Detailed information for compound 154154

Basic information

Technical information
  • TDR Targets ID: 154154
  • Name: 5-methylindolo[3,2-b]quinoline hydrochloride
  • MW: 268.741 | Formula: C16H13ClN2
  • H donors: 0 H acceptors: 1 LogP: 4.13 Rotable bonds: 0 Rule of 5 violations (Lipinski): 1
  • SMILES: Cn1c2ccccc2cc2c1c1ccccc1n2.Cl
  • InChi: 1S/C16H12N2.ClH/c1-18-15-9-5-2-6-11(15)10-14-16(18)12-7-3-4-8-13(12)17-14;/h2-10H,1H3;1H
  • InChiKey: PACBZNVVTJRUCN-UHFFFAOYSA-N  

Network

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Synonyms

  • 5-methyl-10H-indolo[3,2-b]quinolin-5-ium chloride
  • 5-methyl-10H-quinolino[3,2-b]indol-5-ium chloride
  • NSC357789
  • 5-methylquinolino[3,2-b]indole hydrochloride
  • 72782-09-3
  • 480-26-2
  • 5-Methyl-5H-quindoline hydrochloride
  • 5H-Quindoline, 5-methyl-, monohydrochloride
  • NSC647765
  • cryptolepine hydrochloride

Targets

Known targets for this compound

No curated genes were found associated with this compound

Predicted pathogen targets for this compound

By orthology
No druggable targets predicted by orthology data
By sequence similarity to non orthologous known druggable targets
No druggable targets predicted by sequence similarity

Obtained from network model

Ranking Plot


Putative Targets List


Species Potential target Raw Global Species

Activities

Activity type Activity value Assay description Source Reference
Activity (functional) Antiplasmodial activity against GFP-expressing liver stage Plasmodium berghei sporozoites infected in human Huh-7 cells at 5 uM by fluorescence activated cell sorting based method ChEMBL. 21207937
Activity (functional) = 10.8 % Antimalarial activity as reduced parasitaemia against Plasmodium berghei yoelii infected Swiss albino mice (Mus musculus) at 50 mg/kg/day peroral dose for 4 days ChEMBL. 9249972
Activity (functional) = 15.6 % Antimalarial activity as reduced parasitaemia against Plasmodium berghei infected Swiss albino mice (Mus musculus) at 50 mg/kg/day peroral dose for 4 days ChEMBL. 9249972
Activity (binding) = 4.53 umol/min/mg Activity of recombinant human NQO1 assessed as specific activity ChEMBL. 17643990
Body weight (functional) = 193 g In vitro effect of drug administration on Body weight in Fructose fed STZ-treated rats,pre dose (Treatment group - Fructose/STZ ) ChEMBL. 9526563
Body weight (functional) = 201 g In vitro effect of drug administration on Body weight in Fructose fed STZ-treated rats,pre dose ((Treatment group - Fructose/STZ + cryptoline HCl, 30 mg/kg) ChEMBL. 9526563
Body weight (functional) = 207 g In vitro effect of drug administration on Body weight in Fructose fed STZ-treated rats,pre dose (Treatment group - Chow) ChEMBL. 9526563
Body weight (functional) = 211 g In vitro effect of drug administration on Body weight in Fructose fed STZ-treated rats,after 24 hr (Treatment group - Fructose/STZ ) ChEMBL. 9526563
Body weight (functional) = 223 g In vitro effect of drug administration on Body weight in Fructose fed STZ-treated rats,after 24 hr (Treatment group - Fructose/STZ + cryptoline HCl, 30 mg/kg) ChEMBL. 9526563
Body weight (functional) = 244 g In vitro effect of drug administration on Body weight in Fructose fed STZ-treated rats,after 24 hr (Treatment group - Chow) ChEMBL. 9526563
Change (functional) = -43.1 % Change in plasma glucose levels measured in genetically altered obese diabetic mice(db/db) at 100 mg/kg at 24 h postdose ChEMBL. 9667966
Change (functional) = -43.1 % Change in plasma glucose levels measured in genetically altered obese diabetic mice(db/db) at 100 mg/kg at 24 h postdose ChEMBL. 9667966
Change (functional) = -16.4 % Change in plasma glucose levels measured in genetically altered obese diabetic mice(db/db) at 100 mg/kg at 3 h postdose ChEMBL. 9667966
Change (functional) = -16.4 % Change in plasma glucose levels measured in genetically altered obese diabetic mice(db/db) at 100 mg/kg at 3 h postdose ChEMBL. 9667966
Change of predose (functional) = -43.1 % Compound was evaluated in vitro for its ability to stimulate glucose transport in 3T3-L1 adipocytes ,given at 100 mg/kg in mouse,after 24 hr ChEMBL. 9526563
Change of predose (functional) = -43.1 % Compound was evaluated in vitro for its ability to stimulate glucose transport in 3T3-L1 adipocytes ,given at 100 mg/kg in mouse,after 24 hr ChEMBL. 9526563
Change of predose (functional) = -16.4 % Compound was evaluated in vitro for its ability to stimulate glucose transport in 3T3-L1 adipocytes ,given at 100 mg/kg in mouse,after 3 hr ChEMBL. 9526563
Change of predose (functional) = -16.4 % Compound was evaluated in vitro for its ability to stimulate glucose transport in 3T3-L1 adipocytes ,given at 100 mg/kg in mouse,after 3 hr ChEMBL. 9526563
Change of predose (functional) = 170.7 % Effect of the compound when given at 30 mg/kg in (C57BL/ks)mouse,after day 3 ChEMBL. 9526563
Change of predose (functional) = 170.7 % Effect of the compound when given at 30 mg/kg in (C57BL/ks)mouse,after day 3 ChEMBL. 9526563
Change of predose (functional) = 184.5 % Effect of the compound when given at 30 mg/kg in (C57BL/ks)mouse,Predose ChEMBL. 9526563
Change of predose (functional) = 184.5 % Effect of the compound when given at 30 mg/kg in (C57BL/ks)mouse,Predose ChEMBL. 9526563
Change of predose (functional) = 358 % Effect of the compound when given at 30 mg/kg in (db/db)mice,3 days postdose ChEMBL. 9526563
Change of predose (functional) = 358 % Effect of the compound when given at 30 mg/kg in (db/db)mice,3 days postdose ChEMBL. 9526563
Food intake (functional) = 18 g day-1 In vitro effect of drug administration on food consumption in Fructose fed STZ-treated rats (Treatment group - Fructose/STZ + cryptoline HCl, 30 mg/kg) ChEMBL. 9526563
Food intake (functional) = 22 g day-1 In vitro effect of drug administration on food consumption in Fructose fed STZ-treated rats (Treatment group - Chow) ChEMBL. 9526563
Food intake (functional) = 25 g day-1 In vitro effect of drug administration on food consumption in Fructose fed STZ-treated rats (Treatment group - Fructose/STZ ) ChEMBL. 9526563
Food intake (functional) = 0.9 g mouse-1 day-1 Food intake in db/db Mice expressed as gram/mouse/day and the observed after 48 hr. ChEMBL. 9526563
Food intake (functional) = 0.9 g mouse-1 day-1 Food intake measured in genetically altered obese diabetic mice(db/db) at 100 mg/kg dose ChEMBL. 9667966
Food intake (functional) = 0.9 g mouse-1 day-1 Food intake in db/db Mice expressed as gram/mouse/day and the observed after 48 hr. ChEMBL. 9526563
Food intake (functional) = 0.9 g mouse-1 day-1 Food intake measured in genetically altered obese diabetic mice(db/db) at 100 mg/kg dose ChEMBL. 9667966
Food intake (functional) = 2.3 g mouse-1 day-1 Food intake in C57BL/ks Mice expressed as gram/mouse/day and the observation made at 24-48 Hrs, when administered at a dose of 30 mg/kg ChEMBL. 9526563
Food intake (functional) = 2.3 g mouse-1 day-1 Food intake in C57BL/ks Mice expressed as gram/mouse/day and the observation made at 24-48 Hrs, when administered at a dose of 30 mg/kg ChEMBL. 9526563
Food intake (functional) = 2.4 g mouse-1 day-1 Food intake in db/db Mice expressed as gram/mouse/day and the observation made at 0 - 24 Hrs, in db/db mice administered at a dose of 30 mg/kg ChEMBL. 9526563
Food intake (functional) = 2.4 g mouse-1 day-1 Food intake in db/db Mice expressed as gram/mouse/day and the observation made at 24 - 48 Hrs, in db/db mice administered at a dose of 30 mg/kg ChEMBL. 9526563
Food intake (functional) = 2.4 g mouse-1 day-1 Food intake in db/db Mice expressed as gram/mouse/day and the observation made at 0 - 24 Hrs, in db/db mice administered at a dose of 30 mg/kg ChEMBL. 9526563
Food intake (functional) = 2.4 g mouse-1 day-1 Food intake in db/db Mice expressed as gram/mouse/day and the observation made at 24 - 48 Hrs, in db/db mice administered at a dose of 30 mg/kg ChEMBL. 9526563
Food intake (functional) = 2.7 g mouse-1 day-1 Food intake in C57BL/ks Mice expressed as gram/mouse/day and the observation made at 0 -24 Hrs, when administered at a dose of 30 mg/kg ChEMBL. 9526563
Food intake (functional) = 2.7 g mouse-1 day-1 Food intake in C57BL/ks Mice expressed as gram/mouse/day and the observation made at 0 -24 Hrs, when administered at a dose of 30 mg/kg ChEMBL. 9526563
Food intake (functional) = 3.3 g mouse-1 day-1 Food intake in db/db Mice expressed as gram/mouse/day and the observation made at 0 - 24 Hrs, in db/db mice administered at a dose of 20 mg/kg ChEMBL. 9526563
Food intake (functional) = 3.3 g mouse-1 day-1 Food intake in db/db Mice expressed as gram/mouse/day and the observation made at 0 - 24 Hrs, in db/db mice administered at a dose of 20 mg/kg ChEMBL. 9526563
Food intake (functional) = 3.8 g mouse-1 day-1 Food intake in db/db Mice expressed as gram/mouse/day and the observation made at 24 - 48 Hrs, in db/db mice administered at a dose of 20 mg/kg ChEMBL. 9526563
Food intake (functional) = 3.8 g mouse-1 day-1 Food intake in db/db Mice expressed as gram/mouse/day and the observation made at 24 - 48 Hrs, in db/db mice administered at a dose of 20 mg/kg ChEMBL. 9526563
Glucose transport (functional) = 148 % In vitro glucose transport activity in 3T3-LI adipocytes at 3 microM concentration. ChEMBL. 9667966
Glucose transport (functional) = 148 % In vitro glucose transport activity in 3T3-LI adipocytes at 3 microM concentration. ChEMBL. 9667966
Glucose transport (functional) = 305 % In vitro glucose transport activity in 3T3-LI adipocytes at 10 microM concentration. ChEMBL. 9667966
Glucose transport (functional) = 305 % In vitro glucose transport activity in 3T3-LI adipocytes at 10 microM concentration. ChEMBL. 9667966
Glucose transport (functional) = 359 % In vitro glucose transport activity in 3T3-LI adipocytes at 30 microM concentration. ChEMBL. 9667966
Glucose transport (functional) = 359 % In vitro glucose transport activity in 3T3-LI adipocytes at 30 microM concentration. ChEMBL. 9667966
IC12 (functional) = 0.6 ug ml-1 Growth inhibition of Saccharomyces cerevisiae 1138 mutant by yeast bioassay ChEMBL. 10425120
IC12 (functional) = 0.6 ug ml-1 Growth inhibition of Saccharomyces cerevisiae 1140 mutant by yeast bioassay ChEMBL. 10425120
IC12 (functional) = 0.6 ug ml-1 Growth inhibition of Saccharomyces cerevisiae 1353 mutant by yeast bioassay ChEMBL. 10425120
IC20 (functional) = 7.5 uM Cytotoxicity against Saccharomyces cerevisiae ChEMBL. 18710911
IC40 (functional) = 17 uM Cytotoxicity against Saccharomyces cerevisiae ChEMBL. 18710911
IC50 (functional) = 1.72 M Inhibition of beta-hematin formation by BHIA assay ChEMBL. 15921407
IC50 (functional) = 41 ng/ml Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D6 infected human erythrocytes by [3H]hypoxanthine uptake ChEMBL. 9249972
IC50 (functional) = 52 ng/ml Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 infected human erythrocytes by [3H]hypoxanthine uptake ChEMBL. 9249972
IC50 (functional) = 222 nM Antiplasmodial activity against chloroquine-sensitive, mefloquine-resistant ring stage Plasmodium falciparum D6 infected in human red blood cells after 48 hrs ChEMBL. 21207937
IC50 (functional) = 259 nM Antiplasmodial activity against chloroquine and pyrimethamine-resistant ring stage Plasmodium falciparum V1/S infected in human red blood cells after 48 hrs ChEMBL. 21207937
IC50 (functional) = 424 nM Antiplasmodial activity against chloroquine-sensitive ring stage Plasmodium falciparum 3D7 infected in human red blood cells after 48 hrs ChEMBL. 21207937
IC50 (functional) = 755 nM Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 ChEMBL. 18207399
IC50 (functional) = 755 nM Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 ChEMBL. 18207399
IC50 (functional) = 755 nM Antiplasmodial activity against chloroquine-resistant ring stage Plasmodium falciparum W2 infected in human red blood cells after 48 hrs ChEMBL. 21207937
IC50 (ADMET) = 1180 nM Cytotoxicity against HUVEC cells ChEMBL. 18207399
IC50 (ADMET) = 1180 nM Cytotoxicity against HUVEC cells ChEMBL. 18207399
IC50 (functional) = 100000 nM Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 ChEMBL. 18395298
IC50 (functional) < 1 ug ml-1 Cytotoxicity against mouse M109 cells ChEMBL. 10425120
IC50 (functional) = 0.12 uM Antimalarial activity against chloroquine and pyrimethamine-resistant Plasmodium falciparum K1 by [3H]hypoxanthine incorporation assay ChEMBL. 19781948
IC50 (functional) = 0.12 uM Antiparasitic activity against Plasmodium falciparum K1 ChEMBL. 20133138
IC50 (functional) = 0.12 uM Antiplasmodial activity against chloroquine and pyrimethamine-resistant Plasmodium falciparum K1 by [3H]hypoxanthine uptake ChEMBL. 15921407
IC50 (functional) = 0.22 uM Antitrypanosomal activity against Trypanosoma cruzi ChEMBL. 15921407
IC50 (functional) = 0.22 uM Antitrypanosomal activity against Trypanosoma cruzi ChEMBL. 19781948
IC50 (functional) = 0.44 uM In vitro antiplasmodial activity of the compound against Plasmodium falciparum ChEMBL. 15801861
IC50 (functional) = 0.44 uM In vitro antiplasmodial activity of the compound against Plasmodium falciparum ChEMBL. 15801861
IC50 (functional) = 0.6 uM Antitrypanosomal activity against Trypanosoma brucei rhodesiense ChEMBL. 15921407
IC50 (functional) = 0.6 uM Antitrypanosomal activity against Trypanosoma brucei rhodesiense ChEMBL. 19781948
IC50 (functional) = 0.8 uM Cytotoxicity against NQO2 expressing human RT112 cells in presence of NRH cofactor by MTT assay ChEMBL. 17643990
IC50 (functional) = 0.82 uM Cytotoxicity against NQO2 expressing human RT112 cells by MTT assay ChEMBL. 17643990
IC50 (functional) = 1.28 uM Cytotoxicity against low NQO1 protein expressing human BE cells by MTT assay ChEMBL. 17643990
IC50 (functional) = 1.45 uM Cytotoxicity against high NQO1 protein expressing human H460 cells by MTT assay ChEMBL. 17643990
IC50 (functional) = 1.75 uM In vitro cell survival assay on cancer KB cell lines ChEMBL. 11300877
IC50 (functional) = 2 uM Antitrypanosomal activity against Trypanosoma brucei brucei ChEMBL. 22926067
IC50 (functional) = 2.68 uM Antileishmanial activity against Leishmania donovani ChEMBL. 15921407
IC50 (functional) = 2.68 uM Antileishmanial activity against Leishmania donovani axenic amastigotes ChEMBL. 19781948
IC50 (functional) = 3.95 uM Cytotoxicity of the compound against MAC15A mouse adenocarcinomas of the colon cells ChEMBL. 15801861
IC50 (functional) = 3.95 uM Cytotoxicity of the compound against MAC15A mouse adenocarcinomas of the colon cells ChEMBL. 15801861
IC50 (functional) = 20.29 uM Cytotoxicity against Saccharomyces cerevisiae JN394 harboring deltarad52 mutant gene after 4 hrs ChEMBL. 18710911
IC50 (binding) = 23 uM Inhibition of Trypanosoma brucei rhodesiense rhodesain ChEMBL. 22926067
IC50 (functional) = 25.03 uM Cytotoxicity against Saccharomyces cerevisiae BY4741 harboring deltaerg6 mutant gene after 4 hrs ChEMBL. 18710911
IC50 (binding) = 64 uM Inhibition of Trypanosoma brucei CatB ChEMBL. 22926067
Inhibition (binding) Inhibition of IL1beta-induced p38 MAPK phosphorylation in human SK-N-SH cells at 10 to 20 uM preincubated for 30 mins prior to IL1beta-stimulation measured after 1 hr by Western blotting analysis ChEMBL. 23507189
Inhibition (binding) Inhibition of p38 MAPK in human SK-N-SH cells assessed as inhibition of IL1beta-induced MAPKAPK2 phosphorylation preincubated for 30 mins prior to IL1beta-stimulation measured after 1 hr by Western blotting analysis ChEMBL. 23507189
Inhibition (binding) Inhibition of IL1beta-induced NFkappaB p65 nuclear translocation in human SK-N-SH cells after 15 mins by ELISA ChEMBL. 23507189
Inhibition (functional) = 30 % Inhibition of LPS-stimulated nitric oxide production in mouse RAW 264.7 cells at 5 uM after 20 hrs relative to control ChEMBL. 17064915
Inhibition (functional) = 50 % Inhibition of LPS-stimulated nitric oxide production in mouse RAW 264.7 cells at 10 uM after 20 hrs relative to control ChEMBL. 17064915
Mean body weight (functional) = 22.7 g mouse-1 Mean body weight expressed as grams/mouse (C57BL/ks) at 48hrs, when given at 30 mg/kg ChEMBL. 9526563
Mean body weight (functional) = 22.7 g mouse-1 Mean body weight expressed as grams/mouse (C57BL/ks) at 48hrs, when given at 30 mg/kg ChEMBL. 9526563
Mean body weight (functional) = 23.3 g mouse-1 Mean body weight expressed as grams/mouse (C57BL/ks) at 24hrs, when given at 30 mg/kg ChEMBL. 9526563
Mean body weight (functional) = 23.3 g mouse-1 Mean body weight expressed as grams/mouse (C57BL/ks) at 24hrs, when given at 30 mg/kg ChEMBL. 9526563
Mean body weight (functional) = 23.7 g mouse-1 Mean body weight expressed as grams/mouse (C57BL/ks) at 0hrs, when given at 30 mg/kg ChEMBL. 9526563
Mean body weight (functional) = 23.7 g mouse-1 Mean body weight expressed as grams/mouse (C57BL/ks) at 0hrs, when given at 30 mg/kg ChEMBL. 9526563
Mean body weight (functional) = 35.5 g mouse-1 Compound was evaluated for the invivo effects on plasma glucose concentrations in db/db mice administered at a dose of 30 mg/kg mean body weight expressed as grams/mouse at 0 hr ChEMBL. 9526563
Mean body weight (functional) = 35.5 g mouse-1 Compound was evaluated for the invivo effects on plasma glucose concentrations in db/db mice administered at a dose of 30 mg/kg mean body weight expressed as grams/mouse at 0 hr ChEMBL. 9526563
Mean body weight (functional) = 36.9 g mouse-1 Compound was evaluated for the invivo effects on plasma glucose concentrations in db/db mice administered at a dose of 30 mg/kg mean body weight expressed as grams/mouse at 24 hr ChEMBL. 9526563
Mean body weight (functional) = 36.9 g mouse-1 Compound was evaluated for the invivo effects on plasma glucose concentrations in db/db mice administered at a dose of 30 mg/kg mean body weight expressed as grams/mouse at 24 hr ChEMBL. 9526563
Mean body weight (functional) = 37 g mouse-1 Compound was evaluated for the invivo effects on plasma glucose concentrations in db/db mice administered at a dose of 30 mg/kg mean body weight expressed as grams/mouse at 0 hr ChEMBL. 9526563
Mean body weight (functional) = 37 g mouse-1 Compound was evaluated for the invivo effects on plasma glucose concentrations in db/db mice administered at a dose of 30 mg/kg mean body weight expressed as grams/mouse at 0 hr ChEMBL. 9526563
Mean body weight (functional) = 37.4 g mouse-1 Compound was evaluated for the invivo effects on plasma glucose concentrations in db/db mice administered at a dose of 20 mg/kg mean body weight expressed as grams/mouse at 0 hr ChEMBL. 9526563
Mean body weight (functional) = 37.4 g mouse-1 Compound was evaluated for the invivo effects on plasma glucose concentrations in db/db mice administered at a dose of 20 mg/kg mean body weight expressed as grams/mouse at 0 hr ChEMBL. 9526563
Mean body weight (functional) = 37.9 g mouse-1 Compound was evaluated for the invivo effects on plasma glucose concentrations in db/db mice administered at a dose of 20 mg/kg mean body weight expressed as grams/mouse at 24 hr ChEMBL. 9526563
Mean body weight (functional) = 37.9 g mouse-1 Compound was evaluated for the invivo effects on plasma glucose concentrations in db/db mice administered at a dose of 20 mg/kg mean body weight expressed as grams/mouse at 24 hr ChEMBL. 9526563
Mean body weight (functional) = 38 g mouse-1 Compound was evaluated for the invivo effects on plasma glucose concentrations in db/db mice administered at a dose of 20 mg/kg mean body weight expressed as grams/mouse at 0 hr ChEMBL. 9526563
Mean body weight (functional) = 38 g mouse-1 Compound was evaluated for the invivo effects on plasma glucose concentrations in db/db mice administered at a dose of 20 mg/kg mean body weight expressed as grams/mouse at 0 hr ChEMBL. 9526563
Mean body weight (functional) = 39.8 g mouse-1 Mean body weight expressed as grams/mouse at 24hrs, when given at 100 mg/kg ChEMBL. 9526563
Mean body weight (functional) = 39.8 g mouse-1 Mean body weight measured in genetically altered obese diabetic mice(db/db) at 100 mg/kg at 24 h postdose ChEMBL. 9667966
Mean body weight (functional) = 39.8 g mouse-1 Mean body weight expressed as grams/mouse at 24hrs, when given at 100 mg/kg ChEMBL. 9526563
Mean body weight (functional) = 39.8 g mouse-1 Mean body weight measured in genetically altered obese diabetic mice(db/db) at 100 mg/kg at 24 h postdose ChEMBL. 9667966
Mean body weight (functional) = 41 g mouse-1 Mean body weight expressed as grams/mouse at 0hrs, when given at 100 mg/kg ChEMBL. 9526563
Mean body weight (functional) = 41 g mouse-1 Mean body weight measured in genetically altered obese diabetic mice(db/db) at 100 mg/kg at 0 h postdose ChEMBL. 9667966
Mean body weight (functional) = 41 g mouse-1 Mean body weight expressed as grams/mouse at 0hrs, when given at 100 mg/kg ChEMBL. 9526563
Mean body weight (functional) = 41 g mouse-1 Mean body weight measured in genetically altered obese diabetic mice(db/db) at 100 mg/kg at 0 h postdose ChEMBL. 9667966
Mean survival time (functional) day Mean survival time taken as number of days before illness due to Plasmodium berghei when mice treated with 20 mg/kg dose for 4 days; c=toxic after the 2nd dose ChEMBL. 15801861
Mean survival time (functional) day Mean survival time taken as number of days before illness due to Plasmodium berghei in untreated mice; c=toxic after the 2nd dose ChEMBL. 15801861
Mean survival time (functional) c 0 day Mean survival time taken as number of days before illness due to Plasmodium berghei in untreated mice; c=toxic after the 2nd dose ChEMBL. 15801861
Mean survival time (functional) c 0 day Mean survival time taken as number of days before illness due to Plasmodium berghei when mice treated with 20 mg/kg dose for 4 days; c=toxic after the 2nd dose ChEMBL. 15801861
Parasitemia (functional) % In vivo antimalarial activity of compound against Plasmodium berghei in mice at dose of 20 mg/kg treated for 4 days; c = toxic after 2nd dose ChEMBL. 15801861
Parasitemia (functional) c 0 % In vivo antimalarial activity of compound against Plasmodium berghei in mice at dose of 20 mg/kg treated for 4 days; c = toxic after 2nd dose ChEMBL. 15801861
Ratio (functional) = 8.98 Ratio of cytotoxic to that of antiplasmodial activity of the compound was determined ChEMBL. 15801861
Ratio IC50 (functional) = 2.9 Resistance index, ratio of IC50 for chloroquine-resistant ring stage Plasmodium falciparum W2 to IC50 for chloroquine-sensitive ring stage Plasmodium falciparum 3D7 ChEMBL. 21207937
Ratio IC50 (functional) = 1.6 Ratio of IC50 for human HUVEC cells to IC50 for Plasmodium falciparum W2 ChEMBL. 18207399
Suppression of parasitemia (functional) % In vivo antimalarial activity of compound against Plasmodium berghei was determined as supression of parasitemia in mice at 20 mg/kg treated for 4 days; c=toxic after the 2nd dose ChEMBL. 15801861
Suppression of parasitemia (functional) c 0 % In vivo antimalarial activity of compound against Plasmodium berghei was determined as supression of parasitemia in mice at 20 mg/kg treated for 4 days; c=toxic after the 2nd dose ChEMBL. 15801861

Phenotypes

Whole-cell/tissue/organism interactions

Species name Source Reference Is orphan
Trypanosoma brucei gambiense 15921407
Plasmodium falciparum 15801861
Mus musculus ChEMBL23 10425120
Trypanosoma cruzi ChEMBL23 15921407
Homo sapiens ChEMBL23 17643990
Leishmania donovani ChEMBL23 15921407

Many chemical entities in TDR Targets come from high-throughput screenings with whole cells or tissue samples, and not all assayed compounds have been tested against a single a single target protein, probably because they get ruled out during screening process. Even if these compounds may have not been of interest in the original screening, they may come as interesting leads for other screening assays. Furthermore, we may be able to propose drug-target associations using chemical similarities and network patterns.

Annotated phenotypes:

We have no manually annotated phenotypes for this drug. What does this mean? / Care to help?
In TDR Targets, information about phenotypes that are caused by drugs, or by genetic manipulation of cells (e.g. gene knockouts or knockdowns) is manually curated from the literature. These descriptions help to describe the potential of the target for drug development. If no information is available for this gene or if the information is incomplete, this may mean that i) the papers containing this information either appeared after the curation effort for this organism was carried out or they were inadvertently missed by curators; or that ii) the curation effort for this organism has not yet started.
 
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External resources for this compound

Bibliographic References

16 literature references were collected for this gene.

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