IC50 (functional)
|
uM
|
In vitro anti-plasmodial activity against Plasmodium falciparum with mutant A16V+S108T (T9/94RC17) dihydrofolate reductase.
|
ChEMBL.
|
14736247
|
IC50 (functional)
|
ND 0 uM
|
In vitro anti-plasmodial activity against Plasmodium falciparum with mutant A16V+S108T (T9/94RC17) dihydrofolate reductase.
|
ChEMBL.
|
14736247
|
IC50 (functional)
|
= 0.06 uM
|
In vitro anti-plasmodial activity against Plasmodium falciparum with wild type dihydrofolate reductase (TM4/8.2).
|
ChEMBL.
|
14736247
|
IC50 (functional)
|
= 0.06 uM
|
In vitro anti-plasmodial activity against Plasmodium falciparum with wild type dihydrofolate reductase (TM4/8.2).
|
ChEMBL.
|
14736247
|
IC50 (functional)
|
= 0.48 uM
|
In vitro anti-plasmodial activity against Plasmodium falciparum with mutant C59R+S108N (K1CB1) dihydrofolate reductase.
|
ChEMBL.
|
14736247
|
IC50 (functional)
|
= 0.48 uM
|
In vitro anti-plasmodial activity against Plasmodium falciparum with mutant C59R+S108N (K1CB1) dihydrofolate reductase.
|
ChEMBL.
|
14736247
|
IC50 (functional)
|
= 0.49 uM
|
In vitro anti-plasmodial activity against Plasmodium falciparum with mutant C59R+S108N+I164L (Csl-2) dihydrofolate reductase.
|
ChEMBL.
|
14736247
|
IC50 (functional)
|
= 0.49 uM
|
In vitro anti-plasmodial activity against Plasmodium falciparum with mutant C59R+S108N+I164L (Csl-2) dihydrofolate reductase.
|
ChEMBL.
|
14736247
|
IC50 (functional)
|
= 0.51 uM
|
In vitro anti-plasmodial activity against Plasmodium falciparum with mutant N51I+C59R+S108N (W2) dihydrofolate reductase.
|
ChEMBL.
|
14736247
|
IC50 (functional)
|
= 0.51 uM
|
In vitro anti-plasmodial activity against Plasmodium falciparum with mutant N51I+C59R+S108N (W2) dihydrofolate reductase.
|
ChEMBL.
|
14736247
|
IC50 (functional)
|
= 2.2 uM
|
In vitro cytotoxicity against Plasmodium falciparum infected BC cell line.
|
ChEMBL.
|
14736247
|
IC50 (functional)
|
= 3 uM
|
Antimicrobial activity against Plasmodium falciparum
|
ChEMBL.
|
20185316
|
IC50 (functional)
|
= 3.2 uM
|
In vitro anti-plasmodial activity against Plasmodium falciparum with mutant CN51I+C59R+S108N+I164L (V1/S) dihydrofolate reductase.
|
ChEMBL.
|
14736247
|
IC50 (functional)
|
= 3.2 uM
|
In vitro anti-plasmodial activity against Plasmodium falciparum with mutant CN51I+C59R+S108N+I164L (V1/S) dihydrofolate reductase.
|
ChEMBL.
|
14736247
|
IC50 (functional)
|
= 4 uM
|
In vitro cytotoxicity against Plasmodium falciparum infected KB cell line
|
ChEMBL.
|
14736247
|
IC50 (functional)
|
= 4 uM
|
In vitro cytotoxicity against Plasmodium falciparum infected KB cell line
|
ChEMBL.
|
14736247
|
IC50 (functional)
|
= 230 uM
|
In vitro cytotoxicity against Plasmodium falciparum infected vero cell line.
|
ChEMBL.
|
14736247
|
Ki (binding)
|
= 2.4 nM
|
Binding affinity towards wild-type dihydrofolate reductase of Plasmodium falciparum.
|
ChEMBL.
|
14736247
|
Ki (binding)
|
= 2.4 nM
|
Binding affinity towards wild-type dihydrofolate reductase of Plasmodium falciparum.
|
ChEMBL.
|
14736247
|
Ki (binding)
|
= 5.5 nM
|
Binding affinity towards mutant dihydrofolate reductase (N51I+C59R+S108N DHFR) of Plasmodium falciparum
|
ChEMBL.
|
14736247
|
Ki (binding)
|
= 5.5 nM
|
Binding affinity towards mutant dihydrofolate reductase (N51I+C59R+S108N DHFR) of Plasmodium falciparum
|
ChEMBL.
|
14736247
|
Ki (binding)
|
= 12.1 nM
|
Binding affinity towards mutant dihydrofolate reductase (C59R+S108N+I164L DHFR) of Plasmodium falciparum
|
ChEMBL.
|
14736247
|
Ki (binding)
|
= 12.1 nM
|
Binding affinity towards mutant dihydrofolate reductase (C59R+S108N+I164L DHFR) of Plasmodium falciparum
|
ChEMBL.
|
14736247
|
Ki (binding)
|
= 15.9 nM
|
Binding affinity towards mutant dihydrofolate reductase (N51I+C59R+S108N+I164L DHFR) of Plasmodium falciparum
|
ChEMBL.
|
14736247
|
Ki (binding)
|
= 15.9 nM
|
Binding affinity towards mutant dihydrofolate reductase (N51I+C59R+S108N+I164L DHFR) of Plasmodium falciparum
|
ChEMBL.
|
14736247
|
Ki (binding)
|
= 101 nM
|
Binding affinity towards mutant dihydrofolate reductase (A16V+S108T DHFR) of Plasmodium falciparum.
|
ChEMBL.
|
14736247
|
Ki (binding)
|
= 101 nM
|
Binding affinity towards mutant dihydrofolate reductase (A16V+S108T DHFR) of Plasmodium falciparum.
|
ChEMBL.
|
14736247
|
Ratio (binding)
|
= 2.3
|
Ratio of binding affinity of compound for mutant (N51I+C59R+S108N) to that of wild type dihydrofolate reductase
|
ChEMBL.
|
14736247
|
Ratio (binding)
|
= 5
|
Ratio of binding affinity of compound for mutant (C59R+S108N+I164L) to that of wild type dihydrofolate reductase
|
ChEMBL.
|
14736247
|
Ratio (binding)
|
= 6.58
|
Ratio of binding affinity of compound for mutant (N51I+C59R+S108N+I164L) to that of wild type dihydrofolate reductase
|
ChEMBL.
|
14736247
|
Ratio (binding)
|
= 41.9
|
Ratio of binding affinity of compound for mutant (A16V+S108T) to that of wild type dihydrofolate reductase
|
ChEMBL.
|
14736247
|
Ratio (binding)
|
= 2.3
|
Ratio of binding affinity of compound for mutant (N51I+C59R+S108N) to that of wild type dihydrofolate reductase
|
ChEMBL.
|
14736247
|
Ratio (binding)
|
= 5
|
Ratio of binding affinity of compound for mutant (C59R+S108N+I164L) to that of wild type dihydrofolate reductase
|
ChEMBL.
|
14736247
|
Ratio (binding)
|
= 6.58
|
Ratio of binding affinity of compound for mutant (N51I+C59R+S108N+I164L) to that of wild type dihydrofolate reductase
|
ChEMBL.
|
14736247
|
Ratio (binding)
|
= 41.9
|
Ratio of binding affinity of compound for mutant (A16V+S108T) to that of wild type dihydrofolate reductase
|
ChEMBL.
|
14736247
|
Safety ratio (functional)
|
= 0.7
|
Ratio of cytotoxicity to that of anti-plasmodial activity against Plasmodium falciparum (V1/S) infected BC cell line
|
ChEMBL.
|
14736247
|
Safety ratio (functional)
|
= 1.3
|
Ratio of cytotoxicity to that of anti-plasmodial activity against Plasmodium falciparum (V1/S) infected KB cell line
|
ChEMBL.
|
14736247
|
Safety ratio (functional)
|
= 4.5
|
Ratio of cytotoxicity to that of anti-plasmodial activity against Plasmodium falciparum (Csl-2) infected BC cell line
|
ChEMBL.
|
14736247
|
Safety ratio (functional)
|
= 8.2
|
Ratio of cytotoxicity to that of anti-plasmodial activity against Plasmodium falciparum (Csl-2) infected KB cell line
|
ChEMBL.
|
14736247
|
Safety ratio (functional)
|
= 36.7
|
Ratio of cytotoxicity to that of anti-plasmodial activity against Plasmodium falciparum (TM4/8.2) infected BC cell line
|
ChEMBL.
|
14736247
|
Safety ratio (functional)
|
= 66.7
|
Ratio of cytotoxicity to that of anti-plasmodial activity against Plasmodium falciparum (TM4/8.2) infected KB cell line
|
ChEMBL.
|
14736247
|
Safety ratio (functional)
|
= 71.9
|
Ratio of cytotoxicity to that of anti-plasmodial activity against Plasmodium falciparum (V1/S) infected vero cell line
|
ChEMBL.
|
14736247
|
Safety ratio (functional)
|
= 469
|
Ratio of cytotoxicity to that of anti-plasmodial activity against Plasmodium falciparum (Csl-2) infected vero cell line
|
ChEMBL.
|
14736247
|
Safety ratio (functional)
|
= 3833
|
Ratio of cytotoxicity versus anti-plasmodial activity against Plasmodium falciparum (TM4/8.2) infected vero cell line
|
ChEMBL.
|
14736247
|