α-methyl-5-HT [Ligand Id: 152] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL275854 |
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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 USA (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 USA (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 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]
