MMV048 [Ligand Id: 9726] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2041980 (J3.367.891F, MMV-048, MMV048, Mmv-390048, MMV-390048) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2019) 62: 10526-10562 [PMID:31385706] |
| ChEMBL | Inhibition of human ERG expressed in CHO cells by IonWorks assay | B | 5.33 | pIC50 | 4700 | nM | IC50 | J Med Chem (2012) 55: 3479-3487 [PMID:22390538] |
| Plasmodium cynomolgi (target type: ORGANISM) [ChEMBL: CHEMBL613883] | ||||||||
| ChEMBL | Antimalarial activity against hypnozoites stage Plasmodium cynomolgi infected in primary rhesus monkey hepatocytes measured on day 5 | F | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2019) 62: 10526-10562 [PMID:31385706] |
| ChEMBL | Antimalarial activity against schizont stage Plasmodium cynomolgi infected in primary rhesus monkey hepatocytes | F | 7.19 | pEC50 | 64 | nM | EC50 | J Med Chem (2019) 62: 10526-10562 [PMID:31385706] |
| ChEMBL | Antimalarial activity against hypnozoites stage Plasmodium cynomolgi infected in primary rhesus monkey hepatocytes | F | 7.21 | pEC50 | 61 | nM | EC50 | J Med Chem (2019) 62: 10526-10562 [PMID:31385706] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antimalarial activity against drug-resistant Plasmodium falciparum Dd2 harboring PI4K S743T mutant | F | 7.06 | pIC50 | 88 | nM | IC50 | J Med Chem (2018) 61: 4213-4227 [PMID:29665687] |
| ChEMBL | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum NF54 after 24 hrs by hypoxanthine incorporation assay | F | 7.55 | pIC50 | 28 | nM | IC50 | J Med Chem (2012) 55: 3479-3487 [PMID:22390538] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum NF54 after 24 to 72 hrs | F | 7.55 | pIC50 | 28 | nM | IC50 | J Med Chem (2018) 61: 8061-8077 [PMID:29771541] |
| 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 | 7.55 | pIC50 | 28 | nM | IC50 | J Med Chem (2021) 64: 2291-2309 [PMID:33573376] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum NF54 | F | 7.55 | pIC50 | 28 | nM | IC50 | Eur J Med Chem (2021) 210: 112955-112955 [PMID:33131885] |
| ChEMBL | Antiplasmodial activity against blood stage plasmodium falciparum NF54 | F | 7.55 | pIC50 | 28 | nM | IC50 | J Med Chem (2022) 65: 13172-13197 [PMID:36166733] |
| ChEMBL | Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 after 24 hrs by hypoxanthine incorporation assay | F | 7.6 | pIC50 | 25 | nM | IC50 | J Med Chem (2012) 55: 3479-3487 [PMID:22390538] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum K1 | F | 7.6 | pIC50 | 25 | nM | IC50 | Eur J Med Chem (2021) 210: 112955-112955 [PMID:33131885] |
| ChEMBL | Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 | F | 7.75 | pIC50 | 17.8 | nM | IC50 | Eur J Med Chem (2013) 66: 314-323 [PMID:23811093] |
| ChEMBL | Antiplasmodial activity against chloroquine-resistant asexual erythrocytic stage of Plasmodium falciparum Dd2 assessed as parasite growth inhibition by lactate dehydrogenase assay | F | 7.75 | pIC50 | 17.8 | nM | IC50 | J Med Chem (2014) 57: 435-448 [PMID:24354322] |
| ChEMBL | Antiplasmodial activity against chloroquine-sensitive asexual erythrocytic stage of Plasmodium falciparum D10 assessed as parasite growth inhibition by lactate dehydrogenase assay | F | 8.05 | pIC50 | 9.01 | nM | IC50 | J Med Chem (2014) 57: 435-448 [PMID:24354322] |
| ChEMBL | Antimalarial activity against wild type Plasmodium falciparum Dd2 | F | 8.28 | pIC50 | 5.2 | nM | IC50 | J Med Chem (2018) 61: 4213-4227 [PMID:29665687] |
| ChEMBL | Antimalarial activity against early stage Plasmodium falciparum gametocytes by luciferase reporter gene assay | F | 6.67 | pEC50 | 214 | nM | EC50 | J Med Chem (2019) 62: 10526-10562 [PMID:31385706] |
| ChEMBL | Antimalarial activity against late stage Plasmodium falciparum gametocytes by luciferase reporter gene assay | F | 6.85 | pEC50 | 140 | nM | EC50 | J Med Chem (2019) 62: 10526-10562 [PMID:31385706] |
| ChEMBL | Antimalarial activity against stage 5 Plasmodium falciparum assessed as reduction in oocyst formation in mosquito midgut pretreated 24 hrs before feeding by standard membrane-feeding assay | F | 6.95 | pEC50 | 111 | nM | EC50 | J Med Chem (2019) 62: 10526-10562 [PMID:31385706] |
| ChEMBL | Antimalarial activity against late stage Plasmodium falciparum gametocytes assessed as reduction in gametogenesis exflagellation after 24 hrs | F | 7.05 | pEC50 | 90 | nM | EC50 | J Med Chem (2019) 62: 10526-10562 [PMID:31385706] |
| ChEMBL | Ex-vivo antimalarial activity against Plasmodium falciparum serum derived from 40 mg, po treated human after 144 hrs | F | 7.62 | pEC50 | 24 | nM | EC50 | J Med Chem (2019) 62: 10526-10562 [PMID:31385706] |
| Plasmodium falciparum phosphatidylinositol 4-kinase beta in Plasmodium cynomolgi [GtoPdb: 2972] | ||||||||
| GtoPdb | Parasite liver stage assay | - | 5 | pIC50 | >10000 | nM | IC50 | Sci Transl Med (2017) 9: [PMID:28446690] |
| GtoPdb | Parasite liver stage assay | - | 7.19 | pIC50 | 64 | nM | IC50 | Sci Transl Med (2017) 9: [PMID:28446690] |
| GtoPdb | Parasite liver stage assay | - | 7.21 | pIC50 | 61 | nM | IC50 | Sci Transl Med (2017) 9: [PMID:28446690] |
| Plasmodium falciparum phosphatidylinositol 4-kinase beta in Plasmodium falciparum [GtoPdb: 2972] | ||||||||
| GtoPdb | - | - | 6.52 | pKd | 300 | nM | Kd | Sci Transl Med (2017) 9: [PMID:28446690] |
| GtoPdb | - | - | 7 | pKd | 100 | nM | Kd | Sci Transl Med (2017) 9: [PMID:28446690] |
| GtoPdb | Standard membrane feeding assay (SMFA) | - | 6.95 | pIC50 | 111 | nM | IC50 | Sci Transl Med (2017) 9: [PMID:28446690] |
| Plasmodium falciparum phosphatidylinositol 4-kinase beta in Plasmodium falciparum NF54 [GtoPdb: 2972] | ||||||||
| GtoPdb | Parasite gametocyte viability assay | - | 6.55 | pIC50 | 285 | nM | IC50 | Sci Transl Med (2017) 9: [PMID:28446690] |
| GtoPdb | Parasite gametocyte viability assay | - | 6.67 | pIC50 | 214 | nM | IC50 | Sci Transl Med (2017) 9: [PMID:28446690] |
| GtoPdb | Parasite gametocyte viability assay | - | 6.85 | pIC50 | 140 | nM | IC50 | Sci Transl Med (2017) 9: [PMID:28446690] |
| GtoPdb | Parasite growth inhibition assay | - | 7.55 | pIC50 | 28 | nM | IC50 | Sci Transl Med (2017) 9: [PMID:28446690] |
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]
