ganaplacide: antimalarial [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
ID Source | ID |
---|---|
PubMed CID | 49856296 |
CHEMBL ID | 2058833 |
SCHEMBL ID | 1047381 |
MeSH ID | M000608344 |
Synonym |
---|
bdbm50388532 |
ganaplacide |
gnf-156 |
kaf 156 |
gnf 156 |
CHEMBL2058833 , |
kaf-156 |
kaf156 |
2-amino-1-[3-(4-fluoroanilino)-2-(4-fluorophenyl)-8,8-dimethyl-5,6-dihydroimidazo[1,2-a]pyrazin-7-yl]ethanone |
SCHEMBL1047381 |
1261113-96-5 |
ganaplacide [who-dd] |
2-amino-1-(2-(4-fluorophenyl)-3-((4-fluorophenyl)amino)-5,6-dihydro-8,8-dimethylimidazo(1,2-a)pyrazin-7(8h)-yl)ethanone |
ganaplacide [inn] |
ethanone, 2-amino-1-(2-(4-fluorophenyl)-3-((4-fluorophenyl)amino)-5,6-dihydro-8,8-dimethylimidazo(1,2-a)pyrazin-7(8h)-yl)- |
85VMN9JU7A , |
AKOS030629999 |
unii-85vmn9ju7a |
H11185 |
2-amino-1-(2-(4-fluorophenyl)-3-((4-fluorophenyl)amino)-8,8-dimethyl-5,6-dihydroimidazo[1,2-a]pyrazin-7(8h)-yl)ethanone |
kaf 156; kaf156; gnf-156; gnf156; gnf 156; ganaplacide |
BCP21186 |
Q28209255 |
mfcd28502124 |
2-amino-1-[2-(4-fluorophenyl)-3-[(4-fluorophenyl)amino]-5,6-dihydro-8,8-dimethylimidazo[1,2-a]pyrazin-7(8h)-yl]ethanone |
AS-49356 |
gtpl9946 |
gnf156 |
SB17068 |
A856033 |
TQR0232 |
EX-A6670 |
DTXSID701105307 |
HY-108024 |
CS-0027183 |
KAF156 is a novel antimalarial drug that is active against both liver- and blood-stage Plasmodium parasites, including drug-resistant strains. KAF156 has activity against pre-erythrocytic liver stages, asexual and sexual blood stages.
Excerpt | Reference | Relevance |
---|---|---|
"KAF156 is a novel antimalarial drug that is active against both liver- and blood-stage Plasmodium parasites, including drug-resistant strains. " | ( Safety, Pharmacokinetics, and Causal Prophylactic Efficacy of KAF156 in a Plasmodium falciparum Human Infection Study. Berger, D; Chang, M; Czartoski, JL; Duke, E; Jain, JP; Kappe, SHI; Kublin, JG; Leong, FJ; Maenza, J; Murphy, SC; Pertel, P; Potochnic, MA; Prince, WT; Seilie, AM; Soon, RL; Spera, D; Vaughan, A; Zhao, R, 2021) | 2.3 |
"KAF156 is a novel imidazolopiperazine anti-malarial with activity against pre-erythrocytic liver stages, asexual and sexual blood stages. " | ( A phase 1 evaluation of the pharmacokinetic/pharmacodynamic interaction of the anti-malarial agents KAF156 and piperaquine. Feng, Y; Goswami, B; Jain, JP; Leong, FJ; Stein, DS, 2018) | 2.14 |
KAF156 was tolerated, with self-limited mild to moderate gastrointestinal and neurological adverse events. KAF156 demonstrated high levels of pre- and post-CHMI protective efficacy.
This first-in-human, single- and multiple-ascending-dose study in 70 healthy male volunteers determined the maximum oral dose of KAF156 tolerated by healthy adults. Co-administration of PPQ and K AF156 had no overall effect on AUC of either compound, but the Cmax values of both KAF 156 and piperaquine increased.
Excerpt | Relevance | Reference |
---|---|---|
" The available data suggest that ganaplacide exerts multi-stage antimalarial activity, and that its pharmacokinetic profile potentially allows for a simplified dosing regimen compared to that of existing antimalarial drug combinations." | ( The early preclinical and clinical development of ganaplacide (KAF156), a novel antimalarial compound. Grobusch, MP; Koller, R; Mombo-Ngoma, G, 2018) | 0.72 |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Cytochrome P450 1A1 | Homo sapiens (human) | IC50 (µMol) | 6.0000 | 0.0079 | 1.2478 | 9.9000 | AID1849707 |
Cytochrome P450 1A2 | Homo sapiens (human) | IC50 (µMol) | 6.0000 | 0.0001 | 1.7740 | 10.0000 | AID1849707; AID673153 |
Cytochrome P450 2E1 | Homo sapiens (human) | IC50 (µMol) | 6.0000 | 0.0140 | 1.6872 | 6.2000 | AID1849707 |
Cytochrome P450 3A4 | Homo sapiens (human) | IC50 (µMol) | 6.0000 | 0.0001 | 1.7536 | 10.0000 | AID1849707; AID673157 |
Cytochrome P450 3A4 | Homo sapiens (human) | Ki | 0.1560 | 0.0001 | 1.4162 | 9.9000 | AID1579733 |
Cytochrome P450 2C8 | Homo sapiens (human) | IC50 (µMol) | 6.0000 | 0.0008 | 1.8848 | 7.9000 | AID1849707 |
Cytochrome P450 2D6 | Homo sapiens (human) | IC50 (µMol) | 6.0000 | 0.0000 | 2.0151 | 10.0000 | AID1849707; AID673156 |
Cytochrome P450 2A6 | Homo sapiens (human) | IC50 (µMol) | 6.0000 | 0.0044 | 3.8895 | 10.0000 | AID1849707 |
Cytochrome P450 2C9 | Homo sapiens (human) | IC50 (µMol) | 6.0000 | 0.0000 | 2.8005 | 10.0000 | AID1849707; AID673155 |
Cytochrome P450 4B1 | Homo sapiens (human) | IC50 (µMol) | 6.0000 | 6.2000 | 6.2000 | 6.2000 | AID1849707 |
Cytochrome P450 2B6 | Homo sapiens (human) | IC50 (µMol) | 6.0000 | 0.0011 | 3.4186 | 10.0000 | AID1849707 |
Cytochrome P450 3A5 | Homo sapiens (human) | IC50 (µMol) | 6.0000 | 0.0033 | 0.7073 | 6.2000 | AID1849707 |
Cytochrome P450 2A7 | Homo sapiens (human) | IC50 (µMol) | 6.0000 | 6.2000 | 6.2000 | 6.2000 | AID1849707 |
Cytochrome P450 3A7 | Homo sapiens (human) | IC50 (µMol) | 6.0000 | 0.0140 | 2.7580 | 6.2000 | AID1849707 |
Cytochrome P450 2F1 | Homo sapiens (human) | IC50 (µMol) | 6.0000 | 6.2000 | 6.2000 | 6.2000 | AID1849707 |
Cytochrome P450 2C18 | Homo sapiens (human) | IC50 (µMol) | 6.0000 | 6.2000 | 6.2000 | 6.2000 | AID1849707 |
Cytochrome P450 2C19 | Homo sapiens (human) | IC50 (µMol) | 6.0000 | 0.0000 | 2.3983 | 10.0000 | AID1849707; AID673154 |
Cytochrome P450 2J2 | Homo sapiens (human) | IC50 (µMol) | 6.0000 | 0.0120 | 2.5312 | 9.4700 | AID1849707 |
Cytochrome P450 4F2 | Homo sapiens (human) | IC50 (µMol) | 6.0000 | 1.6000 | 4.2667 | 6.2000 | AID1849707 |
Cytochrome P450 4F8 | Homo sapiens (human) | IC50 (µMol) | 6.0000 | 6.2000 | 6.2000 | 6.2000 | AID1849707 |
Cytochrome P450 4A11 | Homo sapiens (human) | IC50 (µMol) | 6.0000 | 6.2000 | 6.2000 | 6.2000 | AID1849707 |
Cytochrome P450 4F3 | Homo sapiens (human) | IC50 (µMol) | 6.0000 | 6.2000 | 6.2000 | 6.2000 | AID1849707 |
Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 (µMol) | 13.4000 | 0.0009 | 1.9014 | 10.0000 | AID1849708; AID673130 |
Cytochrome P450 1B1 | Homo sapiens (human) | IC50 (µMol) | 6.0000 | 0.0013 | 0.8696 | 9.9000 | AID1849707 |
Cytochrome P450 2A13 | Homo sapiens (human) | IC50 (µMol) | 6.0000 | 6.2000 | 6.2000 | 6.2000 | AID1849707 |
Cytochrome P450 4A22 | Homo sapiens (human) | IC50 (µMol) | 6.0000 | 6.2000 | 6.2000 | 6.2000 | AID1849707 |
Vitamin D 25-hydroxylase | Homo sapiens (human) | IC50 (µMol) | 6.0000 | 6.2000 | 6.2000 | 6.2000 | AID1849707 |
Cytochrome P450 2U1 | Homo sapiens (human) | IC50 (µMol) | 6.0000 | 6.2000 | 6.2000 | 6.2000 | AID1849707 |
Cytochrome P450 2W1 | Homo sapiens (human) | IC50 (µMol) | 6.0000 | 6.2000 | 6.2000 | 6.2000 | AID1849707 |
Cytochrome P450 2S1 | Homo sapiens (human) | IC50 (µMol) | 6.0000 | 6.2000 | 6.2000 | 6.2000 | AID1849707 |
Cytochrome P450 3A43 | Homo sapiens (human) | IC50 (µMol) | 6.0000 | 0.0140 | 2.7580 | 6.2000 | AID1849707 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID673158 | Cytotoxicity against human 293T cells | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID1731950 | Ratio of IC50 for CARL L1073Q mutant in multidrug-resistant Plasmodium falciparum to IC50 for wild type CARL in multidrug-resistant Plasmodium falciparum Dd2 | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite |
AID673148 | Antimalarial activity against Plasmodium berghei ANKA expressing GFP infected in NMRI mouse assessed as increase of mouse survival at 100 mg/kg, po administered 24 hrs post infection (Rvb = 6 to 7 days) | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID673175 | Tmax in Wistar rat at 30 mg/kg, po | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID1731954 | Ratio of IC50 for CARL L1108W mutant in multidrug-resistant Plasmodium falciparum to IC50 for wild type CARL in multidrug-resistant Plasmodium falciparum Dd2 | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite |
AID1731928 | Oral bioavailability in Balb/c mouse at 10 mg/kg measured upto 24 hrs by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite |
AID1579722 | Volume of distribution at steady state in Wistar Hannover rat at 3 mg/kg, iv by LC-MS/MS analysis | 2019 | Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23 | The Development Process for Discovery and Clinical Advancement of Modern Antimalarials. |
AID673169 | Half life in Wistar rat at 3 mg/kg, iv | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID1579738 | Half life in human infected with Plasmodium vivax at 400 mg administered for 3 consecutive days and measured up to 192 hrs | 2019 | Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23 | The Development Process for Discovery and Clinical Advancement of Modern Antimalarials. |
AID1579740 | Antimalarial activity against Plasmodium falciparum infected in human assessed as median parasite clearance time at 800 mg/kg, po and measured on day 5 | 2019 | Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23 | The Development Process for Discovery and Clinical Advancement of Modern Antimalarials. |
AID673280 | Oral bioavailability in Wistar rat at 100 mg/kg | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID1579726 | Oral bioavailability in Wistar Hannover rat at 10 mg/kg by LC-MS/MS analysis | 2019 | Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23 | The Development Process for Discovery and Clinical Advancement of Modern Antimalarials. |
AID1731929 | Intrinsic clearance in Balb/c mouse at 3 mg/kg, iv measured upto 24 hrs by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite |
AID673125 | Antimalarial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green fluorescence assay | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID673159 | Cytotoxicity against mouse BA/F3 cells | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID673146 | Antimalarial activity against Plasmodium berghei ANKA expressing GFP infected in po dosed NMRI mouse assessed as reduction of parasite level in blood administered 24 hrs post infection measured after 72 hrs post infection by flow cytometry | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID1579732 | Half life in human at 10 to 1200 mg and measured up to 360 hrs by LC-MS/MS method | 2019 | Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23 | The Development Process for Discovery and Clinical Advancement of Modern Antimalarials. |
AID1731901 | Antiplasmodial activity against multidrug-sensitive Plasmodium falciparum NF54 transfected with GFP-Luc infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation pretreated for 48 hrs followed by [3H]-hypoxanthine addition me | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite |
AID1849708 | Inhibition of human ERG | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | An insight into the recent development of the clinical candidates for the treatment of malaria and their target proteins. |
AID673278 | Oral bioavailability in Wistar rat at 10 mg/kg | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID673132 | Apparent permeability across apical to basolateral side in human Caco2 cells by LC/MS analysis | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID1731942 | Binding affinity to CARL L1073Q mutant in multidrug-resistant Plasmodium falciparum infected in human O-postive erythrocytes assessed as inhibition of parasite growth measured after 72 hrs by SYBR Green 1 staining based fluorescence assay | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite |
AID673167 | Volume of distribution in Wistar rat at 3 mg/kg, iv | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID673174 | Tmax in Wistar rat at 10 mg/kg, po | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID1579739 | Antimalarial activity against Plasmodium falciparum infected in human assessed as median parasite clearance time at 400 mg/kg, po administered for 3 consecutive day and measured on day 5 | 2019 | Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23 | The Development Process for Discovery and Clinical Advancement of Modern Antimalarials. |
AID673276 | AUC (all) in Wistar rat at 30 mg/kg, po | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID673285 | Selectivity index, ratio of CC50 for human HeLa cells to EC50 for Plasmodium falciparum | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID673129 | Metabolic stability in human liver microsomes assessed as hepatic extraction ratio by LC/MS/MS analysis in presence of CYP | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID673157 | Inhibition of human CYP3A4 | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID673282 | Selectivity index, ratio of CC50 for mouse BA/F3 cells to EC50 for Plasmodium falciparum | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID1731947 | Binding affinity to CARL M1050I mutant in multidrug-resistant Plasmodium falciparum infected in human O-postive erythrocytes assessed as inhibition of parasite growth measured after 72 hrs by SYBR Green 1 staining based fluorescence assay | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite |
AID673137 | AUC (0 to 24 hrs) in Balb/c mouse at 5 mg/kg, iv | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID673275 | AUC (all) in Wistar rat at 10 mg/kg, po | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID1579718 | Antimalarial activity against Plasmodium vivax assessed as reduction in parasite growth after 72 hrs by SYBR-green based fluorescence assay | 2019 | Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23 | The Development Process for Discovery and Clinical Advancement of Modern Antimalarials. |
AID1731955 | Ratio of IC50 for CARL V1053G mutant in multidrug-resistant Plasmodium falciparum to IC50 for wild type CARL in multidrug-resistant Plasmodium falciparum Dd2 | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite |
AID1731933 | Protein binding in human plasma | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite |
AID1849716 | Antimalarial activity against Plasmodium falciparum 3D7 | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | An insight into the recent development of the clinical candidates for the treatment of malaria and their target proteins. |
AID1579733 | Inhibition of CYP3A4 (unknown origin) | 2019 | Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23 | The Development Process for Discovery and Clinical Advancement of Modern Antimalarials. |
AID673163 | Cytotoxicity against human HuH7 cells | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID1731932 | Ratio of unbound average drug concentration in Balb/c mouse at 20 mg/kg, po to IC50 for antiplasmodial activity against multidrug-sensitive Plasmodium falciparum NF54 | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite |
AID673152 | Dose normalized AUC (0 to 5 hrs) in Wistar rat at 10 mg/kg, po | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID673155 | Inhibition of human CYP2C9 | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID673273 | Half life in Wistar rat at 30 mg/kg, po | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID673168 | Clearance in Wistar rat at 3 mg/kg, iv | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID673143 | Antimalarial activity against Plasmodium berghei ANKA expressing GFP infected in NMRI mouse assessed as reduction of parasite level in blood at 30 mg/kg, po administered 24 hrs post infection measured after 72 hrs post infection by flow cytometry | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID1849700 | Dissociation constant, pKa of compound | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | An insight into the recent development of the clinical candidates for the treatment of malaria and their target proteins. |
AID1731931 | Unbound average drug concentration in Balb/c mouse at 20 mg/kg, po measured upto 24 hrs by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite |
AID673150 | AUC (0 to 5 hrs) in Wistar rat at 10 mg/kg, po | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID1731945 | Binding affinity to CARL L1108W mutant in multidrug-resistant Plasmodium falciparum infected in human O-postive erythrocytes assessed as inhibition of parasite growth measured after 72 hrs by SYBR Green 1 staining based fluorescence assay | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite |
AID673284 | Selectivity index, ratio of CC50 for human HepG2 cells to EC50 for Plasmodium falciparum | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID673139 | Tmax in Balb/c mouse at 20 mg/kg, po | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID1731943 | Binding affinity to CARL A1122E mutant in multidrug-resistant Plasmodium falciparum infected in human O-postive erythrocytes assessed as inhibition of parasite growth measured after 72 hrs by SYBR Green 1 staining based fluorescence assay | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite |
AID673124 | Antimalarial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green fluorescence assay | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID673160 | Cytotoxicity against CHO cells | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID673144 | Antimalarial activity against Plasmodium berghei ANKA expressing GFP infected in NMRI mouse assessed as reduction of parasite level in blood at 100 mg/kg, po administered 24 hrs post infection measured after 72 hrs post infection by flow cytometry | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID673274 | Half life in Wistar rat at 100 mg/kg, po | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID1731956 | Ratio of IC50 for CARL M1050I mutant in multidrug-resistant Plasmodium falciparum to IC50 for wild type CARL in multidrug-resistant Plasmodium falciparum Dd2 | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite |
AID673147 | Antimalarial activity against Plasmodium berghei ANKA expressing GFP infected in NMRI mouse assessed as increase of mouse survival at 30 mg/kg, po administered 24 hrs post infection (Rvb = 6 to 7 days) | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID1731957 | Ratio of IC50 for CARL I1139K mutant in multidrug-resistant Plasmodium falciparum to IC50 for wild type CARL in multidrug-resistant Plasmodium falciparum Dd2 | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite |
AID673151 | Cmax in Wistar rat at 10 mg/kg, po | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID673156 | Inhibition of human CYP2D6 | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID1579741 | Antimalarial activity against Plasmodium vivax infected in human assessed as median parasite clearance time at 400 mg/kg, po administered for 3 consecutive day and measured on day 5 | 2019 | Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23 | The Development Process for Discovery and Clinical Advancement of Modern Antimalarials. |
AID673145 | Antimalarial activity against Plasmodium berghei ANKA expressing GFP infected in NMRI mouse assessed as reduction of parasite level in blood at 30 mg/kg, po administered 24 hrs post infection qd for 3 days measured after 96 hrs post infection by flow cyto | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID1579728 | Cmax in human at 10 to 1200 mg and measured up to 360 hrs by LC-MS/MS method | 2019 | Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23 | The Development Process for Discovery and Clinical Advancement of Modern Antimalarials. |
AID1579719 | Antimalarial activity against Plasmodium falciparum assessed as reduction in parasite growth after 72 hrs by SYBR-green based fluorescence assay | 2019 | Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23 | The Development Process for Discovery and Clinical Advancement of Modern Antimalarials. |
AID1579736 | Cardiotoxicity in human assessed as effect on QT parameters at 800 mg in presence of PPQ | 2019 | Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23 | The Development Process for Discovery and Clinical Advancement of Modern Antimalarials. |
AID673141 | AUC (0 to 24 hrs) in Balb/c mouse at 20 mg/kg, po | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID673281 | Selectivity index, ratio of CC50 for human 293T cells to EC50 for Plasmodium falciparum | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID1579731 | Volume of distribution in human at 10 to 1200 mg and measured up to 360 hrs by LC-MS/MS method | 2019 | Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23 | The Development Process for Discovery and Clinical Advancement of Modern Antimalarials. |
AID1579720 | Half life in Wistar Hannover rat at 3 mg/kg, iv by LC-MS/MS analysis | 2019 | Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23 | The Development Process for Discovery and Clinical Advancement of Modern Antimalarials. |
AID1579737 | Half life in human infected with Plasmodium falciparum at 400 mg administered for 3 consecutive days and measured up to 192 hrs | 2019 | Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23 | The Development Process for Discovery and Clinical Advancement of Modern Antimalarials. |
AID673135 | Clearance in Balb/c mouse plasma at 5 mg/kg, iv | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID1731953 | Ratio of IC50 for CARL E1104K mutant in multidrug-resistant Plasmodium falciparum to IC50 for wild type CARL in multidrug-resistant Plasmodium falciparum Dd2 | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite |
AID673153 | Inhibition of human CYP1A2 | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID673134 | Volume of distribution in Balb/c mouse at 5 mg/kg, iv | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID1731952 | Ratio of IC50 for CARL 11072V mutant in multidrug-resistant Plasmodium falciparum to IC50 for wild type CARL in multidrug-resistant Plasmodium falciparum Dd2 | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite |
AID673161 | Cytotoxicity against human Hep2 cells | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID1731946 | Binding affinity to CARL V1053G mutant in multidrug-resistant Plasmodium falciparum infected in human O-postive erythrocytes assessed as inhibition of parasite growth measured after 72 hrs by SYBR Green 1 staining based fluorescence assay | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite |
AID1731951 | Ratio of IC50 for CARL A1122E mutant in multidrug-resistant Plasmodium falciparum to IC50 for wild type CARL in multidrug-resistant Plasmodium falciparum Dd2 | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite |
AID673138 | Cmax in Balb/c mouse at 20 mg/kg, po | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID1731925 | Blood clearance in Balb/c mouse at 3 mg/kg, iv measured upto 24 hrs by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite |
AID673142 | Oral bioavailability in Balb/c mouse at 20 mg/kg | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID673154 | Inhibition of human CYP2C19 | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID1731944 | Binding affinity to CARL 11072V mutant in multidrug-resistant Plasmodium falciparum infected in human O-postive erythrocytes assessed as inhibition of parasite growth measured after 72 hrs by SYBR Green 1 staining based fluorescence assay | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite |
AID673272 | Half life in Wistar rat at 10 mg/kg, po | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID673127 | Metabolic stability in mouse liver microsomes assessed as hepatic extraction ratio by LC/MS/MS analysis in presence of CYP | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID673283 | Selectivity index, ratio of CC50 for CHO cells to EC50 for Plasmodium falciparum | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID1849707 | Inhibition of CYP450 (unknown origin) | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | An insight into the recent development of the clinical candidates for the treatment of malaria and their target proteins. |
AID1731948 | Binding affinity to CARL I1139K mutant in multidrug-resistant Plasmodium falciparum infected in human O-postive erythrocytes assessed as inhibition of parasite growth measured after 72 hrs by SYBR Green 1 staining based fluorescence assay | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite |
AID1731949 | Binding affinity to CARL E1104K mutant in multidrug-resistant Plasmodium falciparum infected in human O-postive erythrocytes assessed as inhibition of parasite growth measured after 72 hrs by SYBR Green 1 staining based fluorescence assay | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite |
AID1579742 | Antimalarial activity against Plasmodium vivax infected in human assessed as median parasite clearance time at 800 mg/kg, po and measured on day 5 | 2019 | Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23 | The Development Process for Discovery and Clinical Advancement of Modern Antimalarials. |
AID1731930 | Unbound AUC in Balb/c mouse at 20 mg/kg, po measured upto 24 hrs by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite |
AID1579723 | Cmax in Wistar Hannover rat at 10 mg/kg, po by LC-MS/MS analysis | 2019 | Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23 | The Development Process for Discovery and Clinical Advancement of Modern Antimalarials. |
AID673279 | Oral bioavailability in Wistar rat at 30 mg/kg | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID673149 | Antimalarial activity against Plasmodium berghei ANKA expressing GFP infected in NMRI mouse assessed as increase of mouse survival at 30 mg/kg, po administered 24 hrs post infection qd for 3 days (Rvb = 6 to 7 days) | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID673176 | Tmax in Wistar rat at 100 mg/kg, po | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID1579721 | Plasma clearance in Wistar Hannover rat at 3 mg/kg, iv by LC-MS/MS analysis | 2019 | Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23 | The Development Process for Discovery and Clinical Advancement of Modern Antimalarials. |
AID1579727 | Tmax in human at 10 to 1200 mg and measured up to 360 hrs by LC-MS/MS method | 2019 | Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23 | The Development Process for Discovery and Clinical Advancement of Modern Antimalarials. |
AID673173 | Cmax in Wistar rat at 100 mg/kg, po | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID673133 | Apparent permeability across basolateral to apical side in human Caco2 cells by LC/MS analysis | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID1579730 | Apparent clearance in human at 10 to 1200 mg and measured up to 360 hrs by LC-MS/MS method | 2019 | Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23 | The Development Process for Discovery and Clinical Advancement of Modern Antimalarials. |
AID673171 | Cmax in Wistar rat at 10 mg/kg, po | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID673136 | Half life in Balb/c mouse at 5 mg/kg, iv | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID673162 | Cytotoxicity against human HeLa cells | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID1849722 | In vivo antimalarial activity against Plasmodium berghei infected in mouse model | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | An insight into the recent development of the clinical candidates for the treatment of malaria and their target proteins. |
AID673277 | AUC (all) in Wistar rat at 100 mg/kg, po | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID1579734 | Cardiotoxicity in human assessed as effect on QT parameters at 800 mg | 2019 | Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23 | The Development Process for Discovery and Clinical Advancement of Modern Antimalarials. |
AID673172 | Cmax in Wistar rat at 30 mg/kg, po | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID673170 | AUC in Wistar rat at 3 mg/kg, iv | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID1731941 | Binding affinity to wild type CARL in multidrug-resistant Plasmodium falciparum Dd2 infected in human O-postive erythrocytes assessed as inhibition of parasite growth measured after 72 hrs by SYBR Green 1 staining based fluorescence assay | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite |
AID673131 | Permeability of the compound by PAMPA | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID1579725 | Half life in Wistar Hannover rat at 10 mg/kg, po by LC-MS/MS analysis | 2019 | Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23 | The Development Process for Discovery and Clinical Advancement of Modern Antimalarials. |
AID673130 | Inhibition of human ERG channel expressed in CHO cells by patch clamp assay | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID1579724 | Tmax in Wistar Hannover rat at 10 mg/kg, po by LC-MS/MS analysis | 2019 | Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23 | The Development Process for Discovery and Clinical Advancement of Modern Antimalarials. |
AID673286 | Selectivity index, ratio of CC50 for human HuH7 cells to EC50 for Plasmodium falciparum | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID1579729 | AUC (0 to 24 hrs) in human at 10 to 1200 mg and measured up to 360 hrs by LC-MS/MS method | 2019 | Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23 | The Development Process for Discovery and Clinical Advancement of Modern Antimalarials. |
AID673140 | Half life in Balb/c mouse at 20 mg/kg, po | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
AID1849721 | Antimalarial activity against Plasmodium falciparum W2 | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | An insight into the recent development of the clinical candidates for the treatment of malaria and their target proteins. |
AID673128 | Metabolic stability in rat liver microsomes assessed as hepatic extraction ratio by LC/MS/MS analysis in presence of CYP | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 0 (0.00) | 29.6817 |
2010's | 10 (62.50) | 24.3611 |
2020's | 6 (37.50) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (27.29) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 5 (31.25%) | 5.53% |
Reviews | 5 (31.25%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 6 (37.50%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |