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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
