mefloquine [Ligand Id: 4252] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL416956 (Mefloquine, Lariam, Mefaquin, Ro-215998, WR-142490, GNF-Pf-5544)
  • glycine receptor α1 subunit/Glycine receptor subunit alpha-1 in Human [ChEMBL: CHEMBL5845] [GtoPdb: 423] [UniProtKB: P23415]
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  • Plasmodium falciparum (isolate K1 / Thailand) in Plasmodium falciparum K1 [ChEMBL: CHEMBL612856]
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  • Protein kinase Pfmrk in Plasmodium falciparum [ChEMBL: CHEMBL4090] [UniProtKB: P90584]
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  • A1 receptor in Human [GtoPdb: 18] [UniProtKB: P30542]
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  • A2A receptor in Human [GtoPdb: 19] [UniProtKB: P29274]
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  • Plasmodium falciparum purine nucleoside phosphorylase in Plasmodium falciparum [GtoPdb: 3077]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
glycine receptor α1 subunit/Glycine receptor subunit alpha-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5845] [GtoPdb: 423] [UniProtKB: P23415]
ChEMBL Potentiation of human GlyR-alpha1 expressed in Xenopus laevis oocytes assessed as induction of glycine-activated currents after 1 to 4 days by two-electrode voltage clamp assay B 5.6 pEC50 2500 nM EC50 J. Med. Chem. (2015) 58: 2958-2966 [PMID:25790278]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibitory concentration against potassium channel HERG B 5.25 pIC50 5623.41 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 2886-2890 [PMID:15911273]
ChEMBL Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique B 5.25 pIC50 5623.41 nM IC50 Bioorg. Med. Chem. (2008) 16: 6252-6260 [PMID:18448342]
ChEMBL Inhibition of human ERG B 5.26 pIC50 5495.41 nM IC50 Eur. J. Med. Chem. (2011) 46: 618-630 [PMID:21185626]
ChEMBL Inhibitory concentration against IKr potassium channel B 5.59 pIC50 2600 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 4771-4777 [PMID:15324906]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Inhibition of hydrogen peroxide-mediated haem detoxification in Plasmodium falciparum F 4.52 pIC50 30000 nM IC50 Bioorg. Med. Chem. Lett. (2001) 11: 2075-2077 [PMID:11514142]
ChEMBL Antimicrobial activity against Plasmodium falciparum F 5.3 pIC50 5000 nM IC50 Bioorg. Med. Chem. (2010) 18: 2225-2231 [PMID:20185316]
ChEMBL In vitro antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 Indochina F 6.71 pIC50 194.6 nM IC50 J. Med. Chem. (2003) 46: 4244-4258 [PMID:13678403]
ChEMBL Antimicrobial activity against Plasmodium falciparum harboring amplified Pfmdr1 gene F 6.74 pIC50 182 nM IC50 Antimicrob. Agents Chemother. (2008) 52: 2435-2441 [PMID:18443130]
ChEMBL In vitro antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 Sierra Leone F 6.77 pIC50 169.5 nM IC50 J. Med. Chem. (2003) 46: 4244-4258 [PMID:13678403]
ChEMBL Antimalarial activity against Plasmodium falciparum W2mef ring form by hoechst 33342-thiazole orange stain based flow cytometry assay F 6.83 pIC50 147 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 5452-5457 [PMID:19666223]
ChEMBL Antimalarial activity against Plasmodium falciparum W2mef by hypoxanthine uptake assay F 6.85 pIC50 142 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 5452-5457 [PMID:19666223]
ChEMBL Antimicrobial activity against Plasmodium falciparum at ring stage F 6.86 pIC50 137 nM IC50 Antimicrob. Agents Chemother. (2008) 52: 2435-2441 [PMID:18443130]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 assessed as inhibition of [3H]hypoxanthine incorporation after 24 hrs by microtiter plate scintillation counting F 7 pIC50 100 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 3863-3867 [PMID:20627564]
ChEMBL Antimalarial activity against Plasmodium falciparum W2mef assessed as DNA positive erythrocytes by hoechst 33342-thiazole orange stain based flow cytometry assay F 7.04 pIC50 91 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 5452-5457 [PMID:19666223]
ChEMBL Growth inhibition of chloroquine-sensitive Plasmodium falciparum D10 F 7.05 pIC50 90 nM IC50 Bioorg. Med. Chem. Lett. (2001) 11: 2075-2077 [PMID:11514142]
ChEMBL Antimalarial activity against multidrug-resistant Plasmodium falciparum isolate 208432 infected in human erythrocytes after 48 hrs by flow-cytometry F 7.05 pIC50 89.4 nM IC50 J. Med. Chem. (2010) 53: 3552-3557 [PMID:20349996]
ChEMBL Antimicrobial activity against Plasmodium falciparum harboring single copy of Pfmdr1 gene F 7.11 pIC50 77 nM IC50 Antimicrob. Agents Chemother. (2008) 52: 2435-2441 [PMID:18443130]
ChEMBL Antimalarial activity against Plasmodium falciparum W2mef trophozoite form by hoechst 33342-thiazole orange stain based flow cytometry assay F 7.13 pIC50 74 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 5452-5457 [PMID:19666223]
ChEMBL Antiplasmodial activity against chloroquine/mefloquine-resistant Plasmodium falciparum SRIV35 F 7.19 pIC50 65 nM IC50 Eur. J. Med. Chem. (2015) 94: 56-62 [PMID:25747499]
ChEMBL Inhibition of Plasmodium falciparum F32A F 7.21 pIC50 62 nM IC50 J. Med. Chem. (2000) 43: 2646-2654 [PMID:10893302]
ChEMBL Antimalarial activity against multidrug-resistant Plasmodium falciparum TM91C235 after 24 hrs by [3H]hypoxanthine uptake F 7.23 pIC50 59 nM IC50 J. Nat. Prod. (2002) 65: 614-615 [PMID:11975516]
ChEMBL Inhibitory activity against Plasmodium falciparum Dd2 in erythrocytes F 7.24 pIC50 57 nM IC50 Bioorg. Med. Chem. Lett. (2001) 11: 423-424 [PMID:11212126]
ChEMBL Antimalarial activity against morfloquine-resistant Plasmodium falciparum TM91C235 assessed as [3H]hypoxanthine incorporation F 7.25 pIC50 55.8 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 1320-1324 [PMID:19171802]
ChEMBL Antiplasmodial activity against chloroquine/mefloquine-resistant Plasmodium falciparum SKF58 F 7.26 pIC50 55 nM IC50 Eur. J. Med. Chem. (2015) 94: 56-62 [PMID:25747499]
ChEMBL Antimalarial activity against multidrug-resistant Plasmodium falciparum thailand TM91C235 assessed as [3H]-hypoxanthine incorporation by liquid scintillation counting analysis F 7.26 pIC50 55 nM IC50 Bioorg. Med. Chem. (2015) 23: 2176-2186 [PMID:25801154]
ChEMBL Antimalarial activity against multidrug-resistant Plasmodium falciparum TM91C235 F 7.32 pIC50 47.47 nM IC50 J. Med. Chem. (2008) 51: 6216-6219 [PMID:18774792]
ChEMBL Antimalarial activity against Plasmodium falciparum TM90C2A by hypoxanthine uptake F 7.34 pIC50 46 nM IC50 J. Med. Chem. (2008) 51: 3437-3448 [PMID:18494463]
ChEMBL Antimalarial activity against drug-resistant Plasmodium falciparum TM90C2A F 7.34 pIC50 46 nM IC50 Antimicrob. Agents Chemother. (2008) 52: 3467-3477 [PMID:18644969]
ChEMBL Antimalarial activity against Plasmodium falciparum W2mef schizont form by hoechst 33342-thiazole orange stain based flow cytometry assay F 7.36 pIC50 44 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 5452-5457 [PMID:19666223]
ChEMBL Antimalarial activity against Plasmodium falciparum TM91C235 by hypoxanthine uptake F 7.38 pIC50 42 nM IC50 J. Med. Chem. (2008) 51: 3437-3448 [PMID:18494463]
ChEMBL Antimalarial activity against drug-resistant Plasmodium falciparum TM91C235 F 7.38 pIC50 42 nM IC50 Antimicrob. Agents Chemother. (2008) 52: 3467-3477 [PMID:18644969]
ChEMBL Antimalarial activity against chloroquine-resistant and mefloquine-sensitive Plasmodium falciparum W2 infected in human O-positive erythrocytes assessed as inhibition of parasite growth by [3H]hypoxanthine incorporation assay F 7.4 pIC50 40 nM IC50 J. Nat. Prod. (2011) 74: 2269-2272 [PMID:21954931]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 F 7.4 pIC50 40 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 3088-3095 [PMID:23562058]
ChEMBL Inhibition of Plasmodium falciparum 3D7 F 7.4 pIC50 40 nM IC50 J. Med. Chem. (2000) 43: 2646-2654 [PMID:10893302]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 24 hrs by [3H]hypoxanthine incorporation assay F 7.41 pIC50 39 nM IC50 Bioorg. Med. Chem. (2010) 18: 6857-6864 [PMID:20719524]
ChEMBL Antimicrobial activity against Plasmodium falciparum harboring NDFCDY genotype after 72 hrs by SYBR green I assay F 7.41 pIC50 39 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2042-2051 [PMID:19258269]
ChEMBL Antimalarial activity against multidrug-resistant Plasmodium falciparum TM91C235 assessed as inhibition of [3H]hypoxanthine uptake F 7.43 pIC50 37.4 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 786-789 [PMID:21168330]
ChEMBL Antimalarial activity against Plasmodium falciparum C235 F 7.44 pIC50 36.5 nM IC50 J. Med. Chem. (2011) 54: 1157-1169 [PMID:21265542]
ChEMBL Antimalarial activity against Plasmodium falciparum D6 after 24 hrs by [3H]hypoxanthine uptake F 7.44 pIC50 36 nM IC50 J. Nat. Prod. (2002) 65: 614-615 [PMID:11975516]
ChEMBL Inhibition of Plasmodium falciparum FCR3 F 7.44 pIC50 36 nM IC50 J. Med. Chem. (2000) 43: 2646-2654 [PMID:10893302]
ChEMBL Antiplasmodial activity against Plasmodium falciparum harboring K1 allele group of msp1, 3D7 allele group of msp2 gene and 94 bp of 7A11, 196bp of C4M79 and 336bp of C4M69 locus measured on day 23 by [3H]hypoxanthine incorporation assay F 7.47 pIC50 34.1 nM IC50 Antimicrob. Agents Chemother. (2008) 52: 2283-2284 [PMID:18411319]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 by SYBR green I-based assay F 7.47 pIC50 34 nM IC50 J. Nat. Prod. (2012) 75: 1299-1304 [PMID:22709138]
ChEMBL Antimalarial activity against multidrug-resistant Plasmodium falciparum TM91C235 F 7.48 pIC50 33.46 nM IC50 J. Med. Chem. (2008) 51: 4388-4391 [PMID:18637666]
ChEMBL Inhibitory concentration against Plasmodium falciparum D6 (Sierra Leone) F 7.48 pIC50 33.38 nM IC50 J. Med. Chem. (1988) 31: 645-650 [PMID:3279208]
ChEMBL Inhibition of Plasmodium falciparum W2 F 7.52 pIC50 30 nM IC50 J. Med. Chem. (2000) 43: 2646-2654 [PMID:10893302]
ChEMBL Growth inhibition of chloroquine-resistant Plasmodium falciparum KI F 7.52 pIC50 30 nM IC50 Bioorg. Med. Chem. Lett. (2001) 11: 2075-2077 [PMID:11514142]
ChEMBL Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D6 by SYBR green I-based assay F 7.54 pIC50 29 nM IC50 J. Nat. Prod. (2012) 75: 1299-1304 [PMID:22709138]
ChEMBL In vitro inhibitory activity against chloroquine-sensitive Plasmodium falciparum African D6 F 7.55 pIC50 28.29 nM IC50 J. Med. Chem. (2002) 45: 3331-3336 [PMID:12139444]
ChEMBL Antimicrobial activity against Plasmodium falciparum harboring NDFCDD genotype after 72 hrs by SYBR green I assay F 7.55 pIC50 28 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2042-2051 [PMID:19258269]
ChEMBL Growth inhibition of Plasmodium falciparum Dd2 ring stage infected erythrocytes after 72 hrs by DAPI fluorimetry F 7.59 pIC50 25.99 nM IC50 Antimicrob. Agents Chemother. (2007) 51: 716-723 [PMID:17116676]
ChEMBL Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum F32-Tanzania by [3H]hypoxanthine uptake F 7.64 pIC50 23 nM IC50 J. Nat. Prod. (2001) 64: 12-16 [PMID:11170658]
ChEMBL Antimalarial activity against multidrug-resistant Plasmodium falciparum TM91C235 F 7.65 pIC50 22.45 nM IC50 J. Med. Chem. (2008) 51: 2261-2266 [PMID:18330976]
ChEMBL Antimicrobial activity against Plasmodium falciparum harboring NGFSDD genotype after 72 hrs by SYBR green I assay F 7.68 pIC50 21 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2042-2051 [PMID:19258269]
ChEMBL Antimalarial activity against mefloquine-resistant, chloroquine-sensitive Plasmodium falciparum D6 assessed as inhibition of [3H]hypoxanthine uptake F 7.7 pIC50 20.1 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 786-789 [PMID:21168330]
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 assessed as [3H]hypoxanthine incorporation F 7.7 pIC50 19.9 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 1320-1324 [PMID:19171802]
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 7.7 pIC50 19.9 nM IC50 Antimicrob. Agents Chemother. (2011) 55: 961-966 [PMID:21135175]
ChEMBL Antimalarial activity against Plasmodium falciparum Dd2 containing attB site inserted in parasite genome and expressing parental ATP4 after 72 hrs by SYBR green based fluorescence assay F 7.7 pIC50 19.85 nM IC50 Science (2010) 329: 1175-1180 [PMID:20813948]
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 F 7.72 pIC50 19.01 nM IC50 J. Med. Chem. (2008) 51: 6216-6219 [PMID:18774792]
ChEMBL Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D6 infected human erythrocytes as [3H]hypoxanthine uptake after 24 hrs F 7.74 pIC50 18.12 nM IC50 J. Nat. Prod. (1999) 62: 59-66 [PMID:9917283]
ChEMBL Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D10 after 48 hrs by lactate dehydrogenase assay F 7.74 pIC50 18 nM IC50 Bioorg. Med. Chem. (2012) 20: 893-902 [PMID:22196513]
ChEMBL Inhibition of Plasmodium falciparum GP1 F 7.77 pIC50 17 nM IC50 J. Med. Chem. (2000) 43: 2646-2654 [PMID:10893302]
ChEMBL Inhibitory concentration against Plasmodium falciparum D6 infected erythrocytes F 7.77 pIC50 17 nM IC50 J. Med. Chem. (1994) 37: 1486-1494 [PMID:8182707]
ChEMBL Antimalarial activity against Plasmodium falciparum TM91C235 F 7.78 pIC50 16.44 nM IC50 J. Med. Chem. (2007) 50: 5118-5127 [PMID:17887664]
ChEMBL Antimalarial activity against mefloquine, chloroquine and quinine-resistant Plasmodium falciparum TM91C235 F 7.78 pIC50 16.44 nM IC50 Bioorg. Med. Chem. (2008) 16: 7039-7045 [PMID:18550377]
ChEMBL Antimalarial activity against Plasmodium falciparum TM91C235 F 7.79 pIC50 16.4 nM IC50 J. Med. Chem. (2006) 49: 3790-3799 [PMID:16789736]
ChEMBL Antimalarial activity against Plasmodium falciparum D6 F 7.8 pIC50 15.7 nM IC50 J. Med. Chem. (2011) 54: 1157-1169 [PMID:21265542]
ChEMBL Antimalarial activity against Plasmodium falciparum isolates assessed as parasite growth inhibition after 72 hrs by ELISA based histidine-rich protein 2 in vitro drug susceptibility assay F 7.84 pIC50 14.38 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 4040-4042 [PMID:19596882]
ChEMBL Antimalarial activity against Plasmodium falciparum Dd2 containing attB site inserted in parasite genome and using EF1-alpha promoter driven expressing ATP4 I398F/P990R mutant after 72 hrs by SYBR green based fluorescence assay F 7.85 pIC50 14.07 nM IC50 Science (2010) 329: 1175-1180 [PMID:20813948]
ChEMBL Antimalarial activity against Plasmodium falciparum IMT K4 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter F 7.85 pIC50 14 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2248-2252 [PMID:19307369]
ChEMBL Antimalarial activity against Plasmodium falciparum 3D7 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter F 7.85 pIC50 14 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2248-2252 [PMID:19307369]
ChEMBL Antimalarial activity against Plasmodium falciparum W2 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter F 7.85 pIC50 14 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2248-2252 [PMID:19307369]
ChEMBL Antimalarial activity against Plasmodium falciparum D6 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter F 7.85 pIC50 14 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2248-2252 [PMID:19307369]
ChEMBL Antimalarial activity against Plasmodium falciparum FCM29 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter F 7.85 pIC50 14 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2248-2252 [PMID:19307369]
ChEMBL Antimalarial activity against Plasmodium falciparum FCR3 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter F 7.85 pIC50 14 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2248-2252 [PMID:19307369]
ChEMBL Antimalarial activity against Plasmodium falciparum PA assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter F 7.85 pIC50 14 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2248-2252 [PMID:19307369]
ChEMBL Antimalarial activity against Plasmodium falciparum HB3 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter F 7.85 pIC50 14 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2248-2252 [PMID:19307369]
ChEMBL Antimalarial activity against Plasmodium falciparum 106/1 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter F 7.85 pIC50 14 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2248-2252 [PMID:19307369]
ChEMBL Antimalarial activity against Plasmodium falciparum IMT Bres assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter F 7.85 pIC50 14 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2248-2252 [PMID:19307369]
ChEMBL Antimalarial activity against Plasmodium falciparum IMT Guy assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter F 7.85 pIC50 14 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2248-2252 [PMID:19307369]
ChEMBL Antimalarial activity against Plasmodium falciparum IMT A4 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter F 7.85 pIC50 14 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2248-2252 [PMID:19307369]
ChEMBL Antimalarial activity against Plasmodium falciparum IMT 31 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter F 7.85 pIC50 14 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2248-2252 [PMID:19307369]
ChEMBL Antimalarial activity against Plasmodium falciparum IMT 8425 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter F 7.85 pIC50 14 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2248-2252 [PMID:19307369]
ChEMBL Antimalarial activity against Plasmodium falciparum IMT 9881 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter F 7.85 pIC50 14 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2248-2252 [PMID:19307369]
ChEMBL Antimalarial activity against Plasmodium falciparum IMT 10336 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter F 7.85 pIC50 14 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2248-2252 [PMID:19307369]
ChEMBL Antimalarial activity against Plasmodium falciparum IMT 10500 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter F 7.85 pIC50 14 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2248-2252 [PMID:19307369]
ChEMBL Antimalarial activity against Plasmodium falciparum IMT 16332 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter F 7.85 pIC50 14 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2248-2252 [PMID:19307369]
ChEMBL Antimalarial activity against Plasmodium falciparum IMT K14 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter F 7.85 pIC50 14 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2248-2252 [PMID:19307369]
ChEMBL Antimalarial activity against Plasmodium falciparum IMT K2 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter F 7.85 pIC50 14 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2248-2252 [PMID:19307369]
ChEMBL Antimalarial activity against Plasmodium falciparum IMT L1 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter F 7.85 pIC50 14 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2248-2252 [PMID:19307369]
ChEMBL Antimalarial activity against Plasmodium falciparum IMT Vol assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter F 7.85 pIC50 14 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2248-2252 [PMID:19307369]
ChEMBL Antimalarial activity against Plasmodium falciparum Dd2 containing attB site inserted in parasite genome and using EF1-alpha promoter driven expressing wild type ATP4 after 72 hrs by SYBR green based fluorescence assay F 7.88 pIC50 13.15 nM IC50 Science (2010) 329: 1175-1180 [PMID:20813948]
ChEMBL Antimalarial activity against Plasmodium falciparum NF54 F 7.89 pIC50 13 nM IC50 J. Med. Chem. (2011) 54: 4581-4589 [PMID:21644541]
ChEMBL Antimalarial activity against Plasmodium falciparum Dd2 containing attB site inserted in parasite genome and using CAM promoter driven expressing ATP4 I398F/P990R mutant after 72 hrs by SYBR green based fluorescence assay F 7.89 pIC50 12.87 nM IC50 Science (2010) 329: 1175-1180 [PMID:20813948]
ChEMBL Antimalarial activity against Plasmodium falciparum Dd2 containing attB site inserted in parasite genome and using EF1-alpha promoter driven expressing ATP4 D1247Y mutant after 72 hrs by SYBR green based fluorescence assay F 7.9 pIC50 12.5 nM IC50 Science (2010) 329: 1175-1180 [PMID:20813948]
ChEMBL Antimicrobial activity against Plasmodium falciparum 3D7 by DAPI growth inhibition assay F 7.91 pIC50 12.3 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2564-2568 [PMID:19307367]
ChEMBL Growth inhibition of Plasmodium falciparum 3D7 ring stage in infected erythrocytes after 72 hrs in DAPI fluorimetry F 7.91 pIC50 12.29 nM IC50 Antimicrob. Agents Chemother. (2007) 51: 716-723 [PMID:17116676]
ChEMBL Antimalarial activity against Plasmodium falciparum 3D7 infected in human erythrocytes assessed as decrease in parasitemia after 72 hrs F 7.92 pIC50 12 nM IC50 J. Med. Chem. (2011) 54: 5116-5130 [PMID:21644570]
ChEMBL Antimalarial activity against Plasmodium falciparum HB3 F 7.92 pIC50 12 nM IC50 J. Med. Chem. (2011) 54: 4581-4589 [PMID:21644541]
ChEMBL Antimalarial activity against chloroquine,mefloquine-sensitive Plasmodium falciparum D6 F 7.95 pIC50 11.25 nM IC50 J. Med. Chem. (2008) 51: 4388-4391 [PMID:18637666]
ChEMBL Antimalarial activity against Plasmodium falciparum Dd2 containing attB site inserted in parasite genome and using CAM promoter driven expressing ATP4 D1247Y mutant after 72 hrs by SYBR green based fluorescence assay F 7.96 pIC50 11.04 nM IC50 Science (2010) 329: 1175-1180 [PMID:20813948]
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as inhibition of [3H]hypoxanthine incorporation F 7.96 pIC50 11 nM IC50 Antimicrob. Agents Chemother. (2011) 55: 961-966 [PMID:21135175]
ChEMBL Antiplasmodial activity against multidrug-resistant Plasmodium falciparum VS/1 by [3H]hypoxanthine incorporation assay F 7.96 pIC50 11 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 3131-3134 [PMID:19364853]
ChEMBL Antimalarial activity against mefloquine-resistant Plasmodium falciparum W2 after 48 hrs by LDH assay F 7.96 pIC50 11 nM IC50 J. Med. Chem. (2011) 54: 4581-4589 [PMID:21644541]
ChEMBL Antimalarial activity against drug-resistant Plasmodium falciparum D6 infected in Aotus lemurinus lemurinus monkey F 7.96 pIC50 11 nM IC50 Antimicrob. Agents Chemother. (2008) 52: 3467-3477 [PMID:18644969]
ChEMBL Antimalarial activity against Plasmodium falciparum D6 by hypoxanthine uptake F 7.96 pIC50 11 nM IC50 J. Med. Chem. (2008) 51: 3437-3448 [PMID:18494463]
ChEMBL Antimalarial activity against Plasmodium falciparum D6 F 7.98 pIC50 10.52 nM IC50 J. Med. Chem. (2007) 50: 5118-5127 [PMID:17887664]
ChEMBL Antimalarial activity against chloroquine and pyrimethamine-sensitive Plasmodium falciparum D6 F 7.98 pIC50 10.52 nM IC50 Bioorg. Med. Chem. (2008) 16: 7039-7045 [PMID:18550377]
ChEMBL Antimalarial activity against Plasmodium falciparum D6 F 7.98 pIC50 10.5 nM IC50 J. Med. Chem. (2006) 49: 3790-3799 [PMID:16789736]
ChEMBL Growth inhibition of Plasmodium falciparum HB3 ring stage in infected erythrocytes after 72 hrs in DAPI fluorimetry F 8.02 pIC50 9.63 nM IC50 Antimicrob. Agents Chemother. (2007) 51: 716-723 [PMID:17116676]
ChEMBL Antimalarial activity against Plasmodium falciparum trophozoites infected in human erythrocytes assessed as growth inhibition by microscopic analysis using giemsa staining F 8.07 pIC50 8.5 nM IC50 Antimicrob. Agents Chemother. (2010) 54: 5146-5150 [PMID:20876370]
ChEMBL Antimalarial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green based fluorescence assay F 8.08 pIC50 8.4 nM IC50 Science (2010) 329: 1175-1180 [PMID:20813948]
ChEMBL Antimalarial activity against Plasmodium falciparum assessed as [35S]Met/Cys incorporation by SYBR green based fluorescence assay F 8.1 pIC50 8 nM IC50 Science (2010) 329: 1175-1180 [PMID:20813948]
ChEMBL Antimalarial activity against Plasmodium falciparum W2 infected in human erythrocytes assessed as decrease in parasitemia after 72 hrs F 8.1 pIC50 8 nM IC50 J. Med. Chem. (2011) 54: 5116-5130 [PMID:21644570]
ChEMBL Inhibition of Plasmodium falciparum FCM29 F 8.1 pIC50 8 nM IC50 J. Med. Chem. (2000) 43: 2646-2654 [PMID:10893302]
ChEMBL Inhibitory concentration against Plasmodium falciparum W2 infected erythrocytes F 8.1 pIC50 8 nM IC50 J. Med. Chem. (1994) 37: 1486-1494 [PMID:8182707]
ChEMBL Antimalarial activity against NITD609-resistant Plasmodium falciparum Dd2 Clone3 bearing P-type ATPase4 D1247Y mutations after 72 hrs by SYBR green based fluorescence assay F 8.1 pIC50 8 nM IC50 Science (2010) 329: 1175-1180 [PMID:20813948]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 infected human erythrocytes as [3H]hypoxanthine uptake after 24 hrs F 8.11 pIC50 7.78 nM IC50 J. Nat. Prod. (1999) 62: 59-66 [PMID:9917283]
ChEMBL Antimalarial activity against Plasmodium falciparum D6 F 8.13 pIC50 7.34 nM IC50 J. Med. Chem. (2008) 51: 2261-2266 [PMID:18330976]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 assessed as [3H]hypoxanthine incorporation F 8.14 pIC50 7.2 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 1320-1324 [PMID:19171802]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum indochina W2 assessed as [3H]-hypoxanthine incorporation by liquid scintillation counting analysis F 8.15 pIC50 7 nM IC50 Bioorg. Med. Chem. (2015) 23: 2176-2186 [PMID:25801154]
ChEMBL Antimalarial activity against NITD609-resistant Plasmodium falciparum Dd2 Clone2 bearing P-type ATPase4 T418N and P990R mutations after 72 hrs by SYBR green based fluorescence assay F 8.15 pIC50 7 nM IC50 Science (2010) 329: 1175-1180 [PMID:20813948]
ChEMBL In vitro sensitivity for Plasmodium falciparum FcB1R F 8.16 pIC50 6.9 nM IC50 J. Med. Chem. (2000) 43: 2646-2654 [PMID:10893302]
ChEMBL Antimalarial activity against NITD609-resistant Plasmodium falciparum Dd2 Clone1 bearing P-type ATPase4 I398F and P990R mutations after 72 hrs by SYBR green based fluorescence assay F 8.17 pIC50 6.7 nM IC50 Science (2010) 329: 1175-1180 [PMID:20813948]
ChEMBL Antimalarial activity against Plasmodium falciparum assessed as parasite growth inhibition after 48 hrs by [3H]hypoxanthin incorporation assay F 8.17 pIC50 6.7 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 4588-4597 [PMID:19704124]
ChEMBL Antimicrobial activity against Plasmodium falciparum at the ring stage by microscopy F 8.19 pIC50 6.4 nM IC50 Antimicrob. Agents Chemother. (2008) 52: 1040-1045 [PMID:18180357]
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 8.19 pIC50 6.4 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 8.2 pIC50 6.3 nM IC50 Antimicrob. Agents Chemother. (2011) 55: 961-966 [PMID:21135175]
ChEMBL Antimalarial activity against chloroquine-resistant, mefloquine-sensitive Plasmodium falciparum W2 assessed as inhibition of [3H]hypoxanthine uptake F 8.22 pIC50 6.01 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 786-789 [PMID:21168330]
ChEMBL Antimalarial activity against drug-resistant Plasmodium falciparum W2 F 8.23 pIC50 5.9 nM IC50 Antimicrob. Agents Chemother. (2008) 52: 3467-3477 [PMID:18644969]
ChEMBL Antimalarial activity against Plasmodium falciparum W2 by hypoxanthine uptake F 8.23 pIC50 5.9 nM IC50 J. Med. Chem. (2008) 51: 3437-3448 [PMID:18494463]
ChEMBL Antimalarial activity against Plasmodium falciparum D6 in MSF assay F 8.23 pIC50 5.9 nM IC50 Bioorg. Med. Chem. (2008) 16: 1174-1183 [PMID:18023189]
ChEMBL Inhibitory concentration against Plasmodium falciparum W2 Indochina F 8.24 pIC50 5.75 nM IC50 J. Med. Chem. (1988) 31: 645-650 [PMID:3279208]
ChEMBL Antimalarial activity against chloroquine-resistant, mefloquine-susceptible Plasmodium falciparum W2 F 8.27 pIC50 5.35