paliperidone [Ligand Id: 7258] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1621 (Paliperidone, RO76477, RO-76477, Risperidone impurity, 9-hydroxyrisperidone-, R-76477, Invega, Trevicta, Xeplion)
  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • Nav1.5/Sodium channel protein type V alpha subunit in Human [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
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  • Kv4.3/Voltage-gated potassium channel subunit Kv4.3 in Human [ChEMBL: CHEMBL1964] [GtoPdb: 554] [UniProtKB: Q9UK17]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Antagonist activity at dopamine D2 receptor (unknown origin) after 60 mins by Ultra lance cAMP assay B 8.08 pIC50 8.28 nM IC50 Bioorg Med Chem (2017) 25: 4904-4916 [PMID:28774576]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG channel B 5.89 pIC50 1300 nM IC50 J. Med. Chem. (2009) 52: 4266-4276 [PMID:19534531]
ChEMBL Inhibition of human ERG channel B 5.89 pIC50 1300 nM IC50 J. Med. Chem. (2009) 52: 4266-4276 [PMID:19534531]
ChEMBL Inhibition of human ERG B 5.89 pIC50 1288.25 nM IC50 Eur. J. Med. Chem. (2011) 46: 618-630 [PMID:21185626]
ChEMBL Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) cells stable expressing hERG measured using IonWorks Barracuda automated patch clamp platform F 5.9 pIC50 1258.93 nM IC50 J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]
ChEMBL Inhibition of rapid delayed inward rectifying potassium current (IKr) measured using manual patch clamp assay F 5.9 pIC50 1258.93 nM IC50 J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]
ChEMBL Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) K1 cells stably expressing hERG measured using IonWorks Quattro automated patch clamp platform F 6 pIC50 1000 nM IC50 J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay B 5 pEC50 >10000 nM EC50 Bioorg Med Chem (2017) 25: 4904-4916 [PMID:28774576]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Antagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay B 8.28 pIC50 5.2 nM IC50 Bioorg Med Chem (2017) 25: 4904-4916 [PMID:28774576]
Nav1.5/Sodium channel protein type V alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
ChEMBL Inhibition of fast sodium current (INa) in Chinese Hamster Ovary (CHO) K1 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platform F 4.6 pIC50 25118.86 nM IC50 J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]
Kv4.3/Voltage-gated potassium channel subunit Kv4.3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1964] [GtoPdb: 554] [UniProtKB: Q9UK17]
ChEMBL Inhibition of transient outward potassium current (Ito) current in Chinese Hamster Ovary (CHO) K1 cells expressing human Kv4.3 measured using IonWorks Quattro automated patch clamp platform F 4.2 pIC50 63095.73 nM IC50 J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]