mescaline [Ligand Id: 13139] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL26687 (2-(3,4,5-Trimethoxyphenyl)Ethanamine, Mescaline, M (psychedelic), NSC-30419)
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
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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 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]