M5717 [Ligand Id: 9737] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4091762 (DDD107498, DDD-107498, DDD498, M5717, M-5717, MMV121, MMV-121) |
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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 by IonWorks patch-clamp electrophysiology method | B | 4.8 | pIC50 | 16000 | nM | IC50 | J Med Chem (2016) 59: 9672-9685 [PMID:27631715] |
| Plasmodium berghei (target type: ORGANISM) [ChEMBL: CHEMBL612653] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium berghei ookinete form assessed as growth inhibition incubated for 22 hrs by GFP-based fluorescence microscopic analysis | F | 8.3 | pEC50 | 5 | nM | EC50 | J Med Chem (2016) 59: 9672-9685 [PMID:27631715] |
| ChEMBL | Antimalarial activity against Plasmodium berghei ookinete form | F | 8.3 | pEC50 | 5 | nM | EC50 | J Med Chem (2016) 59: 9668-9671 [PMID:27775354] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against erythrocytic stage of chloroquine-sensitive Plasmodium falciparum NF54 assessed as reduction in [3H]hypoxanthine incorporation after 48 hrs by liquid scintillation counting method | F | 9.89 | pIC50 | 0.13 | nM | IC50 | Bioorg Med Chem (2017) 25: 2251-2259 [PMID:28279559] |
| 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 | 7.62 | pEC50 | 24 | nM | EC50 | J Med Chem (2016) 59: 9672-9685 [PMID:27631715] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum late stage (IV-V) gametocytes | F | 7.62 | pEC50 | 24 | nM | EC50 | J Med Chem (2016) 59: 9668-9671 [PMID:27775354] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum 3D7 | F | 9 | pEC50 | 1 | nM | EC50 | J Med Chem (2016) 59: 9668-9671 [PMID:27775354] |
| ChEMBL | Antimalarial activity against drug resistant Plasmodium falciparum D6 | F | 9 | pEC50 | <1 | nM | EC50 | J Med Chem (2016) 59: 9668-9671 [PMID:27775354] |
| ChEMBL | Antimalarial activity against drug resistant Plasmodium falciparum V1/S | F | 9 | pEC50 | <1 | nM | EC50 | J Med Chem (2016) 59: 9668-9671 [PMID:27775354] |
| ChEMBL | Antimalarial activity against drug resistant Plasmodium falciparum 7G8 | F | 9 | pEC50 | <1 | nM | EC50 | J Med Chem (2016) 59: 9668-9671 [PMID:27775354] |
| ChEMBL | Antimalarial activity against drug resistant Plasmodium falciparum TM90C2A | F | 9 | pEC50 | <1 | nM | EC50 | J Med Chem (2016) 59: 9668-9671 [PMID:27775354] |
| ChEMBL | Antimalarial activity against drug resistant Plasmodium falciparum K1 | F | 9 | pEC50 | <1 | nM | EC50 | J Med Chem (2016) 59: 9668-9671 [PMID:27775354] |
| ChEMBL | Antimalarial activity against drug resistant Plasmodium falciparum W2 | F | 9 | pEC50 | <1 | nM | EC50 | J Med Chem (2016) 59: 9668-9671 [PMID:27775354] |
| ChEMBL | Antimalarial activity against drug resistant Plasmodium falciparum NF5 | F | 9 | pEC50 | <1 | nM | EC50 | J Med Chem (2016) 59: 9668-9671 [PMID:27775354] |
| ChEMBL | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in human red blood cells assessed as growth inhibition by SYBR Green fluorescence assay | F | 9 | pEC50 | 1 | nM | EC50 | J Med Chem (2016) 59: 9672-9685 [PMID:27631715] |
| ChEMBL | Antiplasmodial activity against drug resistant Plasmodium falciparum V1/S by [3H]hypoxanthine incorporation assay | F | 9.15 | pEC50 | 0.7 | nM | EC50 | J Med Chem (2016) 59: 9672-9685 [PMID:27631715] |
| ChEMBL | Antiplasmodial activity against drug resistant Plasmodium falciparum K1 by [3H]hypoxanthine incorporation assay | F | 9.4 | pEC50 | 0.4 | nM | EC50 | J Med Chem (2016) 59: 9672-9685 [PMID:27631715] |
| ChEMBL | Antiplasmodial activity against drug resistant Plasmodium falciparum 7G8 by [3H]hypoxanthine incorporation assay | F | 9.4 | pEC50 | 0.4 | nM | EC50 | J Med Chem (2016) 59: 9672-9685 [PMID:27631715] |
| ChEMBL | Antiplasmodial activity against drug resistant Plasmodium falciparum D6 by [3H]hypoxanthine incorporation assay | F | 9.4 | pEC50 | 0.4 | nM | EC50 | J Med Chem (2016) 59: 9672-9685 [PMID:27631715] |
| ChEMBL | Antiplasmodial activity against drug resistant Plasmodium falciparum TM90C2A by [3H]hypoxanthine incorporation assay | F | 9.4 | pEC50 | 0.4 | nM | EC50 | J Med Chem (2016) 59: 9672-9685 [PMID:27631715] |
| ChEMBL | Antiplasmodial activity against drug resistant Plasmodium falciparum W2 by [3H]hypoxanthine incorporation assay | F | 9.4 | pEC50 | 0.4 | nM | EC50 | J Med Chem (2016) 59: 9672-9685 [PMID:27631715] |
| ChEMBL | Antiplasmodial activity against drug resistant Plasmodium falciparum NF5 by [3H]hypoxanthine incorporation assay | F | 9.52 | pEC50 | 0.3 | nM | EC50 | J Med Chem (2016) 59: 9672-9685 [PMID:27631715] |
| Plasmodium falciparum (isolate K1 / Thailand) in Plasmodium falciparum K1 (target type: ORGANISM) [ChEMBL: CHEMBL612856] | ||||||||
| ChEMBL | Antiplasmodial activity against erythrocytic stage of chloroquine/pyrimethamine-resistant Plasmodium falciparum K1 assessed as reduction in [3H]hypoxanthine incorporation after 48 hrs by liquid scintillation counting method | F | 9.66 | pIC50 | 0.22 | nM | IC50 | Bioorg Med Chem (2017) 25: 2251-2259 [PMID:28279559] |
| Plasmodium yoelii (target type: ORGANISM) [ChEMBL: CHEMBL612889] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium yoelli liver stage forms | F | 9 | pEC50 | 1 | nM | EC50 | J Med Chem (2016) 59: 9672-9685 [PMID:27631715] |
| ChEMBL | Antimalarial activity against Plasmodium yoelii | F | 9 | pEC50 | 1 | nM | EC50 | J Med Chem (2016) 59: 9668-9671 [PMID:27775354] |
| Plasmodium falciparum elongation factor 2 in Plasmodium berghei [GtoPdb: 2975] | ||||||||
| GtoPdb | Parasite liver stage assay | - | 8.78 | pEC50 | 1.65 | nM | EC50 | Nature (2015) 522: 315-20 [PMID:26085270] |
| Plasmodium falciparum elongation factor 2 in Plasmodium falciparum NF54 [GtoPdb: 2975] | ||||||||
| GtoPdb | Standard membrane feeding assay (SMFA) | - | 8 | pEC50 | 10 | nM | EC50 | Nature (2015) 522: 315-20 [PMID:26085270] |
| GtoPdb | Parasite gamete formation assay | - | 8.74 | pEC50 | 1.8 | nM | EC50 | Nature (2015) 522: 315-20 [PMID:26085270] |
| GtoPdb | Standard membrane feeding assay (SMFA) | - | 8.74 | pEC50 | 1.8 | nM | EC50 | Nature (2015) 522: 315-20 [PMID:26085270] |
| GtoPdb | Parasite gamete formation assay | - | 8.92 | pEC50 | 1.2 | nM | EC50 | Nature (2015) 522: 315-20 [PMID:26085270] |
| Plasmodium falciparum elongation factor 2 in Plasmodium falciparum 3D7 [GtoPdb: 2975] [UniProtKB: Q8IKW5] | ||||||||
| GtoPdb | Parasite growth inhibition assay | - | 9 | pEC50 | 1 | nM | EC50 | Nature (2015) 522: 315-20 [PMID:26085270] |
ChEMBL data shown on this page come from version 31:
Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]
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