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 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]
