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 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]
