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 34:

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]