dimethyltryptamine [Ligand Id: 141] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL12420 (DEA NO. 7435, Dimethyltryptamine, N,n-dimethyltryptamine, NSC-63795)
  • 5-HT1A receptor/5-hydroxytryptamine receptor 1A in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/5-hydroxytryptamine receptor 1A in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT2A receptor/5-hydroxytryptamine receptor 2A in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
  • 5-HT2A receptor/5-hydroxytryptamine receptor 2A in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
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  • 5-HT2B receptor/5-hydroxytryptamine receptor 2B in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
  • 5-HT2B receptor/5-hydroxytryptamine receptor 2B in Rat [ChEMBL: CHEMBL323] [GtoPdb: 7] [UniProtKB: P30994]
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  • 5-HT2C receptor/5-hydroxytryptamine receptor 2C in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • sigma non-opioid intracellular receptor 1/Sigma non-opioid intracellular receptor 1 in Rat [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
  • Sigma non-opioid intracellular receptor 1 in Guinea pig [ChEMBL: CHEMBL4153] [UniProtKB: Q60492]
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  • 5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221]
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  • 5-HT6 receptor in Human [GtoPdb: 11] [UniProtKB: P50406]
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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 Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Displacement of [3H]8-OH-DPAT from 5HT1A receptor by vacuum filtration B 6.39 pKi 410 nM Ki J Nat Prod (1997) 60: 1196-1198
5-HT1A receptor/5-hydroxytryptamine receptor 1A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Compound was tested for the displacement of [3H]-8-OH- DPAT from rat brain 5-hydroxytryptamine 1A receptor B 6.59 pKi 259 nM Ki J Med Chem (1999) 42: 1106-1111 [PMID:10090793]
5-HT2A receptor/5-hydroxytryptamine receptor 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Compound was tested for the displacement of [125I]DOI from clone human 5-hydroxytryptamine 2A receptor B 7.19 pKi 65 nM Ki J Med Chem (1999) 42: 1106-1111 [PMID:10090793]
ChEMBL Agonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assay F 7.65 pEC50 22.2 nM EC50 ACS Med Chem Lett (2021) 12: 1874-1875 [PMID:34917241]
ChEMBL Agonist activity at 5-HT2A receptor (unknown origin) by calcium flux assay F 7.65 pEC50 22.2 nM EC50 ACS Med Chem Lett (2022) 13: 537-539 [PMID:35450349]
5-HT2A receptor/5-hydroxytryptamine receptor 2A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
ChEMBL Displacement of [3H]MDL100907 from 5HT2A receptor in Sprague-Dawley rat brain by liquid scintillation spectroscopy B 5.79 pKi 1636 nM Ki Bioorg Med Chem (2008) 16: 4661-4669 [PMID:18296055]
5-HT2B receptor/5-hydroxytryptamine receptor 2B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL Compound was tested for the displacement of [3H]5-HT from clone human 5-hydroxytryptamine 2B receptor B 7 pKi 101 nM Ki J Med Chem (1999) 42: 1106-1111 [PMID:10090793]
5-HT2B receptor/5-hydroxytryptamine receptor 2B in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL323] [GtoPdb: 7] [UniProtKB: P30994]
ChEMBL The binding affinity to 5-hydroxytryptamine 2B receptor of rat fundus B 6 pKd 1000 nM Kd J Med Chem (1982) 25: 68-70 [PMID:7086824]
5-HT2C receptor/5-hydroxytryptamine receptor 2C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL Compound was tested for the displacement of [125I]DOI from cloned human 5-hydroxytryptamine 2C receptor B 7.48 pKi 33 nM Ki J Med Chem (1999) 42: 1106-1111 [PMID:10090793]
GABAA receptor π subunit/GABAA receptor β1 subunit/GABAA receptor δ subunit/GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor γ1 subunit/GABAA receptor α2 subunit/GABAA receptor α4 subunit/GABAA receptor γ3 subunit/GABAA receptor α6 subunit/GABAA receptor α1 subunit/GABAA receptor β3 subunit/GABAA receptor β2 subunit/GABAA receptor ε subunit/GABA-A receptor; anion channel in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907607] [GtoPdb: 419, 410, 416, 414, 408, 406, 413, 405, 407, 415, 409, 404, 412, 411, 417] [UniProtKB: O09028, P15431, P18506, P18508, P19969, P20236, P23574, P23576, P28471, P28473, P30191, P62813, P63079, P63138, Q91ZM7, Q9ES14]
ChEMBL In vitro inhibition of [3H]diazepam binding to benzodiazepine receptor in rat cerebral cortical membrane B 4 pKi >100000 nM Ki J Med Chem (1982) 25: 1081-1091 [PMID:6127411]
sigma non-opioid intracellular receptor 1/Sigma non-opioid intracellular receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in rat liver homogenates B 4.81 pKi 15400 nM Ki J Med Chem (2013) 56: 9809-9819 [PMID:23964901]
Sigma non-opioid intracellular receptor 1 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4153] [UniProtKB: Q60492]
ChEMBL Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain by scintillation analyzer B 4.82 pKi 15000 nM Ki Bioorg Med Chem (2011) 19: 3141-3151 [PMID:21531141]
5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221]
GtoPdb - - 7.3 pKi - - - Mol Pharmacol (1996) 50: 1567-80 [PMID:8967979]
5-HT6 receptor in Human [GtoPdb: 11] [UniProtKB: P50406]
GtoPdb - - 7.2 pKi - - - J Neurochem (1996) 66: 47-56 [PMID:8522988]

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]