SB 242084 [Ligand Id: 193] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL14563 (SB-242084) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| CYP19A1/Cytochrome P450 19A1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1978] [GtoPdb: 1362] [UniProtKB: P11511] | ||||||||
| ChEMBL | Inhibition of heterologously expressed human Cytochrome P450 19A1 at 100 uM | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1997) 40: 3494-3496 [PMID:9357513] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Displacement of [3H]ketanserin from 5-hydroxytryptamine 2A receptor expressed in HEK 293 cells | B | 6.8 | pKi | 158.49 | nM | Ki | J Med Chem (1997) 40: 3494-3496 [PMID:9357513] |
| ChEMBL | Binding affinity towards human cloned 5-hydroxytryptamine receptor 2A in HEK293 cells, using [3H]ketanserin as radioligand. | B | 6.8 | pKi | 158.49 | nM | Ki | J Med Chem (2000) 43: 1123-1134 [PMID:10737744] |
| ChEMBL | Binding affinity towards human cloned 5-hydroxytryptamine 2A receptor of HEK293 cells by displacement of [3H]ketanserin | B | 6.8 | pKi | 158.49 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1863-1866 [PMID:10969986] |
| ChEMBL | Binding affinity for human 5-hydroxytryptamine 2A receptor expressed in HEK 293 cells using [3H]ketanserin | B | 6.8 | pKi | 158.49 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4989-4993 [PMID:16168649] |
| GtoPdb | - | - | 6.8 | pKi | - | - | - |
Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]; Neuropharmacology (1997) 36: 609-20 [PMID:9225286] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842] | ||||||||
| ChEMBL | Displacement of [3H]ketanserin from 5HT2A in Wistar rat frontal cortex membranes after 1 hr by liquid scintillation spectrometry | B | 6.56 | pKi | 274 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 914-920 [PMID:26748694] |
| 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| GtoPdb | - | - | 7 | pKi | - | - | - |
Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]; Neuropharmacology (1997) 36: 609-20 [PMID:9225286] |
| ChEMBL | Displacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells | B | 7 | pKi | 100 | nM | Ki | J Med Chem (1997) 40: 3494-3496 [PMID:9357513] |
| ChEMBL | Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand. | B | 7 | pKi | 100 | nM | Ki | J Med Chem (2000) 43: 1123-1134 [PMID:10737744] |
| ChEMBL | Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT | B | 7 | pKi | 100 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1863-1866 [PMID:10969986] |
| ChEMBL | Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT | B | 7 | pKi | 100 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4989-4993 [PMID:16168649] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| GtoPdb | - | - | 9 | pKi | 1 | nM | Ki |
Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]; Neuropharmacology (1997) 36: 609-20 [PMID:9225286] |
| ChEMBL | Displacement of [3H]mesulergine from 5-hydroxytryptamine 2C receptor expressed in HEK 293 cells | B | 9 | pKi | 1 | nM | Ki | J Med Chem (1997) 40: 3494-3496 [PMID:9357513] |
| ChEMBL | Binding affinity towards human cloned 5-hydroxytryptamine receptor 2C in HEK293 cells, using [3H]mesulergine as radioligand. | B | 9 | pKi | 1 | nM | Ki | J Med Chem (2000) 43: 1123-1134 [PMID:10737744] |
| ChEMBL | Binding affinity towards human cloned 5-hydroxytryptamine 2C receptor of HEK293 cells by displacement of [3H]mesulergine | B | 9 | pKi | 1 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1863-1866 [PMID:10969986] |
| ChEMBL | Binding affinity for human 5-hydroxytryptamine 2C receptor expressed in HEK 293 cells using [3H]mesulergine | B | 9 | pKi | 1 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4989-4993 [PMID:16168649] |
| ChEMBL | Antagonist activity at recombinant human 5-HT2C expressed in human U2OS cells by pathhunter beta-arrestin assay | B | 9.48 | pIC50 | 0.33 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127358-127358 [PMID:32631554] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909] | ||||||||
| ChEMBL | Displacement of [3H]mesulergine from 5HT2C in Sprague-Dawley rat whole brain membranes after 1 hr by liquid scintillation spectrometry | B | 9.8 | pKi | 0.16 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 914-920 [PMID:26748694] |
| SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] | ||||||||
| ChEMBL | Displacement of [3H]citalopram from SERT in Sprague-Dawley rat whole brain membranes after 1 hr by liquid scintillation spectrometry | B | 5.75 | pKi | 1772 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 914-920 [PMID:26748694] |
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]
