Med Chem. 1998 Jun 18;41(13):2243-51. | ||||
REF 3 | 2-(Anilino)imidazolines and 2-(benzyl)imidazoline derivatives as h5-HT1D serotonin receptor ligands. Bioorg Med Chem Lett. 2004 Sep 20;14(18):4697-9. | ||||
REF 4 | Methylation of imidazoline related compounds leads to loss of alpha?-adrenoceptor affinity. Synthesis and biological evaluation of selective I? imidazoline receptor ligands. Bioorg Med Chem. 2012 Aug 1;20(15):4710-5. | ||||
REF 5 | Synthesis and pharmacologic evaluation of 2-endo-amino-3-exo-isopropylbicyclo[2.2.1]heptane: a potent imidazoline1 receptor specific agent. J Med Chem. 1996 Mar 15;39(6):1193-5. | ||||
REF 6 | Bicyclic alpha-Iminophosphonates as High Affinity Imidazoline I 2 Receptor Ligands for Alzheimer's Disease. J Med Chem. 2020 Apr 9;63(7):3610-3633. | ||||
REF 7 | QSAR study of imidazoline antihypertensive drugs. Bioorg Med Chem. 2008 Aug 1;16(15):7134-40. |
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