DOM [Ligand Id: 164] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL8600 (2-(2,5-Dimethoxy-4-Methyl-Phenyl)-1-Methyl-Ethylamine)
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Rat [ChEMBL: CHEMBL323] [GtoPdb: 7] [UniProtKB: P30994]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Monoamine oxidase A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3358] [UniProtKB: P21396]
ChEMBL Inhibitory concentration against monoamine oxidase A in rat brain mitochondrial suspension B 4.62 pIC50 24000 nM IC50 J Med Chem (2005) 48: 2407-2419 [PMID:15801832]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Binding affinity against 5-hydroxytryptamine 1A receptor in rat hippocampal tissue B 5.29 pKi 5125 nM Ki J Med Chem (1988) 31: 867-870 [PMID:2965244]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
ChEMBL Binding affinity against 5-HT1B serotonin receptor in rat striatum B 5.68 pKi 2070 nM Ki J Med Chem (1988) 31: 867-870 [PMID:2965244]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
GtoPdb - - 6.8 pKi - - - J Pharmacol Exp Ther (1998) 286: 85-90 [PMID:9655845]
ChEMBL Displacement of [3H]ketanserin from 5HT2A receptor in Sprague-Dawley rat brain by liquid scintillation spectroscopy B 7 pKi 100 nM Ki Bioorg Med Chem (2008) 16: 4661-4669 [PMID:18296055]
ChEMBL Compound was evaluated for its ability to displace [125I](R)-DOI from 5-hydroxytryptamine 2A receptor in cloned rat prefrontal cortex homogenate B 7.72 pKi 19 nM Ki Bioorg Med Chem Lett (2002) 12: 1997-1999 [PMID:12113827]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL323] [GtoPdb: 7] [UniProtKB: P30994]
ChEMBL Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus B 7.12 pKd 75.86 nM Kd J Med Chem (1981) 24: 1414-1421 [PMID:7310818]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
ChEMBL Binding affinity towards 5-hydroxytryptamine 1C receptor from frontal cortical regions of male Sprague-Dawley rat homogenates, using [3H]mesulergine as radioligand B 6.71 pKi 193 nM Ki J Med Chem (1992) 35: 734-740 [PMID:1542100]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]