ELQ-300 [Ligand Id: 10021] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2431810 |
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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 drug-resistant Plasmodium falciparum Dd2 harboring CytB Ile22Leu mutant | F | 6.83 | pIC50 | 148 | nM | IC50 | J Med Chem (2018) 61: 4213-4227 [PMID:29665687] |
| ChEMBL | Antimalarial activity against wild type Plasmodium falciparum Dd2 | F | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2018) 61: 4213-4227 [PMID:29665687] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum 3D7 | F | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2016) 59: 5587-5603 [PMID:26791529] |
| ChEMBL | Antimalarial activity against atovaquone-resistant Plasmodium falciparum TM90C2B | F | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2016) 59: 5587-5603 [PMID:26791529] |
| ChEMBL | Antimalarial activity against atovaquone-resistant clinical isolate Plasmodium falciparum TM90-C2B infected in human red blood cells assessed as suppression of parasitemia after 72 hrs by SYBR Green I-based fluorescence method | F | 8.85 | pEC50 | 1.4 | nM | EC50 | J Med Chem (2014) 57: 3818-3834 [PMID:24720377] |
| ChEMBL | Antiparasitic activity against Plasmodium falciparum 3D7 | F | 8.89 | pEC50 | 1.3 | nM | EC50 | Eur J Med Chem (2019) 181: 111353-111353 [PMID:31525705] |
| ChEMBL | Antiparasitic activity against Plasmodium falciparum D6 | F | 8.89 | pEC50 | 1.3 | nM | EC50 | Eur J Med Chem (2019) 181: 111353-111353 [PMID:31525705] |
| ChEMBL | Antiparasitic activity against Plasmodium falciparum infected in human PBMC | F | 8.89 | pEC50 | 1.3 | nM | EC50 | Eur J Med Chem (2019) 181: 111353-111353 [PMID:31525705] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum TM93-C1088 assessed as suppression of parasitemia after 72 hrs by SYBR Green I-based fluorescence method | F | 9 | pEC50 | 1 | nM | EC50 | J Med Chem (2014) 57: 3818-3834 [PMID:24720377] |
| ChEMBL | Antimicrobial activity against clinical isolates of Plasmodium falciparum | F | 9 | pEC50 | 1 | nM | EC50 | J Med Chem (2013) 56: 7741-7749 [PMID:23927720] |
| ChEMBL | Antiparasitic activity against Plasmodium falciparum | F | 9.24 | pEC50 | 0.58 | nM | EC50 | Eur J Med Chem (2019) 181: 111353-111353 [PMID:31525705] |
| Plasmodium falciparum D6 (target type: ORGANISM) [ChEMBL: CHEMBL2367107] | ||||||||
| ChEMBL | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 MRA-285 infected in human red blood cells assessed as suppression of parasitemia after 72 hrs by SYBR Green I-based fluorescence method | F | 8.66 | pEC50 | 2.2 | nM | EC50 | J Med Chem (2014) 57: 3818-3834 [PMID:24720377] |
| Plasmodium falciparum cytochrome b in Plasmodium falciparum TM90C2B [GtoPdb: 3087] | ||||||||
| GtoPdb | Parasite growth inhibition assay | - | 8.55 | pIC50 | 2.84 | nM | IC50 | Sci Transl Med (2013) 5: 177ra37 [PMID:23515079] |
| GtoPdb | Parasite growth inhibition assay | - | 8.77 | pIC50 | 1.7 | nM | IC50 | Sci Transl Med (2013) 5: 177ra37 [PMID:23515079] |
| Plasmodium falciparum cytochrome b in Plasmodium berghei [GtoPdb: 3087] | ||||||||
| GtoPdb | Parasite liver stage assay | - | 8.99 | pEC50 | 1.02 | nM | EC50 | Sci Transl Med (2013) 5: 177ra37 [PMID:23515079] |
| Plasmodium falciparum cytochrome b in Plasmodium cynomolgi [GtoPdb: 3087] | ||||||||
| GtoPdb | Parasite liver stage assay | - | 7 | pIC50 | ~100 | nM | IC50 | Sci Transl Med (2013) 5: 177ra37 [PMID:23515079] |
| Plasmodium falciparum cytochrome b in Plasmodium falciparum NF54 [GtoPdb: 3087] | ||||||||
| GtoPdb | Parasite late stage (IV–V) gametocyte assay | - | 7.14 | pIC50 | 71.9 | nM | IC50 | Sci Transl Med (2013) 5: 177ra37 [PMID:23515079] |
| Plasmodium falciparum cytochrome b in Plasmodium falciparum Dd2 [GtoPdb: 3087] | ||||||||
| GtoPdb | Parasite growth inhibition assay | - | 8.6 | pIC50 | 2.5 | nM | IC50 | Sci Transl Med (2013) 5: 177ra37 [PMID:23515079] |
| Plasmodium falciparum cytochrome b in Plasmodium falciparum D6 [GtoPdb: 3087] | ||||||||
| GtoPdb | Parasite growth inhibition assay | - | 8.51 | pIC50 | 3.06 | nM | IC50 | Sci Transl Med (2013) 5: 177ra37 [PMID:23515079] |
| GtoPdb | Parasite growth inhibition assay | - | 8.66 | pIC50 | 2.2 | nM | IC50 | Sci Transl Med (2013) 5: 177ra37 [PMID:23515079] |
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]
