α-methyl-5-HT [Ligand Id: 152] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL275854
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • 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 Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
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  • 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
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  • 5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566]
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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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  • 5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939]
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  • 5-HT4 receptor in Human [GtoPdb: 9] [UniProtKB: Q13639]
  • 5-HT4 receptor in Rat [GtoPdb: 9] [UniProtKB: Q62758]
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  • 5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
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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 7.92 pKi 12 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 7.71 pIC50 19.6 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 6.42 pEC50 378 nM EC50 J. Med. Chem. (2003) 46: 4188-4195 [PMID:12954071]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement B 7.05 pKi 89.13 nM Ki J. Med. Chem. (1996) 39: 126-134 [PMID:8568799]
ChEMBL Evaluated for the binding affinity to hippocampus striatal membranes at 5-hydroxytryptamine 1A receptor binding site by using [3H]-8-OH- DPAT as a radioligand. B 7.07 pKi 85 nM Ki J. Med. Chem. (1987) 30: 1-12 [PMID:3543362]
ChEMBL Binding affinity was determined against 5-hydroxytryptamine 1A receptor was determined in male Sprague-Dawley rat brain. B 7.38 pKi 42 nM Ki J. Med. Chem. (1990) 33: 755-758 [PMID:2299641]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
ChEMBL Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta B 6.6 pKi 250 nM Ki J. Med. Chem. (1996) 39: 314-322 [PMID:8568822]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
ChEMBL Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand. B 6 pKi 1000 nM Ki J. Med. Chem. (1987) 30: 1-12 [PMID:3543362]
ChEMBL Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain. B 7.07 pKi 85 nM Ki J. Med. Chem. (1990) 33: 755-758 [PMID:2299641]
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
GtoPdb - - 6.6 pKi - - - Mol. Pharmacol. (1996) 50: 1567-80 [PMID:8967979]
ChEMBL Binding affinity was determined against 5-hydroxytryptamine 1D receptor in bovine caudate homogenate B 6.82 pKi 150 nM Ki J. Med. Chem. (1990) 33: 755-758 [PMID:2299641]
5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566]
ChEMBL Binding affinity was determined against 5-hydroxytryptamine 1E receptor in human cortical homogenate B 5 pKi >10000 nM Ki J. Med. Chem. (1990) 33: 755-758 [PMID:2299641]
GtoPdb - - 7 pKi - - - Proc. Natl. Acad. Sci. U.S.A. (1993) 90: 408-12 [PMID:8380639];
Eur. J. Pharmacol. (2004) 484: 127-39 [PMID:14744596]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
GtoPdb - - 7.8 pKi - - - Naunyn Schmiedebergs Arch. Pharmacol. (2004) 370: 114-23 [PMID:15322733]
ChEMBL Displacement of [125I]DOI from cloned human 5HT2A receptor expressed in CHO cells B 7.92 pKi 12 nM Ki J. Med. Chem. (2006) 49: 318-328 [PMID:16392816]
ChEMBL Agonist activity at human 5-HT2A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assay F 8.7 pEC50 2 nM EC50 Bioorg Med Chem Lett (2018) 28: 2039-2049 [PMID:29730027]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
GtoPdb - - 5.9 pKi - - - Mol. Pharmacol. (2000) 58: 877-86 [PMID:11040033]
ChEMBL In vitro inhibitory constant against [125I]DOI binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex B 9 pKi 1 nM Ki J. Med. Chem. (2003) 46: 4188-4195 [PMID:12954071]
ChEMBL Inhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortex B 8.46 pIC50 3.5 nM IC50 J. Med. Chem. (2006) 49: 318-328 [PMID:16392816]
ChEMBL In vitro inhibition of [125I]DOI binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex B 8.82 pIC50 1.5 nM IC50 J. Med. Chem. (2003) 46: 4188-4195 [PMID:12954071]
ChEMBL In vitro relative agonist activity against 5-hydroxytryptamine 2A using PI assay in rat vascular smooth muscle cells F 6.74 pEC50 184 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 7.24 pEC50 58 nM EC50 J. Med. Chem. (2006) 49: 318-328 [PMID:16392816]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand B 7.89 pKi 13 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 7.89 pKi 13 nM Ki J. Med. Chem. (2006) 49: 318-328 [PMID:16392816]
GtoPdb - - 8.3 pKi - - - Naunyn Schmiedebergs Arch. Pharmacol. (2004) 370: 114-23 [PMID:15322733];
Mol. Pharmacol. (1994) 46: 227-34 [PMID:8078486];
Br. J. Pharmacol. (2004) 143: 549-60 [PMID:15466450]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL323] [GtoPdb: 7] [UniProtKB: P30994]
GtoPdb - - 8 pKi - - - Mol. Pharmacol. (1993) 43: 419-26 [PMID:8450835]
ChEMBL Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats F 8.38 pEC50 4.2 nM EC50 J. Med. Chem. (2006) 49: 318-328 [PMID:16392816]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL Evaluated for the binding affinity to porcine choroid plexus at 5-hydroxytryptamine 2C receptor binding site by using [3H]-MES as a radioligand. B 7.22 pKi 60 nM Ki J. Med. Chem. (1987) 30: 1-12 [PMID:3543362]
ChEMBL Displacement of [125I]DOI from cloned human 5HT2C receptor expressed in CHO cells B 8.15 pKi 7 nM Ki J. Med. Chem. (2006) 49: 318-328 [PMID:16392816]
ChEMBL Inhibitory constant against cloned human 5-hydroxytryptamine 2C receptor using with [125I]- DOI radioligand B 8.18 pKi 6.6 nM Ki J. Med. Chem. (2003) 46: 4188-4195 [PMID:12954071]
GtoPdb - - 8.6 pKi - - - Naunyn Schmiedebergs Arch. Pharmacol. (2004) 370: 114-23 [PMID:15322733];
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 Binding affinity was determined against 5-hydroxytryptamine 1C receptor was determined in male Sprague-Dawley rat brain. B 6.82 pKi 150 nM Ki J. Med. Chem. (1990) 33: 755-758 [PMID:2299641]
ChEMBL Activity against recombinant rat 5HT2C mediated intracellular calcium mobilization by FLIPR in SR3T3 cells F 8.74 pEC50 1.8 nM EC50 J. Med. Chem. (2006) 49: 318-328 [PMID:16392816]
5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939]
GtoPdb - - 6.7 pKi - - - Proc. Natl. Acad. Sci. U.S.A. (1993) 90: 408-12 [PMID:8380639]
5-HT4 receptor in Human [GtoPdb: 9] [UniProtKB: Q13639]
GtoPdb - - 5.8 pKi - - - Br. J. Pharmacol. (2004) 143: 549-60 [PMID:15466450];
EMBO J. (1995) 14: 2806-15 [PMID:7796807]
5-HT4 receptor in Rat [GtoPdb: 9] [UniProtKB: Q62758]
GtoPdb - - 6.6 pKi - - - Eur. J. Pharmacol. (1996) 304: 231-5 [PMID:8813606];
Neuropharmacology (1997) 36: 671-9 [PMID:9225293]
5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
GtoPdb - - 5.5 pKi - - - J. Neurochem. (1998) 71: 2169-77 [PMID:9798944]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]