ganaplacide [Ligand Id: 9946] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2058833 (Ganaplacide, GNF 156, GNF-156, Kaf156, KAF156, KAF 156, KAF-156)
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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 channel expressed in CHO cells by patch clamp assay B 4.87 pIC50 13400 nM IC50 J Med Chem (2012) 55: 4244-4273 [PMID:22524250]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against multidrug-sensitive Plasmodium falciparum NF54 transfected with GFP-Luc infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation pretreated for 48 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by liquid scintillation counting method F 7.8 pIC50 16 nM IC50 J Med Chem (2021) 64: 2291-2309 [PMID:33573376]
ChEMBL Antimalarial activity against Plasmodium falciparum assessed as reduction in parasite growth after 72 hrs by SYBR-green based fluorescence assay F 7.9 pEC50 12.6 nM EC50 J Med Chem (2019) 62: 10526-10562 [PMID:31385706]
ChEMBL Antimalarial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green fluorescence assay F 8 pEC50 10 nM EC50 J Med Chem (2012) 55: 4244-4273 [PMID:22524250]
ChEMBL Antimalarial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green fluorescence assay F 8.22 pEC50 6 nM EC50 J Med Chem (2012) 55: 4244-4273 [PMID:22524250]
Plasmodium vivax (target type: ORGANISM) [ChEMBL: CHEMBL613013]
ChEMBL Antimalarial activity against Plasmodium vivax assessed as reduction in parasite growth after 72 hrs by SYBR-green based fluorescence assay F 8.26 pEC50 5.5 nM EC50 J Med Chem (2019) 62: 10526-10562 [PMID:31385706]

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]