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-HT1A receptor/5-hydroxytryptamine receptor 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Radioligand Binding Assay: The binding affinities shown in table 5 of psilocin and compound 8 at various monoaminergic receptors were determined in radioligand competition binding assays by Psychiatric Drug Screening Program according to the experimental described in Assay Protocol Book, Version III 11, 16. As shown compound 8 shows less affinity for various monoaminergic receptors compared to Psilocin. | B | 7.2 | pKi | 63 | nM | Ki | US-11642336-B2. 5-HT2A agonists for use in treatment of depression (2023) |
| 5-HT1B receptor/5-hydroxytryptamine receptor 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
| ChEMBL | Radioligand Binding Assay: The binding affinities shown in table 5 of psilocin and compound 8 at various monoaminergic receptors were determined in radioligand competition binding assays by Psychiatric Drug Screening Program according to the experimental described in Assay Protocol Book, Version III 11, 16. As shown compound 8 shows less affinity for various monoaminergic receptors compared to Psilocin. | B | 6.52 | pKi | 305 | nM | Ki | US-11642336-B2. 5-HT2A agonists for use in treatment of depression (2023) |
| 5-HT1D receptor/5-hydroxytryptamine receptor 1D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
| ChEMBL | Radioligand Binding Assay: The binding affinities shown in table 5 of psilocin and compound 8 at various monoaminergic receptors were determined in radioligand competition binding assays by Psychiatric Drug Screening Program according to the experimental described in Assay Protocol Book, Version III 11, 16. As shown compound 8 shows less affinity for various monoaminergic receptors compared to Psilocin. | B | 7.72 | pKi | 19 | nM | Ki | US-11642336-B2. 5-HT2A agonists for use in treatment of depression (2023) |
| 5-ht1e receptor/5-hydroxytryptamine receptor 1E in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566] | ||||||||
| ChEMBL | Radioligand Binding Assay: The binding affinities shown in table 5 of psilocin and compound 8 at various monoaminergic receptors were determined in radioligand competition binding assays by Psychiatric Drug Screening Program according to the experimental described in Assay Protocol Book, Version III 11, 16. As shown compound 8 shows less affinity for various monoaminergic receptors compared to Psilocin. | B | 7.36 | pKi | 44 | nM | Ki | US-11642336-B2. 5-HT2A agonists for use in treatment of depression (2023) |
| 5-HT2A receptor/5-hydroxytryptamine receptor 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Radioligand Binding Assay: The binding affinities shown in table 5 of psilocin and compound 8 at various monoaminergic receptors were determined in radioligand competition binding assays by Psychiatric Drug Screening Program according to the experimental described in Assay Protocol Book, Version III 11, 16. As shown compound 8 shows less affinity for various monoaminergic receptors compared to Psilocin. | B | 6.47 | pKi | 340 | nM | Ki | US-11642336-B2. 5-HT2A agonists for use in treatment of depression (2023) |
| 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 | Radioligand Binding Assay: Table 2: i. Prepare the assay buffer following the table below;Reagent ConcentrationTris 50 mMCaCl2 4 mMBSA 0.1% (w/v)Adjust pH to 7.4 followed by 0.2 μM sterile filtrationii. Preparation of 8 doses of reference and test compounds starting from 10 mM stock solution as requested by 5-fold serial dilutions with 100%;iii. Prepare (v/v) DMSO: a. Add 50 μl/well of 0.5% (v/v) PEI to UniFilter-96 GF/B plates. Seal the plates and incubate at 4° C. for 3 hrs; b. After incubation, wash the plates 3 times with ice-cold wash buffer (50 mM Tris, pH7.4);iv. Preparation of assay plates: a. Dilute cell membrane with assay buffer and add 330 μl/well to 96 round deep well plates to reach a concentration of 20 μg/well; b. Prepare 8 concentrations of reference or exemplary compounds of the application and add 110 μl/well to 96 round deep well plates; c. Dilute [3H]-ketanserin with assay buffer to 5 nM (5× final concentration) and add 110 μl/well to 96 round deep well plates.v. Centrifuge the plate at 1000 rpm for 30 secs and then agitate at 600 rpm, R.T. for 5 min.vi. Seal the plates and incubate the plate at 27° C. for 90 min.vii. Stop the incubation by vacuum filtration onto GF/B filter plates followed by 4 times washing with ice-cold wash buffer (50 mM Tris, pH7.4).viii. Dry the plates at 37° C. for 45 min.ix. Seal the filter plates and add 40 μl/well of scintillation cocktail.x. Read the plate by using a Microbeta2 microplate counter. | B | 6.3 | pIC50 | <500 | nM | IC50 | US-11427604-B2. Psilocin derivatives as serotonergic psychedelic agents for the treatment of CNS disorders (2022) |
| ChEMBL | Radioligand Binding Assay: Table 2: i. Prepare the assay buffer following the table below;Reagent ConcentrationTris 50 mMCaCl2 4 mMBSA 0.1% (w/v)Adjust pH to 7.4 followed by 0.2 μM sterile filtrationii. Preparation of 8 doses of reference and test compounds starting from 10 mM stock solution as requested by 5-fold serial dilutions with 100%;iii. Prepare (v/v) DMSO: a. Add 50 μl/well of 0.5% (v/v) PEI to UniFilter-96 GF/B plates. Seal the plates and incubate at 4° C. for 3 hrs; b. After incubation, wash the plates 3 times with ice-cold wash buffer (50 mM Tris, pH7.4);iv. Preparation of assay plates: a. Dilute cell membrane with assay buffer and add 330 μl/well to 96 round deep well plates to reach a concentration of 20 μg/well; b. Prepare 8 concentrations of reference or exemplary compounds of the application and add 110 μl/well to 96 round deep well plates; c. Dilute [3H]-ketanserin with assay buffer to 5 nM (5× final concentration) and add 110 μl/well to 96 round deep well plates.v. Centrifuge the plate at 1000 rpm for 30 secs and then agitate at 600 rpm, R.T. for 5 min.vi. Seal the plates and incubate the plate at 27° C. for 90 min.vii. Stop the incubation by vacuum filtration onto GF/B filter plates followed by 4 times washing with ice-cold wash buffer (50 mM Tris, pH7.4).viii. Dry the plates at 37° C. for 45 min.ix. Seal the filter plates and add 40 μl/well of scintillation cocktail.x. Read the plate by using a Microbeta2 microplate counter. | B | 6.3 | pIC50 | <500 | nM | IC50 | US-11427604-B2. Psilocin derivatives as serotonergic psychedelic agents for the treatment of CNS disorders (2022) |
| ChEMBL | Radioligand Binding Assay: i. Prepare the assay buffer following the table below;Reagent ConcentrationTris 50 mMCaCl2 4 mMBSA 0.1% (w/v)Adjust pH to 7.4 followed by 0.2 μM sterile filtrationii. Preparation of 8 doses of reference and exemplary test compounds starting from 10 mM stock solution as requested by 5-fold serial dilutions with 100%;iii. Prepare (v/v) DMSO: a. Add 50 μl/well of 0.5% (v/v) PEI to UniFilter-96 GF/B plates. Seal the plates and incubate at 4° C. for 3 hrs; b. After incubation, wash the plates 3 times with ice-cold wash buffer (50 mM Tris, pH7.4);iv. Preparation of assay plates: a. Dilute cell membrane with assay buffer and add 330 μl/well to 96 round deep well plates to reach a concentration of 20 μg/well; b. Prepare 8 concentrations of reference or exemplary test compounds and add 110 μl/well to 96 round deep well plates; c. Dilute [3H]-ketanserin with assay buffer to 5 nM (5× final concentration) and add 110 μl/well to 96 round deep well plates.v. Centrifuge the plate at 1000 rpm for 30 secs and then agitate at 600 rpm, R.T. for 5 min.vi. Seal the plates and incubate the plate at 27° C. for 90 min.vii. Stop the incubation by vacuum filtration onto GF/B filter plates followed by 4 times washing with ice-cold wash buffer (50 mM Tris, pH7.4).vii. Dry the plates at 37° C. for 45 min.ix. Seal the filter plates and add 40 μl/well of scintillation cocktail.x. Read the plate by using a Microbeta2 microplate counter. | B | 6.3 | pIC50 | <500 | nM | IC50 | US-11453689-B2. 3-pyrrolidine-indole derivatives as serotonergic psychedelic agents for the treatment of CNS disorders (2022) |
| ChEMBL | FLIPR Assay: 1. Culture the cells in cell culture medium (DMEM containing 10% FBS 1× penicillin-streptomycin 300 μg/ml G418 and 100 μg/ml hygromycin B) at 37° C., 5% (v/v) CO2. One day before the assays, detach the cell using TrypLE Express and count cells using cell counter. Only cells with >85% viability are used for the assay. 3. Seed 20000 cells/well in 30 μl/well culture medium to a 384-well cell plate and incubate the cells overnight at 37° C., 5% (v/v) CO2. 4. On the assay day, prepare 2× dye solution following the manual of the FLIPR® Calcium 6 Assay Kit: i. Dilute the dye with assay buffer (20 mM HEPES in 1×HBSS, PH7.4); ii. Add probenecid to the final concentration of 5 mM; iii. Vortex vigorously for 1-2 minutes. 5. Medium from cell plate by flicking the cell plate on towel papers. 6. Add 10 μl of assay buffer and 10 μl of 2× dye solution to each well of the cell plate. 7. Put the cell plate on plate shaker, agitate the plate at 600 rpm for 2 minutes. Incubate the plate at 37° C. for 2 hours followed by additional 15-minute incubation at 25° C. 8. Prepare 3× compound in assay buffer: a. Dilute reference compounds to required concentration with DMSO. Add the compounds to a 384-well compound plate; b. Perform serial dilutions; c. Add 10 mM test compounds to the compound plate, perform 3-fold serial dilutions. d. Transfer 60 nl/well of compounds from source plate to a 384-well compound plate (Corning, 3657) by using an Echo; e. Add 20 μl/well assay buffer to the compound plate; f. Mix the plate-on-plate shaker for 2 mins; 9. Put the cell plate, compound plate and tips into FLIPR, transfer 10 μl of 3× compound to the cell plate per well with FLIPR. I.d Data Analysis i. The normalized fluorescence reading (RFU) is calculated as shown follow, while Fmax and Fmin stand for maximum and minimum of calcium signal during defined time window: RFU=Fmax−Fmin | B | 6.45 | pIC50 | 352 | nM | IC50 | US-11591353-B2. Psilocin derivatives as serotonergic psychedelic agents for the treatment of CNS disorders (2023) |
| ChEMBL | FLIPR Assay: 1. Culture the cells in cell culture medium (DMEM containing 10% FBS 1× penicillin-streptomycin 300 μg/ml G418 and 100 μg/ml hygromycin B) at 37° C., 5% (v/v) CO2. One day before the assays, detach the cell using TrypLE Express and count cells using cell counter. Only cells with >85% viability are used for the assay. 3. Seed 20000 cells/well in 30 μl/well culture medium to a 384-well cell plate and incubate the cells overnight at 37° C., 5% (v/v) CO2. 4. On the assay day, prepare 2× dye solution following the manual of the FLIPR® Calcium 6 Assay Kit: i. Dilute the dye with assay buffer (20 mM HEPES in 1×HBSS, PH7.4); ii. Add probenecid to the final concentration of 5 mM; iii. Vortex vigorously for 1-2 minutes. 5. Medium from cell plate by flicking the cell plate on towel papers. 6. Add 10 μl of assay buffer and 10 μl of 2× dye solution to each well of the cell plate. 7. Put the cell plate on plate shaker, agitate the plate at 600 rpm for 2 minutes. Incubate the plate at 37° C. for 2 hours followed by additional 15-minute incubation at 25° C. 8. Prepare 3× compound in assay buffer: a. Dilute reference compounds to required concentration with DMSO. Add the compounds to a 384-well compound plate; b. Perform serial dilutions; c. Add 10 mM test compounds to the compound plate, perform 3-fold serial dilutions. d. Transfer 60 nl/well of compounds from source plate to a 384-well compound plate (Corning, 3657) by using an Echo; e. Add 20 μl/well assay buffer to the compound plate; f. Mix the plate-on-plate shaker for 2 mins; 9. Put the cell plate, compound plate and tips into FLIPR, transfer 10 μl of 3× compound to the cell plate per well with FLIPR. I.d Data Analysis i. The normalized fluorescence reading (RFU) is calculated as shown follow, while Fmax and Fmin stand for maximum and minimum of calcium signal during defined time window: RFU=Fmax−Fmin | B | 6.95 | pIC50 | 112 | nM | IC50 | US-11591353-B2. Psilocin derivatives as serotonergic psychedelic agents for the treatment of CNS disorders (2023) |
| 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 | Radioligand Binding Assay: i. Prepare the assay buffer following the table below;Reagent ConcentrationTris 50 mMCaCl2 4 mMBSA 0.1% (w/v)Adjust pH to 7.4 followed by 0.2 μM sterile filtrationii. Preparation of 8 doses of reference and exemplary test compounds starting from 10 mM stock solution as requested by 5-fold serial dilutions with 100%;iii. Prepare (v/v) DMSO: a. Add 50 μl/well of 0.5% (v/v) PEI to UniFilter-96 GF/B plates. Seal the plates and incubate at 4° C. for 3 hrs; b. After incubation, wash the plates 3 times with ice-cold wash buffer (50 mM Tris, pH7.4);iv. Preparation of assay plates: a. Dilute cell membrane with assay buffer and add 330 μl/well to 96 round deep well plates to reach a concentration of 20 μg/well; b. Prepare 8 concentrations of reference or exemplary test compounds and add 110 μl/well to 96 round deep well plates; c. Dilute [3H]-ketanserin with assay buffer to 5 nM (5× final concentration) and add 110 μl/well to 96 round deep well plates.v. Centrifuge the plate at 1000 rpm for 30 secs and then agitate at 600 rpm, R.T. for 5 min.vi. Seal the plates and incubate the plate at 27° C. for 90 min.vii. Stop the incubation by vacuum filtration onto GF/B filter plates followed by 4 times washing with ice-cold wash buffer (50 mM Tris, pH7.4).vii. Dry the plates at 37° C. for 45 min.ix. Seal the filter plates and add 40 μl/well of scintillation cocktail.x. Read the plate by using a Microbeta2 microplate counter. | B | 6 | pEC50 | <1000 | nM | EC50 | US-11453689-B2. 3-pyrrolidine-indole derivatives as serotonergic psychedelic agents for the treatment of CNS disorders (2022) |
| 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/5-hydroxytryptamine receptor 2A 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/5-hydroxytryptamine receptor 2A 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/5-hydroxytryptamine receptor 2B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| ChEMBL | Radioligand Binding Assay: The binding affinities shown in table 5 of psilocin and compound 8 at various monoaminergic receptors were determined in radioligand competition binding assays by Psychiatric Drug Screening Program according to the experimental described in Assay Protocol Book, Version III 11, 16. As shown compound 8 shows less affinity for various monoaminergic receptors compared to Psilocin. | B | 8.33 | pKi | 4.7 | nM | Ki | US-11642336-B2. 5-HT2A agonists for use in treatment of depression (2023) |
| 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/5-hydroxytryptamine receptor 2C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Radioligand Binding Assay: The binding affinities shown in table 5 of psilocin and compound 8 at various monoaminergic receptors were determined in radioligand competition binding assays by Psychiatric Drug Screening Program according to the experimental described in Assay Protocol Book, Version III 11, 16. As shown compound 8 shows less affinity for various monoaminergic receptors compared to Psilocin. | B | 6.85 | pKi | 140 | nM | Ki | US-11642336-B2. 5-HT2A agonists for use in treatment of depression (2023) |
| 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] |
| 5-HT5A receptor/5-hydroxytryptamine receptor 5A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898] | ||||||||
| ChEMBL | Radioligand Binding Assay: The binding affinities shown in table 5 of psilocin and compound 8 at various monoaminergic receptors were determined in radioligand competition binding assays by Psychiatric Drug Screening Program according to the experimental described in Assay Protocol Book, Version III 11, 16. As shown compound 8 shows less affinity for various monoaminergic receptors compared to Psilocin. | B | 7.15 | pKi | 70 | nM | Ki | US-11642336-B2. 5-HT2A agonists for use in treatment of depression (2023) |
| 5-HT6 receptor/5-hydroxytryptamine receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
| ChEMBL | Radioligand Binding Assay: The binding affinities shown in table 5 of psilocin and compound 8 at various monoaminergic receptors were determined in radioligand competition binding assays by Psychiatric Drug Screening Program according to the experimental described in Assay Protocol Book, Version III 11, 16. As shown compound 8 shows less affinity for various monoaminergic receptors compared to Psilocin. | B | 7.14 | pKi | 72 | nM | Ki | US-11642336-B2. 5-HT2A agonists for use in treatment of depression (2023) |
| 5-HT7 receptor/5-hydroxytryptamine receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
| ChEMBL | Radioligand Binding Assay: The binding affinities shown in table 5 of psilocin and compound 8 at various monoaminergic receptors were determined in radioligand competition binding assays by Psychiatric Drug Screening Program according to the experimental described in Assay Protocol Book, Version III 11, 16. As shown compound 8 shows less affinity for various monoaminergic receptors compared to Psilocin. | B | 7.14 | pKi | 72 | nM | Ki | US-11642336-B2. 5-HT2A agonists for use in treatment of depression (2023) |
| A1 receptor/Adenosine receptor A1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542] | ||||||||
| ChEMBL | Radioligand Binding Assay: The binding affinities shown in table 5 of psilocin and compound 8 at various monoaminergic receptors were determined in radioligand competition binding assays by Psychiatric Drug Screening Program according to the experimental described in Assay Protocol Book, Version III 11, 16. As shown compound 8 shows less affinity for various monoaminergic receptors compared to Psilocin. | B | 5 | pKi | >10000 | nM | Ki | US-11642336-B2. 5-HT2A agonists for use in treatment of depression (2023) |
| A2A receptor/Adenosine receptor A2a in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
| ChEMBL | Radioligand Binding Assay: The binding affinities shown in table 5 of psilocin and compound 8 at various monoaminergic receptors were determined in radioligand competition binding assays by Psychiatric Drug Screening Program according to the experimental described in Assay Protocol Book, Version III 11, 16. As shown compound 8 shows less affinity for various monoaminergic receptors compared to Psilocin. | B | 5.7 | pKi | 2000 | nM | Ki | US-11642336-B2. 5-HT2A agonists for use in treatment of depression (2023) |
| A2B receptor/Adenosine receptor A2b in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275] | ||||||||
| ChEMBL | Radioligand Binding Assay: The binding affinities shown in table 5 of psilocin and compound 8 at various monoaminergic receptors were determined in radioligand competition binding assays by Psychiatric Drug Screening Program according to the experimental described in Assay Protocol Book, Version III 11, 16. As shown compound 8 shows less affinity for various monoaminergic receptors compared to Psilocin. | B | 5.89 | pKi | 1300 | nM | Ki | US-11642336-B2. 5-HT2A agonists for use in treatment of depression (2023) |
| D1 receptor/D(1A) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] | ||||||||
| ChEMBL | Radioligand Binding Assay: The binding affinities shown in table 5 of psilocin and compound 8 at various monoaminergic receptors were determined in radioligand competition binding assays by Psychiatric Drug Screening Program according to the experimental described in Assay Protocol Book, Version III 11, 16. As shown compound 8 shows less affinity for various monoaminergic receptors compared to Psilocin. | B | 7.7 | pKi | 20 | nM | Ki | US-11642336-B2. 5-HT2A agonists for use in treatment of depression (2023) |
| D5 receptor/D(1B) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918] | ||||||||
| ChEMBL | Radioligand Binding Assay: The binding affinities shown in table 5 of psilocin and compound 8 at various monoaminergic receptors were determined in radioligand competition binding assays by Psychiatric Drug Screening Program according to the experimental described in Assay Protocol Book, Version III 11, 16. As shown compound 8 shows less affinity for various monoaminergic receptors compared to Psilocin. | B | 5 | pKi | >10000 | nM | Ki | US-11642336-B2. 5-HT2A agonists for use in treatment of depression (2023) |
| D2 receptor/D(2) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Radioligand Binding Assay: The binding affinities shown in table 5 of psilocin and compound 8 at various monoaminergic receptors were determined in radioligand competition binding assays by Psychiatric Drug Screening Program according to the experimental described in Assay Protocol Book, Version III 11, 16. As shown compound 8 shows less affinity for various monoaminergic receptors compared to Psilocin. | B | 5 | pKi | >10000 | nM | Ki | US-11642336-B2. 5-HT2A agonists for use in treatment of depression (2023) |
| D3 receptor/D(3) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | Radioligand Binding Assay: The binding affinities shown in table 5 of psilocin and compound 8 at various monoaminergic receptors were determined in radioligand competition binding assays by Psychiatric Drug Screening Program according to the experimental described in Assay Protocol Book, Version III 11, 16. As shown compound 8 shows less affinity for various monoaminergic receptors compared to Psilocin. | B | 7 | pKi | 100 | nM | Ki | US-11642336-B2. 5-HT2A agonists for use in treatment of depression (2023) |
| D4 receptor/D(4) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
| ChEMBL | Radioligand Binding Assay: The binding affinities shown in table 5 of psilocin and compound 8 at various monoaminergic receptors were determined in radioligand competition binding assays by Psychiatric Drug Screening Program according to the experimental described in Assay Protocol Book, Version III 11, 16. As shown compound 8 shows less affinity for various monoaminergic receptors compared to Psilocin. | B | 5 | pKi | >10000 | nM | Ki | US-11642336-B2. 5-HT2A agonists for use in treatment of depression (2023) |
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]
