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 ELQ-300 resistant Plasmodium falciparum Dd2 harboring Cyt b I22L mutant assessed as reduction in parasite growth incubated for 72 hrs by [3H]-hypoxanthine incorporation assay | F | 6.74 | pEC50 | 180 | nM | EC50 | Eur J Med Chem (2024) 270: 116354-116354 [PMID:38554474] |
| ChEMBL | Antiplasmodial activity against multidrug-resistant Plasmodium falciparum Dd2 harboring cyt b-I22L mutant infected in erythrocytes assessed as inhibition of parasite growth incubated for 72 hrs by [3H]hypoxanthine incorporation based microbeta counting analysis | F | 6.92 | pEC50 | 120 | nM | EC50 | Eur J Med Chem (2024) 276: 116677-116677 [PMID:39024967] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum Dd2 assessed as reduction in parasite growth incubated for 72 hrs by [3H]-hypoxanthine incorporation assay | F | 7.68 | pEC50 | 21 | nM | EC50 | Eur J Med Chem (2024) 270: 116354-116354 [PMID:38554474] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum Dd2 infected in erythrocytes assessed as inhibition of parasite growth incubated for 72 hrs by [3H]hypoxanthine incorporation based microbeta counting analysis | F | 7.85 | pEC50 | 14 | nM | EC50 | Eur J Med Chem (2024) 276: 116677-116677 [PMID:39024967] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum Dd2 | F | 8.6 | pEC50 | 2.5 | nM | EC50 | Eur J Med Chem (2021) 210: 112955-112955 [PMID:33131885] |
| 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] |
| 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 | Antimalarial activity against Plasmodium falciparum Tm90-C2B | F | 8.85 | pEC50 | 1.4 | nM | EC50 | Eur J Med Chem (2021) 210: 112955-112955 [PMID:33131885] |
| 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 | 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 3D7 | F | 8.89 | pEC50 | 1.3 | nM | EC50 | Eur J Med Chem (2019) 181: 111353-111353 [PMID:31525705] |
| 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 | 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 | 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 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 36:
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]
