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 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]
