Synonyms: GNF-Pf-4188 | TCMDC-125815
Compound class:
Synthetic organic
Comment: MMV008138 is a drug-like compound with antimalarial activity that was chosen as one of the chemotypes to be included in the MMV Malaria Box [2-3].
The 1R,3S enantiomer, represented by PubChem CID 987146, has the highest antimalarial potency [4-5]. The Malaria tab on this ligand page provides additional curator comments of relevance to the Guide to MALARIA PHARMACOLOGY. ![]() Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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References |
1. Bowman JD, Merino EF, Brooks CF, Striepen B, Carlier PR, Cassera MB. (2014)
Antiapicoplast and gametocytocidal screening to identify the mechanisms of action of compounds within the malaria box. Antimicrob Agents Chemother, 58 (2): 811-9. [PMID:24247137] |
2. Spangenberg T, Burrows JN, Kowalczyk P, McDonald S, Wells TN, Willis P. (2013)
The open access malaria box: a drug discovery catalyst for neglected diseases. PLoS ONE, 8 (6): e62906. [PMID:23798988] |
3. Van Voorhis WC, Adams JH, Adelfio R, Ahyong V, Akabas MH, Alano P, Alday A, Alemán Resto Y, Alsibaee A, Alzualde A et al.. (2016)
Open Source Drug Discovery with the Malaria Box Compound Collection for Neglected Diseases and Beyond. PLoS Pathog, 12 (7): e1005763. [PMID:27467575] |
4. Wu W, Herrera Z, Ebert D, Baska K, Cho SH, DeRisi JL, Yeh E. (2015)
A chemical rescue screen identifies a Plasmodium falciparum apicoplast inhibitor targeting MEP isoprenoid precursor biosynthesis. Antimicrob Agents Chemother, 59 (1): 356-64. [PMID:25367906] |
5. Yao ZK, Krai PM, Merino EF, Simpson ME, Slebodnick C, Cassera MB, Carlier PR. (2015)
Determination of the active stereoisomer of the MEP pathway-targeting antimalarial agent MMV008138, and initial structure-activity studies. Bioorg Med Chem Lett, 25 (7): 1515-9. [PMID:25754494] |