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ChEMBL ligand: CHEMBL26687 (2-(3,4,5-Trimethoxyphenyl)Ethanamine, Mescaline, M (psychedelic), NSC-30419) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
ChEMBL | Ability to displace [3H]-8-OH-DPAT from rat hippocampal homogenate 5-hydroxytryptamine 1A receptor | B | 5.16 | pKi | 6900 | nM | Ki | J Med Chem (1997) 40: 2997-3008 [PMID:9301661] |
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
ChEMBL | Agonist activity at cloned human 5-hydroxytryptamine 2A receptor using [125I]DOI radioligand | F | 6.26 | pKi | 551 | nM | Ki | J Med Chem (1997) 40: 2997-3008 [PMID:9301661] |
GtoPdb | Potency determined in an IP3 accumulation assay | - | 5.59 | pEC50 | 2600 | nM | EC50 | J Med Chem (2003) 46: 3526-35 [PMID:12877591] |
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842] | ||||||||
ChEMBL | Ability to displace [3H]ketanserin from rat cortical homogenate 5-hydroxytryptamine 2A receptor | B | 5.26 | pKi | 5500 | nM | Ki | J Med Chem (1997) 40: 2997-3008 [PMID:9301661] |
ChEMBL | Displacement of [3H]ketanserin from 5HT2A receptor in Sprague-Dawley rat brain by liquid scintillation spectroscopy | B | 5.26 | pKi | 5500 | nM | Ki | Bioorg Med Chem (2008) 16: 4661-4669 [PMID:18296055] |
ChEMBL | Displacement of [125I]DOI from rat 5HT2A receptor | B | 6.44 | pKi | 360 | nM | Ki | J Med Chem (2006) 49: 4269-4274 [PMID:16821786] |
ChEMBL | Activity at rat 5HT2A receptor assessed as 5-HT-stimulated IP3 accumulation | F | 4.95 | pEC50 | 11300 | nM | EC50 | J Med Chem (2006) 49: 4269-4274 [PMID:16821786] |
ChEMBL | Effect on phosphoinositide hydrolysis in NIH 3T3 fibroblast 5-hydroxytryptamine 2A receptor | F | 5.4 | pEC50 | 4000 | nM | EC50 | J Med Chem (1997) 40: 2997-3008 [PMID:9301661] |
ChEMBL | Tested for its ability to activate phospholipase c by quantification of IP3 at cloned rat 5-hydroxytryptamine 2A receptor | B | 5.59 | pEC50 | 2600 | nM | EC50 | J Med Chem (2003) 46: 3526-3535 [PMID:12877591] |
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
ChEMBL | Agonist activity at cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT radioligand | F | 6.1 | pKi | 795.1 | nM | Ki | J Med Chem (1997) 40: 2997-3008 [PMID:9301661] |
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
ChEMBL | Agonist activity at cloned human 5-hydroxytryptamine 2C receptor using [125I]DOI radioligand | F | 6.52 | pKi | 302.8 | nM | Ki | J Med Chem (1997) 40: 2997-3008 [PMID:9301661] |
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909] | ||||||||
ChEMBL | Displacement of [125I]DOI from rat 5HT2C receptor | B | 6.42 | pKi | 380 | nM | Ki | J Med Chem (2006) 49: 4269-4274 [PMID:16821786] |
ChEMBL | Effect on phosphoinositide hydrolysis in NIH 3T3 fibroblast 5-hydroxytryptamine 2C receptor | F | 4.62 | pEC50 | 24000 | nM | EC50 | J Med Chem (1997) 40: 2997-3008 [PMID:9301661] |
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]