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) |
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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 | |||