IC50 (functional)
|
= 0.04 uM
|
In vitro Antiplasmodial activity (IC50) against Plasmodium falciparum Clone with wild-type (TM4/8.2)
|
ChEMBL.
|
11881993
|
IC50 (functional)
|
= 0.04 uM
|
In vitro Antiplasmodial activity (IC50) against Plasmodium falciparum Clone with wild-type (TM4/8.2)
|
ChEMBL.
|
11881993
|
IC50 (functional)
|
= 22.3 uM
|
Antiplasmodial activity (IC50) against Plasmodium falciparum Clone with mutant enzyme C59R+S108N- pfDihydrofolate reductase (K1CB1)
|
ChEMBL.
|
11881993
|
IC50 (functional)
|
= 22.3 uM
|
Antiplasmodial activity (IC50) against Plasmodium falciparum Clone with mutant enzyme C59R+S108N- pfDihydrofolate reductase (K1CB1)
|
ChEMBL.
|
11881993
|
Ki (binding)
|
= 0.14 nM
|
Inhibition constant against Plasmodium falciparum dihydrofolate reductase
|
ChEMBL.
|
15293997
|
Ki (binding)
|
= 0.14 nM
|
Inhibition constant against Plasmodium falciparum dihydrofolate reductase
|
ChEMBL.
|
15293997
|
Ki (binding)
|
= 0.3 nM
|
Inhibition of the wild-type dihydrofolate reductase (DHFR)
|
ChEMBL.
|
11881993
|
Ki (binding)
|
= 0.3 nM
|
Binding affinity towards wild-type dihydrofolate reductase of Plasmodium falciparum.
|
ChEMBL.
|
14736247
|
Ki (binding)
|
= 0.3 nM
|
Inhibition of the wild-type dihydrofolate reductase (DHFR)
|
ChEMBL.
|
11881993
|
Ki (binding)
|
= 0.3 nM
|
Binding affinity towards wild-type dihydrofolate reductase of Plasmodium falciparum.
|
ChEMBL.
|
14736247
|
Ki (binding)
|
= 16.9 nM
|
Inhibition of the S108N mutant of dihydrofolate reductase (DHFR)
|
ChEMBL.
|
11881993
|
Ki (binding)
|
= 16.9 nM
|
Inhibition of the S108N mutant of dihydrofolate reductase (DHFR)
|
ChEMBL.
|
11881993
|
Ki (binding)
|
= 27.4 nM
|
Inhibition of the C59R+S108N mutant of dihydrofolate reductase (DHFR)
|
ChEMBL.
|
11881993
|
Ki (binding)
|
= 27.4 nM
|
Inhibition of the C59R+S108N mutant of dihydrofolate reductase (DHFR)
|
ChEMBL.
|
11881993
|
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)
|
= 360 nM
|
Binding affinity towards mutant dihydrofolate reductase (N51I+C59R+S108N+I164L DHFR) of Plasmodium falciparum
|
ChEMBL.
|
14736247
|
Ki (binding)
|
= 360 nM
|
Binding affinity towards mutant dihydrofolate reductase (N51I+C59R+S108N+I164L DHFR) of Plasmodium falciparum
|
ChEMBL.
|
14736247
|
Ratio (binding)
|
= 97.7
|
Ratio of binding affinity of compound for mutant (N51I+C59R+S108N) to that of wild type dihydrofolate reductase
|
ChEMBL.
|
14736247
|
Ratio (binding)
|
= 483
|
Ratio of binding affinity of compound for mutant (C59R+S108N+I164L) to that of wild type dihydrofolate reductase
|
ChEMBL.
|
14736247
|
Ratio (functional)
|
= 557.5
|
IC50 ratio of the compound (K1CB1/TM4)
|
ChEMBL.
|
11881993
|
Ratio (binding)
|
= 1200
|
Ratio of binding affinity of compound for mutant (N51I+C59R+S108N+I164L) to that of wild type dihydrofolate reductase
|
ChEMBL.
|
14736247
|
Ratio (binding)
|
= 56.3
|
Ratio of Inhibition of the S108N mutant of dihydrofolate reductase (DHFR) to inhibition of wild type dihydrofolate reductase.
|
ChEMBL.
|
11881993
|
Ratio (binding)
|
= 91.3
|
Ratio of Inhibition of the C59R+S108N mutant of dihydrofolate reductase (DHFR) to inhibition of wild type dihydrofolate reductase.
|
ChEMBL.
|
11881993
|
Ratio (binding)
|
= 97.7
|
Ratio of binding affinity of compound for mutant (N51I+C59R+S108N) to that of wild type dihydrofolate reductase
|
ChEMBL.
|
14736247
|
Ratio (binding)
|
= 483
|
Ratio of binding affinity of compound for mutant (C59R+S108N+I164L) to that of wild type dihydrofolate reductase
|
ChEMBL.
|
14736247
|
Ratio (functional)
|
= 557.5
|
IC50 ratio of the compound (K1CB1/TM4)
|
ChEMBL.
|
11881993
|
Ratio (binding)
|
= 1200
|
Ratio of binding affinity of compound for mutant (N51I+C59R+S108N+I164L) to that of wild type dihydrofolate reductase
|
ChEMBL.
|
14736247
|
Relative activity (binding)
|
= 0.5
|
Inhibition of Plasmodium falciparum wild-type dihydrofolate reductase (DHFR) relative to Pyrimethamine.
|
ChEMBL.
|
11881993
|
Relative activity (binding)
|
= 0.5
|
Inhibition of mutant C59R+S108N dihydrofolate reductase (DHFR) relative to Pyr
|
ChEMBL.
|
11881993
|
Relative activity (binding)
|
= 0.6
|
Inhibition of mutant S108N dihydrofolate reductase (DHFR) relative to Pyr
|
ChEMBL.
|
11881993
|