tafenoquine [Ligand Id: 9722] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL298470 (SB-252263-AAB, Tafenoquine, WR 238605)
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Plasmodium cynomolgi (target type: ORGANISM) [ChEMBL: CHEMBL613883]
ChEMBL Antiplasmodial activity against liver stage Plasmodium cynomolgi B infected in non-human primate hepatocytes assessed as reduction in liver schizonts development incubated for 4 days starting on day 4 post-sporozoite inoculation by radial cure mode analysis F 5.44 pIC50 3610 nM IC50 ACS Med Chem Lett (2021) 12: 1962-1967 [PMID:34917261]
ChEMBL Antiplasmodial activity against liver stage Plasmodium cynomolgi B infected in non-human primate hepatocytes assessed as reduction in liver hypnozoites development incubated for 4 days starting on day 4 post-sporozoite inoculation by radial cure mode analysis F 5.46 pIC50 3500 nM IC50 ACS Med Chem Lett (2021) 12: 1962-1967 [PMID:34917261]
ChEMBL Antiplasmodial activity against liver stage Plasmodium cynomolgi B infected in non-human primate hepatocytes assessed as inhibition of liver schizonts development incubated for 4 days from sporozoite addition by prophylactic assay F 6.72 pIC50 190 nM IC50 ACS Med Chem Lett (2021) 12: 1962-1967 [PMID:34917261]
ChEMBL Antiplasmodial activity against liver stage Plasmodium cynomolgi B infected in non-human primate hepatocytes assessed as inhibition of hypnozoite development incubated for 4 days from sporozoite addition by prophylactic assay F 6.85 pIC50 140 nM IC50 ACS Med Chem Lett (2021) 12: 1962-1967 [PMID:34917261]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antimalarial activity against late (4 to 5) gametocytic stage of Plasmodium falciparum after 72 hrs by image-based HTS assay F 5.47 pIC50 3366 nM IC50 J Med Chem (2013) 56: 7727-7740 [PMID:23927763]
ChEMBL OSM: Late stage gametocytes. IC50 values determined from 21 point dose response curves. Avery Group Griffith. F 5.55 pIC50 2800 nM IC50 Open Source Malaria Deposition 1. http://malaria.ourexperiment.org
ChEMBL Antimalarial activity against asexual stage of Plasmodium falciparum 3D7 after 72 hrs by image-based HTS assay F 5.97 pIC50 1070 nM IC50 J Med Chem (2013) 56: 7727-7740 [PMID:23927763]
ChEMBL Antimalarial activity against multidrug-resistant Plasmodium falciparum W2 by SYBR green-based assay F 6.66 pIC50 217 nM IC50 Bioorg Med Chem Lett (2015) 25: 1100-1103 [PMID:25650255]
ChEMBL Antiplasmodial activity against late stage (IV/V) Plasmodium falciparum NF54 gametocytes transfected with GFP-LUC assessed as growth inhibition incubated for 72 hrs by mitotracker Red-CMXROS dye based fluorescence microscopic analysis F 5.28 pEC50 5250 nM EC50 J Med Chem (2016) 59: 9672-9685 [PMID:27631715]
Plasmodium yoelii (target type: ORGANISM) [ChEMBL: CHEMBL612889]
ChEMBL Antimalarial activity against sporozoite stage of Plasmodium yoelii assessed as invasion of human HepG2 cells expressing CD81 incubated for 2 hrs prior to inoculation measured after 1 hr by immunofluorescence assay in presence of penicillin/streptomycin F 6 pIC50 <1000 nM IC50 J Med Chem (2013) 56: 7761-7771 [PMID:23927658]

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]