SB 242084 [Ligand Id: 193] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL14563 (SB-242084)
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
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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 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]