dimethyltryptamine [Ligand Id: 141] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL12420 (N,n-dimethyltryptamine) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 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] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor 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/Serotonin 1a (5-HT1a) receptor 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/Serotonin 2a (5-HT2a) receptor 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/Serotonin 2a (5-HT2a) receptor 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/Serotonin 2b (5-HT2b) receptor 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/Serotonin 2b (5-HT2b) receptor 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/Serotonin 2c (5-HT2c) receptor 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] |
| Sigma-1 receptor 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] |
| sigma non-opioid intracellular receptor 1/Sigma opioid receptor 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] |
| 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 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]
