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

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ChEMBL ligand: CHEMBL8600
  • 5-HT1A receptor/5-hydroxytryptamine receptor 1A in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT1B receptor/5-hydroxytryptamine receptor 1B in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
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  • 5-HT2A receptor/5-hydroxytryptamine receptor 2A in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
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  • 5-HT2B receptor/5-hydroxytryptamine receptor 2B in Rat [ChEMBL: CHEMBL323] [GtoPdb: 7] [UniProtKB: P30994]
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  • 5-HT2C receptor/5-hydroxytryptamine receptor 2C in Rat [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
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  • Amine oxidase [flavin-containing] A in Rat [ChEMBL: CHEMBL3358] [UniProtKB: P21396]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-HT1A receptor/5-hydroxytryptamine receptor 1A 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/5-hydroxytryptamine receptor 1B 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/5-hydroxytryptamine receptor 2A 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/5-hydroxytryptamine receptor 2B 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/5-hydroxytryptamine receptor 2C 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]
Amine oxidase [flavin-containing] 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]

ChEMBL data shown on this page come from version 36:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]