nebivolol [Ligand Id: 7246] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL434394 (Nebivolol, R-65824, R65,824, Hypoloc, Nebilet)
  • Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
  • This target only has 0 pki data point
  • 0
1 CHEMBL434394_lig_chart_1 HERG Human
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  • Nav1.5/Sodium channel protein type V alpha subunit in Human [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
  • This target only has 0 pki data point
  • 0
2 CHEMBL434394_lig_chart_2 Sodium channel protein type V alpha subunit Human
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  • Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936]
  • This target only has 0 pki data point
  • 0
3 CHEMBL434394_lig_chart_3 Voltage-gated L-type calcium channel alpha-1C subunit Human
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  • Kv7.1/Voltage-gated potassium channel, IKs; KCNQ1(Kv7.1)/KCNE1(MinK) in Human [ChEMBL: CHEMBL2221347] [GtoPdb: 560] [UniProtKB: P15382P51787]
  • This target only has 0 pki data point
  • 0
4 CHEMBL434394_lig_chart_4 Voltage-gated potassium channel, IKs; KCNQ1(Kv7.1)/KCNE1(MinK) Human
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  • Kv4.3/Voltage-gated potassium channel subunit Kv4.3 in Human [ChEMBL: CHEMBL1964] [GtoPdb: 554] [UniProtKB: Q9UK17]
  • This target only has 0 pki data point
  • 0
5 CHEMBL434394_lig_chart_5 Voltage-gated potassium channel subunit Kv4.3 Human
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  • β1-adrenoceptor in Human [GtoPdb: 28] [UniProtKB: P08588]
  • β1-adrenoceptor in Rabbit [GtoPdb: 28]
  • This target only has 1 pki data point
  • 0
6 CHEMBL434394_lig_chart_6 β1-adrenoceptor HumanRabbit
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  • β2-adrenoceptor in Human [GtoPdb: 29] [UniProtKB: P07550]
  • This target only has 1 pki data point
  • 7.96
7 CHEMBL434394_lig_chart_7 β2-adrenoceptor Human
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  • β3-adrenoceptor in Human [GtoPdb: 30] [UniProtKB: P13945]
  • This target only has 1 pki data point
  • 5.66
8 CHEMBL434394_lig_chart_8 β3-adrenoceptor Human
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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 5.2 pIC50 6309.57 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) cells stable expressing hERG measured using IonWorks Barracuda automated patch clamp platform F 5.2 pIC50 6309.57 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 6.5 pIC50 316.23 nM IC50 J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]
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 HEK293 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platform F 5.1 pIC50 7943.28 nM IC50 J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]
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 5.2 pIC50 6309.57 nM IC50 J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]
Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936]
ChEMBL Inhibition of long-lasting type calcium current (ICaL) in HEK293 cells (alpha1C/beta2a/alpha2delta1) cells measured using IonWorks Barracuda automated patch clamp platform F 4.8 pIC50 15848.93 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 transfected with KCNQ1 / Kv1.7 / KvLQT1 and KCNE1/minK measured using IonWorks automated patch clamp platform F 4.4 pIC50 39810.72 nM IC50 J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]
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 4.8 pIC50 15848.93 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 4.3 pIC50 50118.72 nM IC50 J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]
β1-adrenoceptor in Human [GtoPdb: 28] [UniProtKB: P08588]
GtoPdb Radioligand binding - 9.17 pKi - - - Eur J Pharmacol (2011) 654: 86-91 [PMID:21172342]
β1-adrenoceptor in Rabbit [GtoPdb: 28]
GtoPdb - - 8.7 pIC50 - - - Mol Pharmacol (1988) 34: 843-51 [PMID:2462161]
β2-adrenoceptor in Human [GtoPdb: 29] [UniProtKB: P07550]
GtoPdb Radioligand binding - 7.96 pKi - - - Eur J Pharmacol (2011) 654: 86-91 [PMID:21172342]
β3-adrenoceptor in Human [GtoPdb: 30] [UniProtKB: P13945]
GtoPdb Radioligand binding - 5.66 pKi - - - Eur J Pharmacol (2011) 654: 86-91 [PMID:21172342]

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]