psilocin [Ligand Id: 11291] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL65547 (4-ho-dmt, Psilocin, Psilocyn) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Modulation of human 5HT2A expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assay | B | 8.08 | pIC50 | 8.34 | nM | IC50 | ACS Med Chem Lett (2021) 12: 1876-1878 [PMID:34917242] |
| ChEMBL | Displacement of [3H]-ketanserin from human 5-HT2A receptor incubated for 90 mins by scintillation counting analysis | B | 7.12 | pEC50 | 75.2 | nM | EC50 | ACS Med Chem Lett (2021) 12: 1519-1520 [PMID:34676027] |
| ChEMBL | Effective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2A receptor determined by phosphoinositide hydrolysis assay | F | 7.62 | pEC50 | 24 | nM | EC50 | Bioorg Med Chem Lett (2005) 15: 4555-4559 [PMID:16061378] |
| GtoPdb | Determined in an [3H]inositol phosphate accumulation assay in cells stably expressing h5-HT2A. | - | 7.62 | pEC50 | 24 | nM | EC50 | Bioorg Med Chem Lett (2005) 15: 4555-9 [PMID:16061378] |
| ChEMBL | Agonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells by FLIPR calcium flux assay | F | 8.19 | pEC50 | 6.5 | 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 | 8.19 | pEC50 | 6.5 | nM | EC50 | ACS Med Chem Lett (2022) 13: 537-539 [PMID:35450349] |
| ChEMBL | Agonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay | F | 8.37 | pEC50 | 4.3 | nM | EC50 | J Nat Prod (2020) 83: 461-467 [PMID:32077284] |
| ChEMBL | Agonist activity at human 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay | F | 8.37 | pEC50 | 4.27 | nM | EC50 | J Nat Prod (2020) 83: 461-467 [PMID:32077284] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5377] [GtoPdb: 6] [UniProtKB: P35363] | ||||||||
| ChEMBL | Agonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay | F | 8 | pEC50 | 9.9 | nM | EC50 | J Nat Prod (2020) 83: 461-467 [PMID:32077284] |
| ChEMBL | Agonist activity at mouse 5-HT2A receptor expressed in Flp-In T-REx 293 cells assessed as induction of Gq-mediated calcium flux incubated for 1 hr by Flou4-AM dye based FLIPR assay | F | 8.01 | pEC50 | 9.77 | nM | EC50 | J Nat Prod (2020) 83: 461-467 [PMID:32077284] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842] | ||||||||
| ChEMBL | Compound was tested for binding affinity using [3H]MDL-100,907 at 5-hydroxytryptamine 2A receptor sites in rat cortical homogenate. | B | 6.41 | pKi | 390 | nM | Ki | J Med Chem (1999) 42: 4257-4263 [PMID:10514296] |
| ChEMBL | Displacement of [3H]MDL100907 from 5HT2A receptor in Sprague-Dawley rat brain by liquid scintillation spectroscopy | B | 6.49 | pKi | 323 | nM | Ki | Bioorg Med Chem (2008) 16: 4661-4669 [PMID:18296055] |
| ChEMBL | In vitro binding to 5-hydroxytryptamine 2A receptor using [125 I]-DOI | B | 7.6 | pKi | 25 | nM | Ki | J Med Chem (2003) 46: 3526-3535 [PMID:12877591] |
| ChEMBL | Tested for its ability to activate phospholipase C by quantification of IP3 at cloned rat 5-hydroxytryptamine 2A receptor | B | 5.64 | pEC50 | 2300 | 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 | Modulation of human 5HT2B expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assay | B | 8.97 | pIC50 | 1.07 | nM | IC50 | ACS Med Chem Lett (2021) 12: 1876-1878 [PMID:34917242] |
| ChEMBL | Effective concentration required for accumulation of [3H]inositol phosphate in cells transiently expressing human 5-hydroxytryptamine 2B receptor determined by phosphoinositide hydrolysis assay | F | 7.24 | pEC50 | 58 | nM | EC50 | Bioorg Med Chem Lett (2005) 15: 4555-4559 [PMID:16061378] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Modulation of human 5HT2C expressed in HEK293T cells co-transfected with Galphaq-RLuc8, Ggamma1-GFP2 and Gbeta1 assessed as dissociation of Galphaq from Ggamma1 preincubated for 1 hr followed by addition of coelenterazine 400a substrate and measured after 15 mins by BRET assay | B | 8.11 | pIC50 | 7.79 | nM | IC50 | ACS Med Chem Lett (2021) 12: 1876-1878 [PMID:34917242] |
| ChEMBL | Effective concentration required for accumulation of [3H]inositol phosphate in cells stably expressing human 5-hydroxytryptamine 2C receptor determined by phosphoinositide hydrolysis assay | F | 7.52 | pEC50 | 30 | nM | EC50 | Bioorg Med Chem Lett (2005) 15: 4555-4559 [PMID:16061378] |
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]
