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 | Inhibition of 5-HT2AR (unknown origin ) assessed as inhibition constant | B | 6.97 | pKi | 107.2 | nM | Ki | RSC Med Chem (2024) 15: 998-1002 [PMID:38516602] |
| 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 | Agonist activity at human 5-HT2A receptor expressed in cells assessed as increase in calcium mobilization by Calcium-6 dye based FLIPR assay | F | 6 | pEC50 | <1000 | nM | EC50 | ACS Med Chem Lett (2022) 13: 749-751 [PMID:35586424] |
| ChEMBL | Agonist activity at human 5-HT2A receptor assessed as activation of calcium mobilization incubated for 2 mins by Calcium-6 dye based FLIPR assay | F | 6 | pEC50 | <1000 | nM | EC50 | ACS Med Chem Lett (2022) 13: 1397-1399 [PMID:36105333] |
| 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 human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay | F | 7.66 | pEC50 | 22 | nM | EC50 | ACS Med Chem Lett (2024) 15: 337-339 [PMID:38505858] |
| ChEMBL | Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay | F | 7.7 | pEC50 | 19.95 | nM | EC50 | ACS Med Chem Lett (2024) 15: 337-339 [PMID:38505858] |
| 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 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 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 | Inhibition of 5-HT2BR (unknown origin ) assessed as inhibition constant | B | 8.34 | pKi | 4.6 | nM | Ki | RSC Med Chem (2024) 15: 998-1002 [PMID:38516602] |
| 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 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]
