(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 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]
