mefloquine [Ligand Id: 4252] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL416956 (GNF-Pf-5544, Lariam, Mefaquin, Mefloquine, NSC-758233, RO 21-5998, RO-215998, WR 142,490) |
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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 | nM | IC50 | J Med Chem (2008) 51: 6216-6219 [PMID:18774792] |
| ChEMBL | In vitro inhibitory activity against chloroquine-resistant Plasmodium falciparum W2 Indochina | F | 8.3 | pIC50 | 5.02 | nM | IC50 | J Med Chem (2002) 45: 3331-3336 [PMID:12139444] |
| ChEMBL | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 | F | 8.3 | pIC50 | 4.96 | nM | IC50 | J Med Chem (2008) 51: 4388-4391 [PMID:18637666] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum W2 | F | 8.31 | pIC50 | 4.93 | nM | IC50 | J Med Chem (2011) 54: 1157-1169 [PMID:21265542] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum infected in human erythrocytes assessed as growth inhibition by microscopic analysis using giemsa staining | F | 8.31 | pIC50 | 4.9 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 5146-5150 [PMID:20876370] |
| 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 | 8.31 | pIC50 | 4.9 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 5146-5150 [PMID:20876370] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum W2 | F | 8.31 | pIC50 | 4.89 | nM | IC50 | J Med Chem (2008) 51: 2261-2266 [PMID:18330976] |
| ChEMBL | Antiparasitic activity against chloroquine-sensitive Plasmodium falciparum by [3H]hypoxanthine incorporation | F | 8.31 | pIC50 | 4.85 | nM | IC50 | J Med Chem (2008) 51: 1260-1277 [PMID:18260613] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum W2 after 24 hrs by [3H]hypoxanthine uptake | F | 8.32 | pIC50 | 4.8 | nM | IC50 | J Nat Prod (2002) 65: 614-615 [PMID:11975516] |
| ChEMBL | Antimicrobial activity against Plasmodium falciparum trophozoites by microscopy treated during ring stage | F | 8.34 | pIC50 | 4.6 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 1040-1045 [PMID:18180357] |
| ChEMBL | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human erythrocytes after 48 hrs by flow-cytometry | F | 8.49 | pIC50 | 3.2 | nM | IC50 | J Med Chem (2010) 53: 3552-3557 [PMID:20349996] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum W2 | F | 8.51 | pIC50 | 3.1 | nM | IC50 | J Med Chem (2006) 49: 3790-3799 [PMID:16789736] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum W2 | F | 8.51 | pIC50 | 3.09 | nM | IC50 | J Med Chem (2007) 50: 5118-5127 [PMID:17887664] |
| ChEMBL | Antimalarial activity against chloroquine and pyrimethamine-resistant Plasmodium falciparum W2 | F | 8.51 | pIC50 | 3.09 | nM | IC50 | Bioorg Med Chem (2008) 16: 7039-7045 [PMID:18550377] |
| ChEMBL | Antimalarial activity against chloroquine-resistant, mefloquine-sensitive Plasmodium falciparum RCS | F | 8.63 | pIC50 | 2.33 | nM | IC50 | Bioorg Med Chem (2008) 16: 7039-7045 [PMID:18550377] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum 3D7 infected in human erythrocytes after 48 hrs by flow-cytometry | F | 8.68 | pIC50 | 2.1 | nM | IC50 | J Med Chem (2010) 53: 3552-3557 [PMID:20349996] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 infected in RBCs by firefly luciferase reporter gene assay | F | 8.68 | pIC50 | 2.1 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3597-3604 [PMID:20547797] |
| ChEMBL | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum PFB Brazil by [3H]hypoxanthine uptake | F | 8.7 | pIC50 | 2 | nM | IC50 | J Nat Prod (2001) 64: 12-16 [PMID:11170658] |
| ChEMBL | Intrinsic equimolar activity against Plasmodium falciparum W2 Indochina relative to QHS | F | 8.95 | pIC50 | 1.11 | nM | IC50 | J Med Chem (1988) 31: 645-650 [PMID:3279208] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum W2 in MSF assay | F | 9.15 | pIC50 | 0.7 | nM | IC50 | Bioorg Med Chem (2008) 16: 1174-1183 [PMID:18023189] |
| ChEMBL | Intrinsic equimolar activity against Plasmodium falciparum D6 (Sierra Leone) relative to QHS | F | 9.51 | pIC50 | 0.31 | nM | IC50 | J Med Chem (1988) 31: 645-650 [PMID:3279208] |
| ChEMBL | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected human erythrocytes after 72 hrs by MSF assay | F | 6.8 | pEC50 | 160 | nM | EC50 | Bioorg Med Chem (2010) 18: 2756-2766 [PMID:20206533] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum D10 | F | 7.19 | pEC50 | 64 | nM | EC50 | Antimicrob Agents Chemother (2007) 51: 759-762 [PMID:17088482] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum Dd2 | F | 7.22 | pEC50 | 60 | nM | EC50 | Antimicrob Agents Chemother (2007) 51: 759-762 [PMID:17088482] |
| ChEMBL | Antimalarial activity against multidrug-resistant and atovaquone-sensitive Plasmodium falciparum TM91C235 | F | 7.57 | pEC50 | 27 | nM | EC50 | J Med Chem (2013) 56: 2975-2990 [PMID:23517371] |
| ChEMBL | NOVARTIS: Inhibition of Plasmodium falciparum 3D7 (drug-susceptible) proliferation in erythrocyte-based infection assay | F | 7.61 | pEC50 | 24.82 | nM | EC50 | Proc Natl Acad Sci U S A (2008) 105: 9059-9064 [PMID:18579783] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum FAC8 | F | 7.64 | pEC50 | 23 | nM | EC50 | Antimicrob Agents Chemother (2007) 51: 759-762 [PMID:17088482] |
| ChEMBL | Antimalarial activity Plasmodium falciparum 3D7 | F | 7.7 | pEC50 | 20 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 4027-4031 [PMID:20610151] |
| ChEMBL | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 | F | 7.96 | pEC50 | 11 | nM | EC50 | J Med Chem (2013) 56: 2975-2990 [PMID:23517371] |
| ChEMBL | Antimalarial activity against atovaquone-resistant Plasmodium falciparum TM90C2B | F | 8.01 | pEC50 | 9.8 | nM | EC50 | J Med Chem (2013) 56: 2975-2990 [PMID:23517371] |
| ChEMBL | NOVARTIS: Inhibition of Plasmodium falciparum W2 (drug-resistant) proliferation in erythrocyte-based infection assay | F | 8.09 | pEC50 | 8.14 | nM | EC50 | Proc Natl Acad Sci U S A (2008) 105: 9059-9064 [PMID:18579783] |
| ChEMBL | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 | F | 8.31 | pEC50 | 4.9 | nM | EC50 | J Med Chem (2013) 56: 2975-2990 [PMID:23517371] |
| Plasmodium falciparum 3D7 (target type: ORGANISM) [ChEMBL: CHEMBL2366922] | ||||||||
| ChEMBL | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 | F | 7.7 | pIC50 | 20 | nM | IC50 | Eur J Med Chem (2015) 94: 56-62 [PMID:25747499] |
| Plasmodium falciparum D6 (target type: ORGANISM) [ChEMBL: CHEMBL2367107] | ||||||||
| ChEMBL | Antimalarial activity against chloroquine-susceptible Plasmodium falciparum african D6 assessed as [3H]-hypoxanthine incorporation by liquid scintillation counting analysis | F | 7.64 | pIC50 | 23 | nM | IC50 | Bioorg Med Chem (2015) 23: 2176-2186 [PMID:25801154] |
| Plasmodium falciparum (isolate K1 / Thailand) in Plasmodium falciparum K1 (target type: ORGANISM) [ChEMBL: CHEMBL612856] | ||||||||
| ChEMBL | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 | F | 7.85 | pIC50 | 14 | nM | IC50 | Eur J Med Chem (2015) 94: 56-62 [PMID:25747499] |
| ChEMBL | Inhibition of Plasmodium falciparum K1 | F | 7.92 | pIC50 | 12 | nM | IC50 | J Med Chem (2000) 43: 2646-2654 [PMID:10893302] |
| ChEMBL | Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 assessed as inhibition of [3H]hypoxanthine incorporation | F | 8.1 | pIC50 | 8 | nM | IC50 | Antimicrob Agents Chemother (2011) 55: 961-966 [PMID:21135175] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum K1 | F | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (2011) 54: 4581-4589 [PMID:21644541] |
| ChEMBL | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 after 48 hrs by lactate dehydrogenase assay | F | 8.1 | pIC50 | 8 | nM | IC50 | Bioorg Med Chem (2012) 20: 893-902 [PMID:22196513] |
| ChEMBL | Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 infected human erythrocytes after 72 hrs by MSF assay | F | 7.4 | pEC50 | 40 | nM | EC50 | Bioorg Med Chem (2010) 18: 2756-2766 [PMID:20206533] |
| 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 | 7.33 | pIC50 | 46.9 | 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 | 7.43 | pIC50 | 36.8 | nM | IC50 | Antimicrob Agents Chemother (2011) 55: 197-202 [PMID:20937779] |
| Plasmodium vivax (target type: ORGANISM) [ChEMBL: CHEMBL613013] | ||||||||
| ChEMBL | Antimicrobial activity against Plasmodium vivax harboring amplified Pvmdr1 gene | F | 6.75 | pIC50 | 176 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 2435-2441 [PMID:18443130] |
| ChEMBL | Antimicrobial activity against Plasmodium vivax at trophozoite stage | F | 7.16 | pIC50 | 69 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 2435-2441 [PMID:18443130] |
| ChEMBL | Antimicrobial activity against Plasmodium vivax harboring single copy of Pvmdr1 gene | F | 7.37 | pIC50 | 43 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 2435-2441 [PMID:18443130] |
| ChEMBL | Antimicrobial activity against Plasmodium vivax at the ring stage measured within 30 hrs by microscopy | F | 7.65 | pIC50 | 22.2 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 1040-1045 [PMID:18180357] |
| ChEMBL | Antimicrobial activity against Plasmodium vivax trophozoites measured within 30 hrs by microscopy | F | 7.76 | pIC50 | 17.4 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 1040-1045 [PMID:18180357] |
| ChEMBL | Antimicrobial activity against Plasmodium vivax trophozoites by microscopy | F | 7.77 | pIC50 | 17 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 1040-1045 [PMID:18180357] |
| ChEMBL | Antimicrobial activity against Plasmodium vivax at the trophozoites by microscopy treated during ring stage | F | 7.9 | pIC50 | 12.5 | 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 | 7.91 | pIC50 | 12.4 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 5146-5150 [PMID:20876370] |
| ChEMBL | Antimalarial activity against Plasmodium vivax infected in human erythrocytes assessed as growth inhibition by microscopic analysis using giemsa staining | F | 7.92 | pIC50 | 12.1 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 5146-5150 [PMID:20876370] |
| 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 | 7.99 | pIC50 | 10.2 | 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 | 8.04 | pIC50 | 9.2 | nM | IC50 | Antimicrob Agents Chemother (2011) 55: 961-966 [PMID:21135175] |
| ChEMBL | Antimalarial activity against chloroquine-resistant Plasmodium vivax by Giemsa staining | F | 8.09 | pIC50 | 8.2 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 1094-1099 [PMID:19104023] |
| 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 | 8.1 | pIC50 | 8 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 5146-5150 [PMID:20876370] |
| 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 | 8.1 | pIC50 | 7.9 | 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 | 8.11 | pIC50 | 7.7 | nM | IC50 | Antimicrob Agents Chemother (2011) 55: 961-966 [PMID:21135175] |
| ChEMBL | Antimicrobial activity against Plasmodium vivax trophozoites measured after 30 hrs by microscopy | F | 8.14 | pIC50 | 7.27 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 1040-1045 [PMID:18180357] |
| ChEMBL | Antimicrobial activity against Plasmodium vivax at the ring stage measured after 30 hrs by microscopy | F | 8.14 | pIC50 | 7.26 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 1040-1045 [PMID:18180357] |
| ChEMBL | Antimicrobial activity against Plasmodium vivax at the ring stage by microscopy | F | 8.19 | pIC50 | 6.39 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 1040-1045 [PMID:18180357] |
| Protein kinase Pfmrk in Plasmodium falciparum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4090] [UniProtKB: P90584] | ||||||||
| ChEMBL | Inhibition of Plasmodium falciparum cyclin-dependent kinase | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (2004) 47: 5418-5426 [PMID:15481979] |
| A1 receptor in Human [GtoPdb: 18] [UniProtKB: P30542] | ||||||||
| GtoPdb | Binding affinity determined by displacement of [3H]-DPCPX from human A1 receptors by increasing concentrations of racemic mefloquine. | - | 6.17 | pKi | 675 | nM | Ki | Neurology (2003) 61: S101-6 [PMID:14663021] |
| A2A receptor in Human [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
| GtoPdb | Binding affinity determined by displacement of [3H]-CGS21680 from human A2A receptors by increasing concentrations of racemic mefloquine. | - | 6.98 | pKi | 104 | nM | Ki | Neurology (2003) 61: S101-6 [PMID:14663021] |
| Plasmodium falciparum purine nucleoside phosphorylase in Plasmodium falciparum [GtoPdb: 3077] | ||||||||
| GtoPdb | - | - | 5.23 | pKi | 5900 | nM | Ki | Sci Transl Med (2019) 11: [PMID:30602534] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
