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ChEMBL ligand: CHEMBL298470 (SB-252263-AAB, Tafenoquina, Tafenoquine, WR 238605) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum NIG59 assessed as parasitic growth inhibition | F | 6.05 | pIC50 | 900 | nM | IC50 | Bioorg Med Chem (2023) 88-89: 117339-117339 [PMID:37236020] |
ChEMBL | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 assessed as parasitic growth inhibition | F | 6.22 | pIC50 | 600 | nM | IC50 | Bioorg Med Chem (2023) 88-89: 117339-117339 [PMID:37236020] |
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 | Antimalarial activity against blood stages Plasmodium falciparum D6 assessed as reduction in parasite growth | F | 7.23 | pIC50 | 59 | nM | IC50 | Bioorg Med Chem (2023) 88-89: 117339-117339 [PMID:37236020] |
ChEMBL | Antimalarial activity against blood stages Plasmodium falciparum W2 assessed as inhibition of parasitic growth | F | 7.23 | pIC50 | 59 | nM | IC50 | Bioorg Med Chem (2023) 88-89: 117339-117339 [PMID:37236020] |
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 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]