norfluoxetine [Ligand Id: 208] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1494 (Norfluoxetine)
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  • K2P2.1/Potassium channel subfamily K member 2 in Human [ChEMBL: CHEMBL2321615] [GtoPdb: 514] [UniProtKB: O95069]
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  • Kv3.1/Potassium voltage-gated channel subfamily C member 1 in Rat [ChEMBL: CHEMBL2321617] [GtoPdb: 548] [UniProtKB: P25122]
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  • Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936]
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  • 5-HT2A receptor in Rat [GtoPdb: 6] [UniProtKB: P14842]
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  • 5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
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  • 5-HT2C receptor in Rat [GtoPdb: 8] [UniProtKB: P08909]
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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 human ERG B 5.64 pIC50 2290.87 nM IC50 Eur J Med Chem (2011) 46: 618-630 [PMID:21185626]
K2P2.1/Potassium channel subfamily K member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2321615] [GtoPdb: 514] [UniProtKB: O95069]
ChEMBL Inhibition of of human TREK1 expressed in tsA201 cells assessed as reduction in channel currents B 5.05 pIC50 9000 nM IC50 J Med Chem (2016) 59: 5149-5157 [PMID:26588045]
GtoPdb - - 5.05 pIC50 9000 nM IC50 Br J Pharmacol (2005) 144: 821-9 [PMID:15685212]
Kv3.1/Potassium voltage-gated channel subfamily C member 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2321617] [GtoPdb: 548] [UniProtKB: P25122]
GtoPdb - - 4.9 pIC50 - - - Neuropharmacology (2001) 41: 443-53 [PMID:11543764]
ChEMBL Inhibition of rat voltage-gated K channel 3.1 expressed in CHO cells by patch clamp assay B 6.1 pIC50 800 nM IC50 J Med Chem (2013) 56: 593-624 [PMID:23121096]
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 Cav1.2 calcium current measured using whole cell patch clamp in dog ventricular myocytes F 5.95 pIC50 1130 nM IC50 IC50 data for the L-type calcium channel extracted from a set of literature articles
5-HT2A receptor in Rat [GtoPdb: 6] [UniProtKB: P14842]
GtoPdb - - 6.2 pKi - - - Circulation (2000) 102: 2836-41 [PMID:11104741]
5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
GtoPdb - - 5.3 pKi - - - Circulation (2000) 102: 2836-41 [PMID:11104741]
5-HT2C receptor in Rat [GtoPdb: 8] [UniProtKB: P08909]
GtoPdb - - 6.5 pKi - - - Circulation (2000) 102: 2836-41 [PMID:11104741]

ChEMBL data shown on this page come from version 32:

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]