(R)-DOI [Ligand Id: 157] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL134519 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Inhibitory constant against cloned human 5-hydroxytryptamine 2A receptor using with [125I]- DOI radioligand | B | 9.19 | pKi | 0.65 | nM | Ki | J Med Chem (2003) 46: 4188-4195 [PMID:12954071] |
| ChEMBL | In vitro inhibitory concentration required against [3H]8-OH-DPAT binding to cloned human 5-hydroxytryptamine 1A receptor | B | 5.42 | pIC50 | 3843 | nM | IC50 | J Med Chem (2003) 46: 4188-4195 [PMID:12954071] |
| ChEMBL | Tested for functional response on CHO cells expressing cloned human 5-hydroxytryptamine 1A receptor | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2003) 46: 4188-4195 [PMID:12954071] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Displacement of [3H]LSD from human recombinant 5-HT2A receptor expressed in HEK cells by radioligand completion assay relative to control | B | 8.17 | pKi | 6.8 | nM | Ki | J Med Chem (2021) 64: 13510-13523 [PMID:34467758] |
| ChEMBL | Displacement of [125I]DOI from cloned human 5HT2A receptor expressed in CHO cells | B | 9.19 | pKi | 0.65 | nM | Ki | J Med Chem (2006) 49: 318-328 [PMID:16392816] |
| GtoPdb | - | - | 9.2 | pKi | - | - | - | J Med Chem (2003) 46: 4188-95 [PMID:12954071] |
| GtoPdb | - | - | 9.3 | pKi | - | - | - |
Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]; J Med Chem (1998) 41: 5148-9 [PMID:9857084] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842] | ||||||||
| ChEMBL | In vitro inhibitory constant against [125I]DOI binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex | B | 10 | pKi | 0.1 | nM | Ki | J Med Chem (2003) 46: 4188-4195 [PMID:12954071] |
| ChEMBL | Displacement of [125I]DOI from 5HT2A receptor in rat cerebral cortex | B | 9.34 | pIC50 | 0.46 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 2998-3002 [PMID:17419053] |
| ChEMBL | In vitro inhibition of [125I]DOI binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex | B | 9.4 | pIC50 | 0.4 | nM | IC50 | J Med Chem (2003) 46: 4188-4195 [PMID:12954071] |
| ChEMBL | Inhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortex | B | 9.68 | pIC50 | 0.21 | nM | IC50 | J Med Chem (2006) 49: 318-328 [PMID:16392816] |
| ChEMBL | In vitro relative agonist activity against 5-hydroxytryptamine 2A using PI assay in rat vascular smooth muscle cells | F | 7.56 | pEC50 | 27.7 | nM | EC50 | J Med Chem (2003) 46: 4188-4195 [PMID:12954071] |
| ChEMBL | Activity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cells | F | 7.7 | pEC50 | 19.8 | nM | EC50 | J Med Chem (2006) 49: 318-328 [PMID:16392816] |
| ChEMBL | Agonist activity at 5HT2A receptor in rat A7r5 cells assessed as intracellular calcium mobilization relative to 5HT | F | 7.75 | pEC50 | 17.8 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 2998-3002 [PMID:17419053] |
| 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| GtoPdb | - | - | 7.4 | pKi | - | - | - |
Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]; J Med Chem (1998) 41: 5148-9 [PMID:9857084] |
| GtoPdb | - | - | 7.7 | pKi | - | - | - | J Med Chem (2003) 46: 4188-95 [PMID:12954071] |
| ChEMBL | Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand | B | 7.74 | pKi | 18 | nM | Ki | J Med Chem (2003) 46: 4188-4195 [PMID:12954071] |
| ChEMBL | Displacement of [125I]DOI from cloned human 5HT2B receptor expressed in CHO cells | B | 7.74 | pKi | 18 | nM | Ki | J Med Chem (2006) 49: 318-328 [PMID:16392816] |
| ChEMBL | Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in CHO cells by radioligand completion assay relative to control | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (2021) 64: 13510-13523 [PMID:34467758] |
| 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL323] [GtoPdb: 7] [UniProtKB: P30994] | ||||||||
| ChEMBL | Activity against 5HT2B receptor in longitudinal stomach fundus strips in wistar rats | F | 7.92 | pEC50 | 11.9 | nM | EC50 | J Med Chem (2006) 49: 318-328 [PMID:16392816] |
| ChEMBL | Agonist activity at 5HT2B receptor in rat stomach fundus assessed as intracellular calcium mobilization relative to 5HT | F | 7.92 | pEC50 | 11.9 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 2998-3002 [PMID:17419053] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Inhibitory constant against cloned human 5-hydroxytryptamine 2C receptor using with [125I]- DOI radioligand | B | 8.4 | pKi | 4 | nM | Ki | J Med Chem (2003) 46: 4188-4195 [PMID:12954071] |
| ChEMBL | Displacement of [125I]DOI from cloned human 5HT2C receptor expressed in CHO cells | B | 8.4 | pKi | 4 | nM | Ki | J Med Chem (2006) 49: 318-328 [PMID:16392816] |
| GtoPdb | - | - | 8.4 | pKi | - | - | - | J Med Chem (2003) 46: 4188-95 [PMID:12954071] |
| GtoPdb | - | - | 8.7 | pKi | - | - | - |
Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]; Naunyn Schmiedebergs Arch Pharmacol (1999) 359: 1-6 [PMID:9933142]; J Neurochem (1999) 72: 2127-34 [PMID:10217294] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909] | ||||||||
| ChEMBL | Activity against recombinant rat 5HT2C mediated intracellular calcium mobilization by FLIPR in SR3T3 cells | F | 7.52 | pEC50 | 30.2 | nM | EC50 | J Med Chem (2006) 49: 318-328 [PMID:16392816] |
| ChEMBL | Agonist activity at 5HT2C receptor expressed in rat SR3T3 cells assessed as intracellular calcium mobilization relative to 5HT | F | 7.52 | pEC50 | 30.2 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 2998-3002 [PMID:17419053] |
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]
