2-methyl-5-HT [Ligand Id: 218] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL266591
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT1B receptor in Human [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-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
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  • 5-HT3A/Serotonin 3a (5-HT3a) receptor in Human [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
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  • 5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
  • 5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Mouse [ChEMBL: CHEMBL3597] [GtoPdb: 10] [UniProtKB: P30966]
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  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
  • 5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
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  • 5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939]
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  • 5-HT2B receptor in Rat [GtoPdb: 7] [UniProtKB: P30994]
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  • 5-HT3AB in Human [GtoPdb: 378]
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  • 5-HT3A in Human [GtoPdb: 379]
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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 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 5.6 pKi 2511.89 nM Ki J. Med. Chem. (1996) 39: 126-134 [PMID:8568799]
ChEMBL Binding affinity was determined against 5-hydroxytryptamine 1A receptor was determined in male Sprague-Dawley rat brain. B 5.92 pKi 1200 nM Ki J. Med. Chem. (1990) 33: 755-758 [PMID:2299641]
5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222]
GtoPdb - - 6.1 pKi - - - Proc Natl Acad Sci USA (1992) 89: 3630-4 [PMID:1565658]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
ChEMBL Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain. B 6.28 pKi 520 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]
ChEMBL Binding affinity was determined against 5-hydroxytryptamine 1D receptor in bovine caudate homogenate B 5.91 pKi 1220 nM Ki J. Med. Chem. (1990) 33: 755-758 [PMID:2299641]
GtoPdb - - 6.2 pKi - - - Proc Natl Acad Sci USA (1992) 89: 3630-4 [PMID:1565658];
Mol Pharmacol (1996) 50: 1567-80 [PMID:8967979]
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 - - 6.1 pKi - - - Proc Natl Acad Sci USA (1993) 90: 408-12 [PMID:8380639]
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 6.19 pKi 650 nM Ki J. Med. Chem. (1990) 33: 755-758 [PMID:2299641]
5-HT3A/5-HT3B/Serotonin 3 (5-HT3) receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094116] [GtoPdb: 373, 374] [UniProtKB: P35563, Q9JJ16]
ChEMBL In vitro displacement of [3H]ICS-205-930 from 5-hydroxytryptamine 3 receptor in cultured NG-108-15 rat glioma cells B 5.91 pKi 1217 nM Ki J. Med. Chem. (1990) 33: 13-16 [PMID:2296012]
ChEMBL The compound was tested for the binding affinity against 5-hydroxytryptamine 3 receptor using [3H]zacopride as radioligand. B 6.7 pKi 199.53 nM Ki J. Med. Chem. (1999) 42: 4362-4379 [PMID:10543880]
ChEMBL Inhibition of [3H]BRL-43694 binding to 5-hydroxytryptamine 3 receptor of rat cortical homogenate. B 6.11 pIC50 779 nM IC50 J. Med. Chem. (1997) 40: 3670-3678 [PMID:9357534]
ChEMBL Compound was evaluated for the displacement of [3H]-Q-ICS 205-930 binding to 5-hydroxytryptamine 3 receptor in rat brain membranes B 6.19 pIC50 645.65 nM IC50 J. Med. Chem. (1991) 34: 140-151 [PMID:1992112]
ChEMBL Compound was evaluated for the displacement of [3H]Q-ICS-205-930 from 5-HT3 recognition sites in rat brain membranes B 6.19 pIC50 645.65 nM IC50 J. Med. Chem. (1992) 35: 1019-1031 [PMID:1552497]
5-HT3A/Serotonin 3a (5-HT3a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
ChEMBL Compound was evaluated for its binding affinity towards 5-hydroxytryptamine 3 receptor B 5.92 pKi 1200 nM Ki J. Med. Chem. (2000) 43: 1011-1018 [PMID:10715164]
5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 5A receptor B 5 pKi >10000 nM Ki J. Med. Chem. (2003) 46: 2795-2812 [PMID:12825922]
5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3597] [GtoPdb: 10] [UniProtKB: P30966]
ChEMBL Binding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [3H]LSD as radioligand B 5 pKi >10000 nM Ki J. Med. Chem. (2003) 46: 2795-2812 [PMID:12825922]
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligand B 6.4 pKi 400 nM Ki J. Med. Chem. (2003) 46: 2795-2812 [PMID:12825922]
ChEMBL Binding affinity towards 5-hydroxytryptamine 6 receptor B 7.34 pKi 46 nM Ki J. Med. Chem. (2003) 46: 2795-2812 [PMID:12825922]
ChEMBL Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand B 7.34 pKi 46 nM Ki J. Med. Chem. (2000) 43: 1011-1018 [PMID:10715164]
5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
GtoPdb - - 7.3 pKi - - - Neuropharmacology (1997) 36: 713-20 [PMID:9225298]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
ChEMBL Binding affinity of compound towards rodent 5-hydroxytryptamine 7 receptor B 5.9 pKi 1258 nM Ki J. Med. Chem. (2003) 46: 2795-2812 [PMID:12825922]
5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939]
GtoPdb - - 6.4 pKi - - - Proc Natl Acad Sci USA (1993) 90: 408-12 [PMID:8380639]
5-HT2B receptor in Rat [GtoPdb: 7] [UniProtKB: P30994]
GtoPdb - - 6.6 pKi - - - Mol Pharmacol (1993) 43: 419-26 [PMID:8450835]
5-HT3AB in Human [GtoPdb: 378]
GtoPdb - - 4.9 pEC50 - - - Nature (1999) 397: 359-63 [PMID:9950429]
5-HT3A in Human [GtoPdb: 379]
GtoPdb - - 6.7 pKi - - - Mol Pharmacol (1995) 48: 407-16 [PMID:7565620];
Mol Pharmacol (1998) 53: 202-12 [PMID:9463477];
Br J Pharmacol (1996) 118: 1237-45 [PMID:8818349];
Eur J Pharmacol (2000) 409: 195-201 [PMID:11104834]
GtoPdb - - 5.6 pEC50 2500 nM EC50 Nature (1999) 397: 359-63 [PMID:9950429];
Mol Pharmacol (1995) 48: 1054-62 [PMID:8848005];
Mol Pharmacol (1995) 48: 407-16 [PMID:7565620];
Mol Pharmacol (1998) 53: 202-12 [PMID:9463477]

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]