P218 [Ligand Id: 9740] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3040038 |
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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 | Antimalarial activity against Plasmodium falciparum V1/S harboring DHFR N51I+C59R+S108N+I164L quadruple mutant assessed as reduction parasite growth by [3H]-hypoxanthine incorporation assay | F | 7.25 | pEC50 | 56 | nM | EC50 | Medchemcomm (2016) 7: 749-768 |
| Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase in Plasmodium falciparum TM4 [GtoPdb: 2981] | ||||||||
| GtoPdb | Parasite growth inhibition assay | - | 8.34 | pIC50 | 4.6 | nM | IC50 | Proc Natl Acad Sci USA (2012) 109: 16823-8 [PMID:23035243] |
| Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase in Plasmodium falciparum [GtoPdb: 2981] | ||||||||
| GtoPdb | Parasite liver stage assay | - | 7.92 | pEC50 | <12 | nM | EC50 | Nat Commun (2018) 9: 1837 [PMID:29743474] |
| Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase in Plasmodium falciparum NF54 [GtoPdb: 2981] | ||||||||
| GtoPdb | Parasite exflagellation assay | - | 8.4 | pIC50 | 4 | nM | IC50 | Int J Parasitol (2021) 51: 635-642 [PMID:33713651] |
| Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase in Plasmodium vivax [GtoPdb: 2981] | ||||||||
| GtoPdb | Parasite liver stage assay | - | 7.35 | pEC50 | 45 | nM | EC50 | Nat Commun (2018) 9: 1837 [PMID:29743474] |
ChEMBL data shown on this page come from version 33:
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]
