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

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ChEMBL ligand: CHEMBL2058833 (Ganaplacida, Ganaplacide, GNF 156, GNF-156, Kaf156, KAF 156, KAF-156, KAF156)
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  • Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 Antiplasmodial activity against multidrug-resistant Plasmodium falciparum Dd2 harboring CARL-I1139K mutant infected in erythrocytes assessed as inhibition of parasite growth incubated for 72 hrs by [3H]hypoxanthine incorporation based microbeta counting analysis F 5.72 pEC50 1920 nM EC50 Eur J Med Chem (2024) 276: 116677-116677 [PMID:39024967]
ChEMBL Antimalarial activity against KAF-156 resistant Plasmodium falciparum Dd2 harboring CARL I1139K mutant assessed as reduction in parasite growth incubated for 72 hrs by [3H]-hypoxanthine incorporation assay F 5.82 pEC50 1530 nM EC50 Eur J Med Chem (2024) 270: 116354-116354 [PMID:38554474]
ChEMBL Antiplasmodial activity against Plasmodium falciparum Dd2 infected in erythrocytes assessed as inhibition of parasite growth incubated for 72 hrs by [3H]hypoxanthine incorporation based microbeta counting analysis F 7.77 pEC50 17 nM EC50 Eur J Med Chem (2024) 276: 116677-116677 [PMID:39024967]
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 F 8 pEC50 10 nM EC50 Eur J Med Chem (2021) 210: 112955-112955 [PMID:33131885]
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 Dd2 assessed as reduction in parasite growth incubated for 72 hrs by [3H]-hypoxanthine incorporation assay F 8.1 pEC50 8 nM EC50 Eur J Med Chem (2024) 270: 116354-116354 [PMID:38554474]
ChEMBL Antimalarial activity against Plasmodium falciparum W2 F 8.22 pEC50 6 nM EC50 Eur J Med Chem (2021) 210: 112955-112955 [PMID:33131885]
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]
Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 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]

ChEMBL data shown on this page come from version 36:

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]