nebivolol [Ligand Id: 7246] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL434394 (Hypoloc, Narbivolol, Nebilet, Nebivolol, R-65824, R65,824) |
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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: P15382, P51787] | ||||||||
| 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 | - | 9.1 | pKi | - | - | - | Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599] |
| 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 | - | 8 | pKi | - | - | - |
Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599]; Eur J Pharmacol (2011) 654: 86-91 [PMID:21172342] |
| β3-adrenoceptor in Human [GtoPdb: 30] [UniProtKB: P13945] | ||||||||
| GtoPdb | Radioligand binding | - | 7 | pKi | - | - | - |
Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599]; Eur J Pharmacol (2011) 654: 86-91 [PMID:21172342] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
