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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]