2-methyl-5-HT [Ligand Id: 218] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL266591 |
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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 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/5-hydroxytryptamine receptor 1B 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/5-hydroxytryptamine receptor 1D 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/5-hydroxytryptamine receptor 1E 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/5-hydroxytryptamine receptor 2C 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-hydroxytryptamine receptor 3A 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/5-hydroxytryptamine receptor 5A 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/5-hydroxytryptamine receptor 5A 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/5-hydroxytryptamine receptor 6 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/5-hydroxytryptamine receptor 7 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-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-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 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]
