M5717 [Ligand Id: 9737] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4091762 (Cabamiquine, DDD-107498, DDD107498, DDD498, M-5717, M5717, MMV-121, MMV121) |
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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/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] |
| 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 blood stage chloroquine-sensitive Plasmodium falciparum 3D7 infected in human red blood cells measured by [3H]hypoxanthine incorporation assay | F | 9 | pEC50 | 1 | nM | EC50 | Bioorg Med Chem (2022) 56: 116614-116614 [PMID:35033884] |
| 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 | Antimalarial activity against Plasmodium falciparum 3D7 | 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 | Antimalarial activity against drug resistant Plasmodium falciparum D6 | F | 9 | pEC50 | <1 | nM | EC50 | J Med Chem (2016) 59: 9668-9671 [PMID:27775354] |
| 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 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 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]
