IC50 (functional)
|
= 0.04 uM
|
In vitro anti-plasmodial activity against Plasmodium falciparum with mutant A16V+S108T (T9/94RC17) dihydrofolate reductase.
|
ChEMBL.
|
14736247
|
IC50 (functional)
|
= 0.04 uM
|
In vitro anti-plasmodial activity against Plasmodium falciparum with mutant A16V+S108T (T9/94RC17) dihydrofolate reductase.
|
ChEMBL.
|
14736247
|
IC50 (functional)
|
= 0.12 uM
|
In vitro anti-plasmodial activity against Plasmodium falciparum with wild type dihydrofolate reductase (TM4/8.2).
|
ChEMBL.
|
14736247
|
IC50 (functional)
|
= 0.12 uM
|
In vitro anti-plasmodial activity against Plasmodium falciparum with wild type dihydrofolate reductase (TM4/8.2).
|
ChEMBL.
|
14736247
|
IC50 (functional)
|
= 3.1 uM
|
In vitro anti-plasmodial activity against Plasmodium falciparum with mutant C59R+S108N (K1CB1) dihydrofolate reductase.
|
ChEMBL.
|
14736247
|
IC50 (functional)
|
= 3.1 uM
|
In vitro anti-plasmodial activity against Plasmodium falciparum with mutant C59R+S108N (K1CB1) dihydrofolate reductase.
|
ChEMBL.
|
14736247
|
IC50 (functional)
|
= 3.2 uM
|
In vitro anti-plasmodial activity against Plasmodium falciparum with mutant N51I+C59R+S108N (W2) dihydrofolate reductase.
|
ChEMBL.
|
14736247
|
IC50 (functional)
|
= 3.2 uM
|
In vitro anti-plasmodial activity against Plasmodium falciparum with mutant N51I+C59R+S108N (W2) dihydrofolate reductase.
|
ChEMBL.
|
14736247
|
IC50 (functional)
|
= 4.8 uM
|
In vitro anti-plasmodial activity against Plasmodium falciparum with mutant C59R+S108N+I164L (Csl-2) dihydrofolate reductase.
|
ChEMBL.
|
14736247
|
IC50 (functional)
|
= 4.8 uM
|
In vitro anti-plasmodial activity against Plasmodium falciparum with mutant C59R+S108N+I164L (Csl-2) dihydrofolate reductase.
|
ChEMBL.
|
14736247
|
IC50 (functional)
|
= 6.9 uM
|
In vitro anti-plasmodial activity against Plasmodium falciparum with mutant CN51I+C59R+S108N+I164L (V1/S) dihydrofolate reductase.
|
ChEMBL.
|
14736247
|
IC50 (functional)
|
= 6.9 uM
|
In vitro anti-plasmodial activity against Plasmodium falciparum with mutant CN51I+C59R+S108N+I164L (V1/S) dihydrofolate reductase.
|
ChEMBL.
|
14736247
|
IC50 (functional)
|
= 7 uM
|
In vitro cytotoxicity against Plasmodium falciparum infected KB cell line
|
ChEMBL.
|
14736247
|
IC50 (functional)
|
= 7 uM
|
In vitro cytotoxicity against Plasmodium falciparum infected KB cell line
|
ChEMBL.
|
14736247
|
IC50 (functional)
|
= 7 uM
|
Antimicrobial activity against Plasmodium falciparum
|
ChEMBL.
|
20185316
|
IC50 (functional)
|
= 8.6 uM
|
In vitro cytotoxicity against Plasmodium falciparum infected BC cell line.
|
ChEMBL.
|
14736247
|
IC50 (functional)
|
> 50 uM
|
In vitro cytotoxicity against Plasmodium falciparum infected vero cell line.
|
ChEMBL.
|
14736247
|
Ki (binding)
|
= 0.4 nM
|
Binding affinity towards wild-type dihydrofolate reductase of Plasmodium falciparum.
|
ChEMBL.
|
14736247
|
Ki (binding)
|
= 0.4 nM
|
Binding affinity towards wild-type dihydrofolate reductase of Plasmodium falciparum.
|
ChEMBL.
|
14736247
|
Ki (binding)
|
= 3.8 nM
|
Binding affinity towards mutant dihydrofolate reductase (A16V+S108T DHFR) of Plasmodium falciparum.
|
ChEMBL.
|
14736247
|
Ki (binding)
|
= 3.8 nM
|
Binding affinity towards mutant dihydrofolate reductase (A16V+S108T DHFR) of Plasmodium falciparum.
|
ChEMBL.
|
14736247
|
Ki (binding)
|
= 29.3 nM
|
Binding affinity towards mutant dihydrofolate reductase (N51I+C59R+S108N DHFR) of Plasmodium falciparum
|
ChEMBL.
|
14736247
|
Ki (binding)
|
= 29.3 nM
|
Binding affinity towards mutant dihydrofolate reductase (N51I+C59R+S108N DHFR) of Plasmodium falciparum
|
ChEMBL.
|
14736247
|
Ki (binding)
|
= 145 nM
|
Binding affinity towards mutant dihydrofolate reductase (C59R+S108N+I164L DHFR) of Plasmodium falciparum
|
ChEMBL.
|
14736247
|
Ki (binding)
|
= 145 nM
|
Binding affinity towards mutant dihydrofolate reductase (C59R+S108N+I164L DHFR) of Plasmodium falciparum
|
ChEMBL.
|
14736247
|
Ki (binding)
|
= 222 nM
|
Binding affinity towards mutant dihydrofolate reductase (N51I+C59R+S108N+I164L DHFR) of Plasmodium falciparum
|
ChEMBL.
|
14736247
|
Ki (binding)
|
= 222 nM
|
Binding affinity towards mutant dihydrofolate reductase (N51I+C59R+S108N+I164L DHFR) of Plasmodium falciparum
|
ChEMBL.
|
14736247
|
Ratio (binding)
|
= 9.5
|
Ratio of binding affinity of compound for mutant (A16V+S108T) to that of wild type dihydrofolate reductase
|
ChEMBL.
|
14736247
|
Ratio (binding)
|
= 73.1
|
Ratio of binding affinity of compound for mutant (N51I+C59R+S108N) to that of wild type dihydrofolate reductase
|
ChEMBL.
|
14736247
|
Ratio (binding)
|
= 363
|
Ratio of binding affinity of compound for mutant (C59R+S108N+I164L) to that of wild type dihydrofolate reductase
|
ChEMBL.
|
14736247
|
Ratio (binding)
|
= 555
|
Ratio of binding affinity of compound for mutant (N51I+C59R+S108N+I164L) to that of wild type dihydrofolate reductase
|
ChEMBL.
|
14736247
|
Ratio (binding)
|
= 9.5
|
Ratio of binding affinity of compound for mutant (A16V+S108T) to that of wild type dihydrofolate reductase
|
ChEMBL.
|
14736247
|
Ratio (binding)
|
= 73.1
|
Ratio of binding affinity of compound for mutant (N51I+C59R+S108N) to that of wild type dihydrofolate reductase
|
ChEMBL.
|
14736247
|
Ratio (binding)
|
= 363
|
Ratio of binding affinity of compound for mutant (C59R+S108N+I164L) to that of wild type dihydrofolate reductase
|
ChEMBL.
|
14736247
|
Ratio (binding)
|
= 555
|
Ratio of binding affinity of compound for mutant (N51I+C59R+S108N+I164L) to that of wild type dihydrofolate reductase
|
ChEMBL.
|
14736247
|
Safety ratio (functional)
|
= 1
|
Ratio of cytotoxicity to that of anti-plasmodial activity against Plasmodium falciparum (V1/S) infected KB cell line
|
ChEMBL.
|
14736247
|
Safety ratio (functional)
|
= 1.2
|
Ratio of cytotoxicity to that of anti-plasmodial activity against Plasmodium falciparum (V1/S) infected BC cell line
|
ChEMBL.
|
14736247
|
Safety ratio (functional)
|
= 1.5
|
Ratio of cytotoxicity to that of anti-plasmodial activity against Plasmodium falciparum (Csl-2) infected KB cell line
|
ChEMBL.
|
14736247
|
Safety ratio (functional)
|
= 1.8
|
Ratio of cytotoxicity to that of anti-plasmodial activity against Plasmodium falciparum (Csl-2) infected BC cell line
|
ChEMBL.
|
14736247
|
Safety ratio (functional)
|
> 7.2
|
Ratio of cytotoxicity to that of anti-plasmodial activity against Plasmodium falciparum (V1/S) infected vero cell line
|
ChEMBL.
|
14736247
|
Safety ratio (functional)
|
> 10.4
|
Ratio of cytotoxicity to that of anti-plasmodial activity against Plasmodium falciparum (Csl-2) infected vero cell line
|
ChEMBL.
|
14736247
|
Safety ratio (functional)
|
= 58.3
|
Ratio of cytotoxicity to that of anti-plasmodial activity against Plasmodium falciparum (TM4/8.2) infected KB cell line
|
ChEMBL.
|
14736247
|
Safety ratio (functional)
|
= 71.7
|
Ratio of cytotoxicity to that of anti-plasmodial activity against Plasmodium falciparum (TM4/8.2) infected BC cell line
|
ChEMBL.
|
14736247
|
Safety ratio (functional)
|
> 417
|
Ratio of cytotoxicity versus anti-plasmodial activity against Plasmodium falciparum (TM4/8.2) infected vero cell line
|
ChEMBL.
|
14736247
|