RS-102221 [Ligand Id: 187] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL88402 (RS-102221) |
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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] | ||||||||
| GtoPdb | - | - | 6 | pKi | - | - | - |
Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]; Neuropharmacology (1997) 36: 621-9 [PMID:9225287] |
| ChEMBL | Displacement of [3H]-ketanserin from human cloned 5-hydroxytryptamine 2A receptor expressed in CHO-K1 cells. | B | 6.2 | pKi | 630.96 | nM | Ki | Bioorg Med Chem Lett (1996) 6: 2687-2692 |
| 5-HT2A receptor in Rat [GtoPdb: 6] [UniProtKB: P14842] | ||||||||
| GtoPdb | - | - | 6.8 | pKi | - | - | - | Neuropharmacology (1997) 36: 621-9 [PMID:9225287] |
| 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| GtoPdb | - | - | 6.1 | pKi | - | - | - |
Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]; Neuropharmacology (1997) 36: 621-9 [PMID:9225287] |
| ChEMBL | Displacement of [3H]-5-5HT from human cloned 5-hydroxytryptamine 2B receptor expressed in CHO-K1 cells | B | 6.5 | pKi | 316.23 | nM | Ki | Bioorg Med Chem Lett (1996) 6: 2687-2692 |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| GtoPdb | - | - | 8.4 | pKi | 3.98 | nM | Ki |
Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]; Neuropharmacology (1997) 36: 621-9 [PMID:9225287] |
| ChEMBL | Displacement of radiolabeled RS 102221 from human 5HT2C receptor | B | 8.41 | pKi | 3.9 | nM | Ki | J Med Chem (2008) 51: 7094-7098 [PMID:18983139] |
| ChEMBL | Displacement of [3H]mesulergine from human cloned 5-hydroxytryptamine 2C receptor expressed in CHO-K1 cells | B | 8.7 | pKi | 2 | nM | Ki | Bioorg Med Chem Lett (1996) 6: 2687-2692 |
| ChEMBL | Binding affinity to human 5-HT2C receptor by radioligand displacement assay | B | 9.04 | pKi | 0.91 | nM | Ki | Eur J Med Chem (2013) 63: 85-94 [PMID:23466604] |
| ChEMBL | Displacement of [3H]mesulergine from human recombinant 5-HT2C receptor expressed in HEK293 cells | B | 9.22 | pKi | 0.6 | nM | Ki | J Med Chem (2014) 57: 4543-4557 [PMID:24805037] |
| ChEMBL | Displacement of [3H]mesulergine from human 5-HT2C receptor expressed in HEK-293 cells | B | 9.22 | pKi | 0.6 | nM | Ki | Eur J Med Chem (2015) 92: 221-235 [PMID:25557493] |
| ChEMBL | Displacement of radiolabeled RS 102221 from human 5HT2C receptor | B | 8.08 | pIC50 | 8.3 | nM | IC50 | J Med Chem (2008) 51: 7094-7098 [PMID:18983139] |
| ChEMBL | Binding affinity to human 5-HT2C receptor by radioligand displacement assay | B | 8.26 | pIC50 | 5.5 | nM | IC50 | Bioorg Med Chem (2013) 21: 2764-2771 [PMID:23582449] |
| ChEMBL | Binding affinity to human 5-HT2C receptor by radioligand displacement assay | B | 8.57 | pIC50 | 2.7 | nM | IC50 | Eur J Med Chem (2013) 63: 85-94 [PMID:23466604] |
| ChEMBL | Displacement of [3H]mesuleregine from human recombinant 5-HT2C receptor expressed in HEK293 cells | B | 8.82 | pIC50 | 1.5 | nM | IC50 | Bioorg Med Chem (2016) 24: 1793-1810 [PMID:26988801] |
| ChEMBL | Displacement of [3H]mesulergine from human recombinant 5HT2C receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method | B | 8.82 | pIC50 | 1.5 | nM | IC50 | Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250] |
| 5-HT2C receptor in Rat [GtoPdb: 8] [UniProtKB: P08909] | ||||||||
| GtoPdb | - | - | 8.4 | pKi | - | - | - | Neuropharmacology (1997) 36: 621-9 [PMID:9225287] |
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]
