piperaquine [Ligand Id: 10025] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL303933 (Piperaquine, Piperaquinoline) |
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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 Plasmodium falciparum FCM29 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter | F | 7.01 | pIC50 | 98 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum FCM29 harboring Ppcrt M74I, N75E, K76T, A220S, Q271E, N326S and I356T mutant gene, Pmdr1 N86Y mutant gene and Pfmrp H191Y and S437A mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter | F | 7.01 | pIC50 | 98 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antiplasmodial activity against multidrug-resistant Plasmodium falciparum VS/1 by [3H]hypoxanthine incorporation assay | F | 7.06 | pIC50 | 88 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 3131-3134 [PMID:19364853] |
| ChEMBL | Antimalarial activity against trophozoites stage of Plasmodium falciparum assessed as parasites growth inhibition using giemsa staining after 24 to 56 hrs by microscopic analysis in presence of 10% human serum | F | 7.06 | pIC50 | 87.6 | nM | IC50 | Antimicrob Agents Chemother (2011) 55: 961-966 [PMID:21135175] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT K2 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter | F | 7.08 | pIC50 | 84 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT K2 harboring Ppcrt M74I, N75E, K76T, A220S, Q271E, N326S mutant gene, Pmdr1 S1034C, N1042D mutant gene and Pfmrp H191Y and S437A mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter | F | 7.08 | pIC50 | 84 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum K1 assessed as inhibition of [3H]hypoxanthine incorporation by beta counting | F | 7.09 | pIC50 | 82.06 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 3534-3537 [PMID:19528277] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum infected in human erythrocytes assessed as inhibition of [G-3H]hypoxanthine uptake incubated for 42 hrs by liquid scintillation spectrometry | F | 7.09 | pIC50 | 81.3 | nM | IC50 | Eur J Med Chem (2020) 188: 111983-111983 [PMID:31911292] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT 10500 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter | F | 7.09 | pIC50 | 81 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT 10500 harboring Pfcrt Q271E mutant gene and Ppcrt I371R mutant gene and Pfnhe-1 ms4760 microsatellite mutant assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter | F | 7.09 | pIC50 | 81 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum PA assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter | F | 7.1 | pIC50 | 80 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum PA harboring Ppcrt M74I, N75E, K76T, A220S, Q271E, N326S and I356T mutant gene, Pmdr1 N86Y mutant gene and Pfmrp H191Y and S437A mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter | F | 7.1 | pIC50 | 80 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum trophozoites infected in human erythrocytes assessed as growth inhibition by microscopic analysis using giemsa staining | F | 7.11 | pIC50 | 77.2 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 5146-5150 [PMID:20876370] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT A4 harboring Ppcrt M74I, N75E, K76T, A220H, Q271E, N326S and I356T mutant gene, Pmdr1 Y184F, N1042D, D1246Y mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter | F | 7.12 | pIC50 | 75 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT A4 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter | F | 7.12 | pIC50 | 75 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT 10336 harboring Pfcrt Q271E mutant gene and Ppcrt I371R mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter | F | 7.13 | pIC50 | 74 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT 10336 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter | F | 7.13 | pIC50 | 74 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum 106/1 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter | F | 7.16 | pIC50 | 69 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum 106/1 harboring Ppcrt M74I, N75E, K76T, A220S, Q271E, N326S and I356T mutant gene, Pmdr1 N86Y mutant gene and Pfmrp H191Y and S437A mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter | F | 7.16 | pIC50 | 69 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT K4 harboring Ppcrt M74I, N75E, K76T, A220S, Q271E, N326S mutant gene, Pmdr1 S1034C, N1042D mutant gene and Pfmrp H191Y and S437A mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter | F | 7.19 | pIC50 | 64 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT K4 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter | F | 7.19 | pIC50 | 64 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT Guy harboring Ppcrt K76T, A220S, N326D and I371R mutant gene, Pmdr1 T184FN, 1042D and D1246Y, mutant gene and Pfmrp H191Y and S437A mutant gene and Pfnhe-1 ms4760 microsatellite mutant assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter | F | 7.2 | pIC50 | 63 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT Guy assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter | F | 7.2 | pIC50 | 63 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT K14 harboring Ppcrt M74I, N75E, K76T, A220S, Q271E, N326S mutant gene, Pmdr1 Y184F, S1034C, N1042D, D1246Y mutant gene and Pfmrp H191Y and S437A mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter | F | 7.21 | pIC50 | 61 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT K14 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter | F | 7.21 | pIC50 | 61 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum D6 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter | F | 7.24 | pIC50 | 58 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum 3D7 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter | F | 7.24 | pIC50 | 58 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum 3D7 harboring Ppcrt I371R mutant gene and Pfnhe-1 ms4760 microsatellite mutant assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter | F | 7.24 | pIC50 | 58 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum D6 harboring Ppcrt I371R mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter | F | 7.24 | pIC50 | 58 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT 9881 harboring Ppcrt I371R mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter | F | 7.25 | pIC50 | 56 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT 9881 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter | F | 7.25 | pIC50 | 56 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum | F | 7.25 | pIC50 | 56 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3302-3307 [PMID:20516285] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum HB3 harboring Ppcrt I371R mutant gene and Pfmdr1 Y184F mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter | F | 7.26 | pIC50 | 55 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum HB3 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter | F | 7.26 | pIC50 | 55 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum FCR3 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter | F | 7.28 | pIC50 | 53 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum FCR3 harboring Ppcrt M74I, N75E, K76T, A220S, Q271E, N326S and I356T mutant gene, Pmdr1 N86Y mutant gene and Pfmrp H191Y and S437A mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter | F | 7.28 | pIC50 | 53 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum W2 harboring Ppcrt M74I, N75E, K76T, A220S, Q271E, N326S and I356T mutant gene, Pmdr1 N86Y mutant gene and Pfmrp H191Y and S437A mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter | F | 7.28 | pIC50 | 52 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum W2 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter | F | 7.28 | pIC50 | 52 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against chloroquine-resistant Plasmodium falciparum RSA11 | F | 7.29 | pIC50 | 51.38 | nM | IC50 | Antimicrob Agents Chemother (2007) 51: 2265-2267 [PMID:17404003] |
| ChEMBL | Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human RBC assessed as reduction in parasite growth after 35 to 56 hrs by nucleic acid staining based flow cytometry | F | 7.29 | pIC50 | 50.8 | nM | IC50 | J Med Chem (2019) 62: 2485-2498 [PMID:30715882] |
| ChEMBL | Antimalarial activity against chloroquine-resistant Plasmodium falciparum 7G8-mdr7G8 | F | 7.3 | pIC50 | 49.71 | nM | IC50 | Antimicrob Agents Chemother (2007) 51: 2265-2267 [PMID:17404003] |
| ChEMBL | Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 | F | 7.31 | pIC50 | 49.03 | nM | IC50 | Antimicrob Agents Chemother (2007) 51: 2265-2267 [PMID:17404003] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT 31 harboring Ppcrt I371R mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter | F | 7.32 | pIC50 | 48 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT 31 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter | F | 7.32 | pIC50 | 48 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT 16332 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter | F | 7.32 | pIC50 | 48 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT 16332 harboring Ppcrt M74I, N75E, K76T, A220S, Q271E mutant gene, Pmdr1 N86Y mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter | F | 7.32 | pIC50 | 48 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT L1 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter | F | 7.33 | pIC50 | 47 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT L1 harboring Ppcrt M74I, N75E, K76T, A220S, Q271E mutant gene, Pmdr1 N86Y mutant gene and Pfmrp H191Y and S437A mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter | F | 7.33 | pIC50 | 47 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT Bres assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter | F | 7.34 | pIC50 | 46 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT Bres harboring Ppcrt M74I, N75E, K76T, A220S, Q271E, N326S and I356T mutant gene, Pmdr1 N86Y mutant gene and Pfmrp H191Y and S437A mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter | F | 7.34 | pIC50 | 46 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT 8425 harboring Ppcrt I371R mutant gene and Pfnhe-1 ms4760 microsatellite mutant assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter | F | 7.36 | pIC50 | 44 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT 8425 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter | F | 7.36 | pIC50 | 44 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antiplasmodial activity against multidrug-resistant Plasmodium falciparum VS/1 after 18 hrs by [3H]hypoxanthine incorporation assay | F | 7.38 | pIC50 | 42 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 5069-5073 [PMID:19770282] |
| ChEMBL | Antimalarial activity against chloroquine-resistant Plasmodium falciparum | F | 7.39 | pIC50 | 41 | nM | IC50 | Eur J Med Chem (2010) 45: 3245-3264 [PMID:20466465] |
| ChEMBL | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum | F | 7.39 | pIC50 | 40.7 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 237-243 [PMID:17967917] |
| ChEMBL | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum FC27 infected in human RBC assessed as reduction in parasite growth after 35 to 56 hrs by nucleic acid staining based flow cytometry | F | 7.41 | pIC50 | 38.5 | nM | IC50 | J Med Chem (2019) 62: 2485-2498 [PMID:30715882] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum harboring mutant pfcrt-76 gene after 18 hrs by [3H]hypoxanthine incorporation assay | F | 7.42 | pIC50 | 38 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 5069-5073 [PMID:19770282] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT Vol assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter | F | 7.43 | pIC50 | 37 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT Vol harboring Ppcrt M74I, N75E, K76T, A220S, Q271E, N326S mutant gene, Pmdr1 N86Y mutant gene and Pfmrp H191Y and S437A mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter | F | 7.43 | pIC50 | 37 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 | F | 7.43 | pIC50 | 36.9 | nM | IC50 | Antimicrob Agents Chemother (2007) 51: 2265-2267 [PMID:17404003] |
| ChEMBL | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum | F | 7.44 | pIC50 | 36 | nM | IC50 | Eur J Med Chem (2010) 45: 3245-3264 [PMID:20466465] |
| ChEMBL | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum | F | 7.45 | pIC50 | 35.5 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 237-243 [PMID:17967917] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum harboring wild type pfcrt-76 gene after 18 hrs by [3H]hypoxanthine incorporation assay | F | 7.46 | pIC50 | 35 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 5069-5073 [PMID:19770282] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum clinical isolate after 18 hrs by [3H]hypoxanthine incorporation assay | F | 7.49 | pIC50 | 32 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 5069-5073 [PMID:19770282] |
| ChEMBL | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum FC27 | F | 7.53 | pIC50 | 29.61 | nM | IC50 | Antimicrob Agents Chemother (2007) 51: 2265-2267 [PMID:17404003] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT 10354 harboring Ppcrt M74I, N75E, K76T, A220S mutant gene, Pmdr1 D1246Y mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter | F | 7.54 | pIC50 | 29 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT 10354 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter | F | 7.54 | pIC50 | 29 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3537-3544 [PMID:20547801] |
| ChEMBL | Antiplasmodial activity against multidrug-sensitive Plasmodium falciparum 3D7 after 18 hrs by [3H]hypoxanthine incorporation assay | F | 7.57 | pIC50 | 27 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 5069-5073 [PMID:19770282] |
| ChEMBL | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 106/1 | F | 7.65 | pIC50 | 22.22 | nM | IC50 | Antimicrob Agents Chemother (2007) 51: 2265-2267 [PMID:17404003] |
| ChEMBL | Antimalarial activity against multidrug-resistant Plasmodium falciparum clinical isolates infected assessed as reduction in parasite growth after 35 to 56 hrs by nucleic acid staining based flow cytometry | F | 7.68 | pIC50 | 20.7 | nM | IC50 | J Med Chem (2019) 62: 2485-2498 [PMID:30715882] |
| ChEMBL | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum T996 | F | 7.7 | pIC50 | 19.93 | nM | IC50 | Antimicrob Agents Chemother (2007) 51: 2265-2267 [PMID:17404003] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum infected in human erythrocytes assessed as growth inhibition by microscopic analysis using giemsa staining | F | 7.77 | pIC50 | 17.1 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 5146-5150 [PMID:20876370] |
| ChEMBL | Antimalarial activity against chloroquine-resistant Plasmodium falciparum 34-1/E | F | 7.79 | pIC50 | 16.38 | nM | IC50 | Antimicrob Agents Chemother (2007) 51: 2265-2267 [PMID:17404003] |
| ChEMBL | In vitro activity against Plasmodium falciparum W-2 | F | 7.8 | pIC50 | 16 | nM | IC50 | J Med Chem (1992) 35: 2129-2134 [PMID:1597862] |
| ChEMBL | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum TM6 infected in erythrocytes assessed as [3H]hypoxanthine incorporation | F | 7.8 | pIC50 | 15.8 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 1362-1366 [PMID:19188388] |
| ChEMBL | Antiparasitic activity against chloroquine-sensitive Plasmodium falciparum by [3H]hypoxanthine incorporation | F | 7.84 | pIC50 | 14.6 | nM | IC50 | J Med Chem (2008) 51: 1260-1277 [PMID:18260613] |
| ChEMBL | Antimicrobial activity against chloroquine-sensitive Plasmodium falciparum W2 by ELISA | F | 7.84 | pIC50 | 14.5 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 1200-1206 [PMID:20065051] |
| ChEMBL | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 infected in erythrocytes assessed as [3H]hypoxanthine incorporation | F | 7.87 | pIC50 | 13.4 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 1362-1366 [PMID:19188388] |
| ChEMBL | Antimicrobial activity against chloroquine-resistant Plasmodium falciparum K1 by ELISA | F | 7.9 | pIC50 | 12.5 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 1200-1206 [PMID:20065051] |
| ChEMBL | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum 7G8 harboring D10 pfcrt allele infected in erythrocytes assessed as [3H]hypoxanthine incorporation | F | 7.92 | pIC50 | 12 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 1362-1366 [PMID:19188388] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum at the ring stage infected in human erythrocytes assessed as growth inhibition by microscopic analysis using giemsa staining | F | 7.93 | pIC50 | 11.8 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 5146-5150 [PMID:20876370] |
| ChEMBL | Antimalarial activity against ring stage of Plasmodium falciparum assessed as parasites growth inhibition using giemsa staining after 24 to 56 hrs by microscopic analysis in presence of 10% human serum | F | 7.94 | pIC50 | 11.5 | nM | IC50 | Antimicrob Agents Chemother (2011) 55: 961-966 [PMID:21135175] |
| ChEMBL | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum C3 harboring Dd2 pfcrt allele infected in erythrocytes assessed as [3H]hypoxanthine incorporation | F | 7.94 | pIC50 | 11.5 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 1362-1366 [PMID:19188388] |
| ChEMBL | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum 7G8 infected in erythrocytes assessed as [3H]hypoxanthine incorporation | F | 7.95 | pIC50 | 11.2 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 1362-1366 [PMID:19188388] |
| ChEMBL | Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 assessed as inhibition of [3H]hypoxanthine incorporation | F | 7.96 | pIC50 | 11 | nM | IC50 | Antimicrob Agents Chemother (2011) 55: 961-966 [PMID:21135175] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum assessed as parasites growth inhibition using giemsa staining after 24 to 56 hrs by microscopic analysis in presence of 10% human serum | F | 7.97 | pIC50 | 10.8 | nM | IC50 | Antimicrob Agents Chemother (2011) 55: 961-966 [PMID:21135175] |
| ChEMBL | Antimicrobial activity against chloroquine-resistant Plasmodium falciparum HB3 by ELISA | F | 7.98 | pIC50 | 10.5 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 1200-1206 [PMID:20065051] |
| ChEMBL | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D10 harboring 7G8 pfcrt allele infected in erythrocytes assessed as [3H]hypoxanthine incorporation | F | 7.98 | pIC50 | 10.4 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 1362-1366 [PMID:19188388] |
| ChEMBL | Antimalarial activity against drug-resistant Plasmodium falciparum Dd2 harboring M133I mutant infected in human erythrocytes after 72 hrs by SYBR green 1-based fluorescence assay | F | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2019) 62: 3475-3502 [PMID:30852885] |
| ChEMBL | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum 7G8 harboring parental pfcrt allele infected in erythrocytes assessed as [3H]hypoxanthine incorporation | F | 8.04 | pIC50 | 9.1 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 1362-1366 [PMID:19188388] |
| ChEMBL | Antimalarial activity against multidrug-resistant Plasmodium falciparum Dd2 infected in human erythrocytes by SYBR green 1-based fluorescence assay | F | 8.05 | pIC50 | 9 | nM | IC50 | J Med Chem (2019) 62: 3475-3502 [PMID:30852885] |
| ChEMBL | In vitro activity against Plasmodium falciparum D6 | F | 8.08 | pIC50 | 8.3 | nM | IC50 | J Med Chem (1992) 35: 2129-2134 [PMID:1597862] |
| ChEMBL | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D10 infected in erythrocytes assessed as [3H]hypoxanthine incorporation | F | 8.09 | pIC50 | 8.1 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 1362-1366 [PMID:19188388] |
| ChEMBL | Antimalarial activity against drug-resistant Plasmodium falciparum Dd2 harboring M133I/A138T double mutant infected in human erythrocytes after 72 hrs by SYBR green 1-based fluorescence assay | F | 8.13 | pIC50 | 7.4 | nM | IC50 | J Med Chem (2019) 62: 3475-3502 [PMID:30852885] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum 3D7 infected in human erythrocytes after 72 hrs by SYBR green 1-based fluorescence assay | F | 8.14 | pIC50 | 7.2 | nM | IC50 | J Med Chem (2019) 62: 3475-3502 [PMID:30852885] |
| ChEMBL | Antimalarial activity against drug-resistant Plasmodium falciparum Dd2 harboring V259L mutant infected in human erythrocytes after 72 hrs by SYBR green 1-based fluorescence assay | F | 8.15 | pIC50 | 7.1 | nM | IC50 | J Med Chem (2019) 62: 3475-3502 [PMID:30852885] |
| ChEMBL | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum C6harboring 7G8 pfcrt allele infected in erythrocytes assessed as [3H]hypoxanthine incorporation | F | 8.18 | pIC50 | 6.6 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 1362-1366 [PMID:19188388] |
| ChEMBL | Antimicrobial activity against chloroquine-sensitive Plasmodium falciparum D6 by ELISA | F | 8.2 | pIC50 | 6.26 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 1200-1206 [PMID:20065051] |
| ChEMBL | Antimicrobial activity against Plasmodium falciparum by ELISA | F | 8.21 | pIC50 | 6.1 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 1200-1206 [PMID:20065051] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum clinical isolates measured after 72 hrs by SYBR green dye based fluorescence assay | F | 8.23 | pIC50 | 5.9 | nM | IC50 | J Med Chem (2020) 63: 6179-6202 [PMID:32390431] |
| ChEMBL | Antimalarial activity against drug-resistant Plasmodium falciparum 3D7 harboring A82T/V259L double mutant infected in human erythrocytes after 72 hrs by SYBR green 1-based fluorescence assay | F | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2019) 62: 3475-3502 [PMID:30852885] |
| ChEMBL | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum C2 infected in erythrocytes assessed as [3H]hypoxanthine incorporation | F | 8.41 | pIC50 | 3.9 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 1362-1366 [PMID:19188388] |
| ChEMBL | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in erythrocytes assessed as [3H]hypoxanthine incorporation | F | 8.47 | pIC50 | 3.4 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 1362-1366 [PMID:19188388] |
| ChEMBL | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as inhibition of [3H]hypoxanthine incorporation | F | 8.52 | pIC50 | 3 | nM | IC50 | Antimicrob Agents Chemother (2011) 55: 961-966 [PMID:21135175] |
| ChEMBL | Antimicrobial activity against Plasmodium falciparum harboring mdr1 N86Y/D1246Y/Y184F mutant gene by ELISA | F | 8.8 | pIC50 | 1.6 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 1200-1206 [PMID:20065051] |
| ChEMBL | Antimalarial activity against multidrug resistant Plasmodium falciparum Dd2 | F | 8.82 | pIC50 | 1.5 | nM | IC50 | Eur J Med Chem (2021) 226: 113865-113865 [PMID:34655985] |
| ChEMBL | Antimalarial activity against CQ-sensitive Plasmodium falciparum D6 | F | 9.15 | pIC50 | 0.7 | nM | IC50 | Eur J Med Chem (2021) 226: 113865-113865 [PMID:34655985] |
| ChEMBL | Antiplasmodial activity against multidrug-resistant Plasmodium falciparum W2 infected in human erythrocytes after 72 hrs by ELISA | F | 7.9 | pEC50 | 12.5 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 2829-2843 [PMID:23587422] |
| Plasmodium malariae (target type: ORGANISM) [ChEMBL: CHEMBL613257] | ||||||||
| ChEMBL | Antimalarial activity against Plasmodium malariae trophozoite stage infected in red blood cells in presence of AB+ human serum by drug susceptibility assay | F | 7.42 | pIC50 | 38.4 | nM | IC50 | Antimicrob Agents Chemother (2011) 55: 197-202 [PMID:20937779] |
| ChEMBL | Antimalarial activity against Plasmodium malariae ring stage infected in red blood cells in presence of AB+ human serum by drug susceptibility assay | F | 7.54 | pIC50 | 29 | nM | IC50 | Antimicrob Agents Chemother (2011) 55: 197-202 [PMID:20937779] |
| Plasmodium vivax (target type: ORGANISM) [ChEMBL: CHEMBL613013] | ||||||||
| ChEMBL | Antimalarial activity against multidrug-resistant Plasmodium vivax clinical isolates assessed as reduction in parasite growth after 35 to 56 hrs by nucleic acid staining based flow cytometry | F | 7.34 | pIC50 | 45.2 | nM | IC50 | J Med Chem (2019) 62: 2485-2498 [PMID:30715882] |
| ChEMBL | Antimicrobial activity against Plasmodium vivax at the ring stage measured within 30 hrs by microscopy | F | 7.51 | pIC50 | 31.2 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 1040-1045 [PMID:18180357] |
| ChEMBL | Antimicrobial activity against Plasmodium vivax trophozoites measured after 30 hrs by microscopy | F | 7.54 | pIC50 | 29.1 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 1040-1045 [PMID:18180357] |
| ChEMBL | Antimalarial activity against Plasmodium vivax infected in human erythrocytes assessed as growth inhibition by microscopic analysis using giemsa staining | F | 7.61 | pIC50 | 24.8 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 5146-5150 [PMID:20876370] |
| ChEMBL | Antimicrobial activity against Plasmodium vivax trophozoites measured within 30 hrs by microscopy | F | 7.64 | pIC50 | 22.9 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 1040-1045 [PMID:18180357] |
| ChEMBL | Antimalarial activity against Plasmodium vivax trophozoites infected in human erythrocytes assessed as growth inhibition by microscopic analysis using giemsa staining | F | 7.66 | pIC50 | 21.7 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 5146-5150 [PMID:20876370] |
| ChEMBL | Antimalarial activity against Plasmodium vivax with >50% parasites at ring stage infected in human erythrocytes assessed as growth inhibition after 30 to 50 hrs by microscopic analysis using giemsa staining | F | 7.71 | pIC50 | 19.6 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 5146-5150 [PMID:20876370] |
| ChEMBL | Antimalarial activity against chloroquine-resistant Plasmodium vivax by Giemsa staining | F | 7.76 | pIC50 | 17.5 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 1094-1099 [PMID:19104023] |
| ChEMBL | Antimalarial activity against trophozoites stage of Plasmodium vivax assessed as parasites growth inhibition using giemsa staining after 24 to 56 hrs by microscopic analysis in presence of 20% human serum | F | 7.8 | pIC50 | 15.9 | nM | IC50 | Antimicrob Agents Chemother (2011) 55: 961-966 [PMID:21135175] |
| ChEMBL | Antimalarial activity against ring stage of Plasmodium vivax assessed as parasites growth inhibition using giemsa staining after 24 to 56 hrs by microscopic analysis in presence of 20% human serum | F | 7.81 | pIC50 | 15.5 | nM | IC50 | Antimicrob Agents Chemother (2011) 55: 961-966 [PMID:21135175] |
| ChEMBL | Antimicrobial activity against Plasmodium vivax at the ring stage measured after 30 hrs by microscopy | F | 7.84 | pIC50 | 14.6 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 1040-1045 [PMID:18180357] |
| ChEMBL | Antimalarial activity against Plasmodium vivax at the ring stage infected in human erythrocytes assessed as growth inhibition by microscopic analysis using giemsa staining | F | 7.85 | pIC50 | 14 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 5146-5150 [PMID:20876370] |
| ChEMBL | Antimalarial activity against Plasmodium vivax assessed as parasites growth inhibition using giemsa staining after 24 to 56 hrs by microscopic analysis in presence of 20% human serum | F | 7.88 | pIC50 | 13.2 | nM | IC50 | Antimicrob Agents Chemother (2011) 55: 961-966 [PMID:21135175] |
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]
