Co-Target(s) Information
Target General Information | Top | ||||
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Target ID | T22118 | Target Info | |||
Target Name | Dopamine D1 receptor (D1R) | ||||
Synonyms |
D(1A) dopamine receptor
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Target Type | Successful Target | ||||
Gene Name | DRD1 | ||||
Biochemical Class | GPCR rhodopsin | ||||
UniProt ID |
Co-Targets of This Target | Top | |||||
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Co-Target Name | 5-HT 2B receptor (HTR2B) | Successful Target | ||||
UniProt ID | 5HT2B_HUMAN | |||||
Gene Name | HTR2B | |||||
Synonyms |
Serotonin receptor 2B; 5-hydroxytryptamine receptor 2B; 5-HT2B; 5-HT-2B; 5-HT 2B
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Representative Drug(s) | Methylergonovine | Drug Info | Ki = 0.8 nM | [1] | ||
Co-Target Name | Dopamine D3 receptor (D3R) | Successful Target | ||||
UniProt ID | DRD3_HUMAN | |||||
Gene Name | DRD3 | |||||
Synonyms |
D(3) dopamine receptor
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Representative Drug(s) | Pergolide | Drug Info | Ki = 0.8511 nM | [2] | ||
Co-Target Name | 5-HT 1A receptor (HTR1A) | Successful Target | ||||
UniProt ID | 5HT1A_HUMAN | |||||
Gene Name | HTR1A | |||||
Synonyms |
Serotonin receptor 1A; G-21; ADRBRL1; ADRB2RL1; 5-hydroxytryptamine receptor 1A; 5-HT1A receptor; 5-HT1A; 5-HT-1A
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Representative Drug(s) | Pergolide | Drug Info | Ki = 1.8 nM | [3] | ||
Co-Target Name | Dopamine D5 receptor (D5R) | Successful Target | ||||
UniProt ID | DRD5_HUMAN | |||||
Gene Name | DRD5 | |||||
Synonyms |
Dopamine receptor 5; DRD5; D1beta dopamine receptor; D(5)D(1B) dopamine receptor dopamine receptor; D(5) dopamine receptor
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Representative Drug(s) | Ecopipam | Drug Info | Ki = 2 nM | Click to Show More | [4] | |
2 | Phenyltoloxamine | Drug Info | Ki = 414 nM | [7] | ||
Co-Target Name | Dopamine D2 receptor (D2R) | Successful Target | ||||
UniProt ID | DRD2_HUMAN | |||||
Gene Name | DRD2 | |||||
Synonyms |
Dopamine receptor 2; D(2) dopamine receptor
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Representative Drug(s) | Pergolide | Drug Info | Ki = 4 nM | Click to Show More | [5] | |
2 | Fenoldopam | Drug Info | Ki = 810 nM | [8] | ||
3 | Ecopipam | Drug Info | Ki = 980 nM | [9] | ||
Co-Target Name | Voltage-gated potassium channel Kv11.1 (KCNH2) | Successful Target | ||||
UniProt ID | KCNH2_HUMAN | |||||
Gene Name | KCNH2 | |||||
Synonyms |
hERG1; hERG-1; Voltage-gated potassium channel subunit Kv11.1; Potassium voltage-gated channel subfamily H member 2; HERG K+ channel; HERG; H-ERG; Ether-a-go-go-related protein 1; Ether-a-go-go-related gene potassium channel 1; Ether-a-go-go related protein 1; Ether-a-go-go related gene potassium channel 1; Eag related protein 1; Eag homolog; ERG-1; ERG
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Representative Drug(s) | Pergolide | Drug Info | IC50 = 120.23 nM | [6] | ||
Co-Target Name | HUAMN alpha-1 adrenergic receptor (ADRA1) | Literature-reported Target | ||||
UniProt ID | ADA1A_HUMAN; ADA1B_HUMAN; ADA1D_HUMAN | |||||
Gene Name | ADRA1A; ADRA1B; ADRA1D | |||||
Synonyms |
Alpha-1 adrenoreceptor
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Representative Drug(s) | Fenoldopam | Drug Info | Ki = 151.36 nM | [10] |
References | Top | ||||
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REF 1 | Development, validation, and use of quantitative structure-activity relationship models of 5-hydroxytryptamine (2B) receptor ligands to identify no... J Med Chem. 2010 Nov 11;53(21):7573-86. | ||||
REF 2 | CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists. J Med Chem. 2005 Apr 7;48(7):2493-508. | ||||
REF 3 | Comparison of 5-HT1A and dopamine D2 pharmacophores. X-ray structures and affinities of conformationally constrained ligands. J Med Chem. 1993 May 14;36(10):1301-15. | ||||
REF 4 | Discovery of new SCH 39166 analogs as potent and selective dopamine D1 receptor antagonists. Bioorg Med Chem Lett. 2010 Feb 1;20(3):836-40. | ||||
REF 5 | Synthesis and biological activities of (R)-5,6-dihydro-N,N-dimethyl-4H-imidazo[4,5,1-ij]quinolin-5-amine and its metabolites. J Med Chem. 1997 Feb 28;40(5):639-46. | ||||
REF 6 | Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model. Eur J Med Chem. 2011 Feb;46(2):618-30. | ||||
REF 7 | Dopamine/serotonin receptor ligands. 9. Oxygen-containing midsized heterocyclic ring systems and nonrigidized analogues. A step toward dopamine D5 ... J Med Chem. 2004 Aug 12;47(17):4155-8. | ||||
REF 8 | CoMFA-based prediction of agonist affinities at recombinant D1 vs D2 dopamine receptors. J Med Chem. 1998 Oct 22;41(22):4385-99. | ||||
REF 9 | Remote functionalization of SCH 39166: discovery of potent and selective benzazepine dopamine D1 receptor antagonists. Bioorg Med Chem Lett. 2010 Feb 1;20(3):832-5. | ||||
REF 10 | N,N-6-bis-[2-(3,4-dihydroxybenzyl)pyrrolidinyl]hexane, a potent, selective, orally active dopamine analog with hypotensive and diuretic activity. Bioorg Med Chem Lett. 1995 Oct 19;5(20):2371-6. |
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