(R)-DOI [Ligand Id: 157] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL134519
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
  • 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 Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
  • 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 Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
  • 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
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Inhibitory constant against cloned human 5-hydroxytryptamine 2A receptor using with [125I]- DOI radioligand B 9.19 pKi 0.65 nM Ki J. Med. Chem. (2003) 46: 4188-4195 [PMID:12954071]
ChEMBL In vitro inhibitory concentration required against [3H]8-OH-DPAT binding to cloned human 5-hydroxytryptamine 1A receptor B 5.42 pIC50 3843 nM IC50 J. Med. Chem. (2003) 46: 4188-4195 [PMID:12954071]
ChEMBL Tested for functional response on CHO cells expressing cloned human 5-hydroxytryptamine 1A receptor B 5 pEC50 >10000 nM EC50 J. Med. Chem. (2003) 46: 4188-4195 [PMID:12954071]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Displacement of [125I]DOI from cloned human 5HT2A receptor expressed in CHO cells B 9.19 pKi 0.65 nM Ki J. Med. Chem. (2006) 49: 318-328 [PMID:16392816]
GtoPdb - - 9.2 pKi - - - J Med Chem (2003) 46: 4188-95 [PMID:12954071]
GtoPdb - - 9.3 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733];
J Med Chem (1998) 41: 5148-9 [PMID:9857084]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
ChEMBL In vitro inhibitory constant against [125I]DOI binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex B 10 pKi 0.1 nM Ki J. Med. Chem. (2003) 46: 4188-4195 [PMID:12954071]
ChEMBL Displacement of [125I]DOI from 5HT2A receptor in rat cerebral cortex B 9.34 pIC50 0.46 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 2998-3002 [PMID:17419053]
ChEMBL In vitro inhibition of [125I]DOI binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex B 9.4 pIC50 0.4 nM IC50 J. Med. Chem. (2003) 46: 4188-4195 [PMID:12954071]
ChEMBL Inhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortex B 9.68 pIC50 0.21 nM IC50 J. Med. Chem. (2006) 49: 318-328 [PMID:16392816]
ChEMBL In vitro relative agonist activity against 5-hydroxytryptamine 2A using PI assay in rat vascular smooth muscle cells F 7.56 pEC50 27.7 nM EC50 J. Med. Chem. (2003) 46: 4188-4195 [PMID:12954071]
ChEMBL Activity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cells F 7.7 pEC50 19.8 nM EC50 J. Med. Chem. (2006) 49: 318-328 [PMID:16392816]
ChEMBL Agonist activity at 5HT2A receptor in rat A7r5 cells assessed as intracellular calcium mobilization relative to 5HT F 7.75 pEC50 17.8 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 2998-3002 [PMID:17419053]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
GtoPdb - - 7.4 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733];
J Med Chem (1998) 41: 5148-9 [PMID:9857084]
GtoPdb - - 7.7 pKi - - - J Med Chem (2003) 46: 4188-95 [PMID:12954071]
ChEMBL Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand B 7.74 pKi 18 nM Ki J. Med. Chem. (2003) 46: 4188-4195 [PMID:12954071]
ChEMBL Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells B 7.74 pKi 18 nM Ki J. Med. Chem. (2006) 49: 318-328 [PMID:16392816]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL323] [GtoPdb: 7] [UniProtKB: P30994]
ChEMBL Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats F 7.92 pEC50 11.9 nM EC50 J. Med. Chem. (2006) 49: 318-328 [PMID:16392816]
ChEMBL Agonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HT F 7.92 pEC50 11.9 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 2998-3002 [PMID:17419053]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL Inhibitory constant against cloned human 5-hydroxytryptamine 2C receptor using with [125I]- DOI radioligand B 8.4 pKi 4 nM Ki J. Med. Chem. (2003) 46: 4188-4195 [PMID:12954071]
ChEMBL Displacement of [125I]DOI from cloned human 5HT2C receptor expressed in CHO cells B 8.4 pKi 4 nM Ki J. Med. Chem. (2006) 49: 318-328 [PMID:16392816]
GtoPdb - - 8.4 pKi - - - J Med Chem (2003) 46: 4188-95 [PMID:12954071]
GtoPdb - - 8.7 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733];
Naunyn Schmiedebergs Arch Pharmacol (1999) 359: 1-6 [PMID:9933142];
J Neurochem (1999) 72: 2127-34 [PMID:10217294]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
ChEMBL Activity against recombinant rat 5HT2C mediated intracellular calcium mobilization by FLIPR in SR3T3 cells F 7.52 pEC50 30.2 nM EC50 J. Med. Chem. (2006) 49: 318-328 [PMID:16392816]
ChEMBL Agonist activity at 5HT2C receptor expressed in rat SR3T3 cells assessed as intracellular calcium mobilization relative to 5HT F 7.52 pEC50 30.2 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 2998-3002 [PMID:17419053]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]