palonosetron [Ligand Id: 7486] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1189679 (Aurothioglucose, NSC-743769, (-)-palonosetron, Palonosetron, Palonosetron, (3as, 3s)-)
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  • 5-HT3A/Serotonin 3a (5-HT3a) receptor in Human [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
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  • 5-HT3B/Serotonin 3b (5-HT3b) receptor in Human [ChEMBL: CHEMBL3895] [GtoPdb: 374] [UniProtKB: O95264]
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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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  • Kv7.1/Voltage-gated potassium channel, IKs; KCNQ1(Kv7.1)/KCNE1(MinK) in Human [ChEMBL: CHEMBL2221347] [GtoPdb: 560] [UniProtKB: P15382P51787]
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  • 5-HT3A in Human [GtoPdb: 379]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
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 5.4 pIC50 3981.07 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 5.7 pIC50 1995.26 nM IC50 J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]
5-HT3B/5-HT3A/Serotonin 3 (5-HT3) receptor in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111332] [GtoPdb: 374373] [UniProtKB: O95264P46098]
ChEMBL Binding affinity to human wild type 5-HT3A/5-HT3B receptor expressed in HEK293 cells after 24 hrs by liquid scintillation counting analysis B 9.74 pKd 0.18 nM Kd Bioorg. Med. Chem. (2013) 21: 7523-7528 [PMID:24128813]
ChEMBL Antagonist activity at human wild type 5-HT3A/5-HT3B receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced response after 45 mins by FLIPR assay B 9.06 pIC50 0.88 nM IC50 Bioorg. Med. Chem. (2013) 21: 7523-7528 [PMID:24128813]
5-HT3A/Serotonin 3a (5-HT3a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
ChEMBL Binding affinity to human 5-HT3A receptor Y73A mutant after 24 hrs by liquid scintillation counting analysis B 9.06 pKd 0.87 nM Kd Bioorg. Med. Chem. (2013) 21: 7523-7528 [PMID:24128813]
ChEMBL Binding affinity to human 5-HT3A receptor F130A mutant after 24 hrs by liquid scintillation counting analysis B 9.17 pKd 0.67 nM Kd Bioorg. Med. Chem. (2013) 21: 7523-7528 [PMID:24128813]
ChEMBL Binding affinity to human 5-HT3A receptor Y73S mutant after 24 hrs by liquid scintillation counting analysis B 9.21 pKd 0.61 nM Kd Bioorg. Med. Chem. (2013) 21: 7523-7528 [PMID:24128813]
ChEMBL Binding affinity to human 5-HT3A receptor D165K mutant after 24 hrs by liquid scintillation counting analysis B 9.44 pKd 0.36 nM Kd Bioorg. Med. Chem. (2013) 21: 7523-7528 [PMID:24128813]
ChEMBL Binding affinity to human wild type 5-HT3A receptor expressed in HEK293 cells after 24 hrs by liquid scintillation counting analysis B 9.49 pKd 0.32 nM Kd Bioorg. Med. Chem. (2013) 21: 7523-7528 [PMID:24128813]
ChEMBL Binding affinity to human 5-HT3A receptor S163A mutant after 24 hrs by liquid scintillation counting analysis B 9.52 pKd 0.3 nM Kd Bioorg. Med. Chem. (2013) 21: 7523-7528 [PMID:24128813]
ChEMBL Binding affinity to human 5-HT3A receptor D165A mutant after 24 hrs by liquid scintillation counting analysis B 9.52 pKd 0.3 nM Kd Bioorg. Med. Chem. (2013) 21: 7523-7528 [PMID:24128813]
ChEMBL Binding affinity to human 5-HT3A receptor F130Y mutant after 24 hrs by liquid scintillation counting analysis B 9.59 pKd 0.26 nM Kd Bioorg. Med. Chem. (2013) 21: 7523-7528 [PMID:24128813]
ChEMBL Binding affinity to human 5-HT3A receptor Y73F mutant after 24 hrs by liquid scintillation counting analysis B 9.6 pKd 0.25 nM Kd Bioorg. Med. Chem. (2013) 21: 7523-7528 [PMID:24128813]
ChEMBL Binding affinity to human 5-HT3A receptor S163T mutant after 24 hrs by liquid scintillation counting analysis B 9.66 pKd 0.22 nM Kd Bioorg. Med. Chem. (2013) 21: 7523-7528 [PMID:24128813]
ChEMBL Binding affinity to 5HT3A receptor B 10.5 pKi 0.03 nM Ki Eur. J. Med. Chem. (2010) 45: 4746-4760 [PMID:20724042]
ChEMBL Antagonist activity at human 5-HT3A receptor Y73A mutant assessed as inhibition of 5-HT-induced response after 45 mins by FLIPR assay B 7.88 pIC50 13.1 nM IC50 Bioorg. Med. Chem. (2013) 21: 7523-7528 [PMID:24128813]
ChEMBL Antagonist activity at human 5-HT3A receptor F130A mutant assessed as inhibition of 5-HT-induced response after 45 mins by FLIPR assay B 8.36 pIC50 4.4 nM IC50 Bioorg. Med. Chem. (2013) 21: 7523-7528 [PMID:24128813]
ChEMBL Antagonist activity at human 5-HT3A receptor Y73S mutant assessed as inhibition of 5-HT-induced response after 45 mins by FLIPR assay B 8.44 pIC50 3.64 nM IC50 Bioorg. Med. Chem. (2013) 21: 7523-7528 [PMID:24128813]
ChEMBL Antagonist activity at human 5-HT3A receptor S163A mutant assessed as inhibition of 5-HT-induced response after 45 mins by FLIPR assay B 8.8 pIC50 1.57 nM IC50 Bioorg. Med. Chem. (2013) 21: 7523-7528 [PMID:24128813]
ChEMBL Antagonist activity at human 5-HT3A receptor D165K mutant assessed as inhibition of 5-HT-induced response after 45 mins by FLIPR assay B 8.89 pIC50 1.3 nM IC50 Bioorg. Med. Chem. (2013) 21: 7523-7528 [PMID:24128813]
ChEMBL Antagonist activity at human 5-HT3A receptor Y73F mutant assessed as inhibition of 5-HT-induced response after 45 mins by FLIPR assay B 8.91 pIC50 1.23 nM IC50 Bioorg. Med. Chem. (2013) 21: 7523-7528 [PMID:24128813]
ChEMBL Antagonist activity at human 5-HT3A receptor S163T mutant assessed as inhibition of 5-HT-induced response after 45 mins by FLIPR assay B 8.99 pIC50 1.02 nM IC50 Bioorg. Med. Chem. (2013) 21: 7523-7528 [PMID:24128813]
ChEMBL Antagonist activity at human wild type 5-HT3A receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced response after 45 mins by FLIPR assay B 9.08 pIC50 0.83 nM IC50 Bioorg. Med. Chem. (2013) 21: 7523-7528 [PMID:24128813]
5-HT3B/Serotonin 3b (5-HT3b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3895] [GtoPdb: 374] [UniProtKB: O95264]
ChEMBL Binding affinity to human 5-HT3B receptor F130A mutant after 24 hrs by liquid scintillation counting analysis B 9.32 pKd 0.48 nM Kd Bioorg. Med. Chem. (2013) 21: 7523-7528 [PMID:24128813]
ChEMBL Binding affinity to human 5-HT3B receptor W90C mutant after 24 hrs by liquid scintillation counting analysis B 9.47 pKd 0.34 nM Kd Bioorg. Med. Chem. (2013) 21: 7523-7528 [PMID:24128813]
ChEMBL Binding affinity to human 5-HT3B receptor I183A mutant after 24 hrs by liquid scintillation counting analysis B 9.64 pKd 0.23 nM Kd Bioorg. Med. Chem. (2013) 21: 7523-7528 [PMID:24128813]
ChEMBL Binding affinity to human 5-HT3B receptor Y143A mutant after 24 hrs by liquid scintillation counting analysis B 9.74 pKd 0.18 nM Kd Bioorg. Med. Chem. (2013) 21: 7523-7528 [PMID:24128813]
ChEMBL Binding affinity to human 5-HT3B receptor H73A mutant after 24 hrs by liquid scintillation counting analysis B 9.85 pKd 0.14 nM Kd Bioorg. Med. Chem. (2013) 21: 7523-7528 [PMID:24128813]
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 4.7 pIC50 19952.62 nM IC50 J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]
Kv7.1/Voltage-gated potassium channel, IKs; KCNQ1(Kv7.1)/KCNE1(MinK) in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2221347] [GtoPdb: 560] [UniProtKB: P15382P51787]
ChEMBL Inhibition of slow delayed inward rectifying potassium current (Iks) in Chinese Hamster Ovary (CHO) cells expressing hKvLQT1/hminK measured using IonWorks Quattro automated patch clamp platform F 4.3 pIC50 50118.72 nM IC50 J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]
5-HT3A in Human [GtoPdb: 379]
GtoPdb - - 10.49 pKi 0.03 nM Ki Eur J Med Chem (2010) 45: 4746-60 [PMID:20724042]

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]