IC50 (functional)
|
< 0.02 uM
|
In vitro antimalarial activity against Plasmodium falciparum Vl/S strain with quadruple mutation (N51I + C59R + S108N + I164L) DHFR, relative to trimethoprim
|
ChEMBL.
|
14711307
|
IC50 (functional)
|
< 0.02 uM
|
In vitro antimalarial activity against Plasmodium falciparum Vl/S strain with quadruple mutation (N51I + C59R + S108N + I164L) DHFR, relative to trimethoprim
|
ChEMBL.
|
14711307
|
IC50 (functional)
|
= 0.03 uM
|
In vitro antimalarial activity against Plasmodium falciparum K1CB1 strain with double mutation (C59R + S108N) DHFR, relative to trimethoprim
|
ChEMBL.
|
14711307
|
IC50 (functional)
|
= 0.03 uM
|
In vitro antimalarial activity against Plasmodium falciparum Csl-2 strain with triple mutation (C59R + S108N + I164L) DHFR, relative to trimethoprim
|
ChEMBL.
|
14711307
|
IC50 (functional)
|
= 0.03 uM
|
In vitro antimalarial activity against Plasmodium falciparum K1CB1 strain with double mutation (C59R + S108N) DHFR, relative to trimethoprim
|
ChEMBL.
|
14711307
|
IC50 (functional)
|
= 0.03 uM
|
In vitro antimalarial activity against Plasmodium falciparum Csl-2 strain with triple mutation (C59R + S108N + I164L) DHFR, relative to trimethoprim
|
ChEMBL.
|
14711307
|
IC50 (functional)
|
= 0.54 uM
|
In vitro antimalarial activity against Plasmodium falciparum TM4/8.2 strain with wild type DHFR, relative to trimethoprim
|
ChEMBL.
|
14711307
|
IC50 (functional)
|
= 0.54 uM
|
In vitro antimalarial activity against Plasmodium falciparum TM4/8.2 strain with wild type DHFR, relative to trimethoprim
|
ChEMBL.
|
14711307
|
IC50 (functional)
|
= 3 uM
|
Antimicrobial activity against Plasmodium falciparum
|
ChEMBL.
|
20185316
|
IC50 (functional)
|
= 3.02 uM
|
In vitro antimalarial activity against Plasmodium falciparum Vl/S strain with quadruple mutation (N51I + C59R + S108N + I164L) DHFR
|
ChEMBL.
|
14711307
|
IC50 (functional)
|
= 3.02 uM
|
In vitro antimalarial activity against Plasmodium falciparum Vl/S strain with quadruple mutation (N51I + C59R + S108N + I164L) DHFR
|
ChEMBL.
|
14711307
|
IC50 (functional)
|
= 3.46 uM
|
In vitro antimalarial activity against Plasmodium falciparum Csl-2 strain with triple mutation (C59R + S108N + I164L) DHFR
|
ChEMBL.
|
14711307
|
IC50 (functional)
|
= 3.46 uM
|
In vitro antimalarial activity against Plasmodium falciparum Csl-2 strain with triple mutation (C59R + S108N + I164L) DHFR
|
ChEMBL.
|
14711307
|
IC50 (functional)
|
= 3.57 uM
|
In vitro antimalarial activity against Plasmodium falciparum TM4/8.2 strain with wild type DHFR
|
ChEMBL.
|
14711307
|
IC50 (functional)
|
= 3.57 uM
|
In vitro antimalarial activity against Plasmodium falciparum TM4/8.2 strain with wild type DHFR
|
ChEMBL.
|
14711307
|
IC50 (functional)
|
= 3.6 uM
|
In vitro Antiplasmodial activity (IC50) against Plasmodium falciparum Clone with wild-type (TM4/8.2)
|
ChEMBL.
|
11881993
|
IC50 (functional)
|
= 3.6 uM
|
In vitro Antiplasmodial activity (IC50) against Plasmodium falciparum Clone with wild-type (TM4/8.2)
|
ChEMBL.
|
11881993
|
IC50 (functional)
|
= 4.18 uM
|
In vitro antimalarial activity against Plasmodium falciparum K1CB1 strain with double mutation (C59R + S108N) DHFR
|
ChEMBL.
|
14711307
|
IC50 (functional)
|
= 4.18 uM
|
In vitro antimalarial activity against Plasmodium falciparum K1CB1 strain with double mutation (C59R + S108N) DHFR
|
ChEMBL.
|
14711307
|
IC50 (functional)
|
= 4.2 uM
|
Antiplasmodial activity (IC50) against Plasmodium falciparum Clone with mutant enzyme C59R+S108N- pfDihydrofolate reductase (K1CB1)
|
ChEMBL.
|
11881993
|
IC50 (functional)
|
= 4.2 uM
|
Antiplasmodial activity (IC50) against Plasmodium falciparum Clone with mutant enzyme C59R+S108N- pfDihydrofolate reductase (K1CB1)
|
ChEMBL.
|
11881993
|
Ki (binding)
|
= 3.7 nM
|
Inhibitory activity against wild-type dihydrofolate reductase (S108N DHFR)
|
ChEMBL.
|
14711307
|
Ki (binding)
|
= 3.7 nM
|
Inhibition of the wild-type dihydrofolate reductase (DHFR)
|
ChEMBL.
|
11881993
|
Ki (binding)
|
= 3.7 nM
|
Inhibitory activity against wild-type dihydrofolate reductase (S108N DHFR)
|
ChEMBL.
|
14711307
|
Ki (binding)
|
= 3.7 nM
|
Inhibition of the wild-type dihydrofolate reductase (DHFR)
|
ChEMBL.
|
11881993
|
Ki (binding)
|
= 46.4 nM
|
Inhibition of the S108N mutant of dihydrofolate reductase (DHFR)
|
ChEMBL.
|
11881993
|
Ki (binding)
|
= 46.4 nM
|
Inhibition of the S108N mutant of dihydrofolate reductase (DHFR)
|
ChEMBL.
|
11881993
|
Ki (binding)
|
= 99.1 nM
|
Inhibitory activity against double mutant dihydrofolate reductase (C59R+S108N DHFR)
|
ChEMBL.
|
14711307
|
Ki (binding)
|
= 99.1 nM
|
Inhibition of the C59R+S108N mutant of dihydrofolate reductase (DHFR)
|
ChEMBL.
|
11881993
|
Ki (binding)
|
= 99.1 nM
|
Inhibitory activity against double mutant dihydrofolate reductase (C59R+S108N DHFR)
|
ChEMBL.
|
14711307
|
Ki (binding)
|
= 99.1 nM
|
Inhibition of the C59R+S108N mutant of dihydrofolate reductase (DHFR)
|
ChEMBL.
|
11881993
|
Ki (binding)
|
= 204.7 nM
|
Inhibitory activity against quadruple mutant dihydrofolate reductase (N51I C59R S108N I164L DHFR)
|
ChEMBL.
|
14711307
|
Ki (binding)
|
= 204.7 nM
|
Inhibitory activity against quadruple mutant dihydrofolate reductase (N51I C59R S108N I164L DHFR)
|
ChEMBL.
|
14711307
|
Ki (binding)
|
= 273.4 nM
|
Inhibitory activity against triple mutant dihydrofolate reductase (C59R S108 NI164L DHFR)
|
ChEMBL.
|
14711307
|
Ki (binding)
|
= 273.4 nM
|
Inhibitory activity against triple mutant dihydrofolate reductase (C59R S108 NI164L DHFR)
|
ChEMBL.
|
14711307
|
Ratio (functional)
|
= 1.2
|
IC50 ratio of the compound (K1CB1/TM4)
|
ChEMBL.
|
11881993
|
Ratio (binding)
|
= 12.5
|
Ratio of Inhibition of the S108N mutant of dihydrofolate reductase (DHFR) to inhibition of wild type dihydrofolate reductase.
|
ChEMBL.
|
11881993
|
Ratio (binding)
|
= 26.8
|
Ratio of Inhibition of the C59R+S108N mutant of dihydrofolate reductase (DHFR) to inhibition of wild type dihydrofolate reductase.
|
ChEMBL.
|
11881993
|
Ratio (functional)
|
= 1.2
|
IC50 ratio of the compound (K1CB1/TM4)
|
ChEMBL.
|
11881993
|
Ratio (binding)
|
= 12.5
|
Ratio of Inhibition of the S108N mutant of dihydrofolate reductase (DHFR) to inhibition of wild type dihydrofolate reductase.
|
ChEMBL.
|
11881993
|
Ratio (binding)
|
= 26.8
|
Ratio of Inhibition of the C59R+S108N mutant of dihydrofolate reductase (DHFR) to inhibition of wild type dihydrofolate reductase.
|
ChEMBL.
|
11881993
|
Relative activity (binding)
|
= 0.03
|
Inhibitory activity against quadruple mutant dihydrofolate reductase (N51I C59R S108N I164L DHFR), relative to trimethoprim
|
ChEMBL.
|
14711307
|
Relative activity (binding)
|
= 0.05
|
Inhibitory activity against triple mutant dihydrofolate reductase (C59R S108 NI164L DHFR), relative to trimethoprim
|
ChEMBL.
|
14711307
|
Relative activity (binding)
|
= 0.4
|
Inhibition of the C59R+S108N mutant of dihydrofolate reductase (DHFR)relative to Tmp
|
ChEMBL.
|
11881993
|
Relative activity (binding)
|
= 0.4
|
Inhibition of S108N mutant dihydrofolate reductase (DHFR)relative to Tmp
|
ChEMBL.
|
11881993
|
Relative activity (binding)
|
= 0.4
|
Inhibitory activity against wild-type dihydrofolate reductase (S108N DHFR), relative to trimethoprim
|
ChEMBL.
|
14711307
|
Relative activity (binding)
|
= 0.4
|
Inhibitory activity against double mutant dihydrofolate reductase (C59R S108N DHFR), relative to trimethoprim
|
ChEMBL.
|
14711307
|
Relative activity (binding)
|
= 0.4
|
Inhibition of the wild-type dihydrofolate reductase (DHFR) relative to Tmp
|
ChEMBL.
|
11881993
|
Relative activity (binding)
|
= 0.03
|
Inhibitory activity against quadruple mutant dihydrofolate reductase (N51I C59R S108N I164L DHFR), relative to trimethoprim
|
ChEMBL.
|
14711307
|
Relative activity (binding)
|
= 0.05
|
Inhibitory activity against triple mutant dihydrofolate reductase (C59R S108 NI164L DHFR), relative to trimethoprim
|
ChEMBL.
|
14711307
|
Relative activity (binding)
|
= 0.4
|
Inhibitory activity against wild-type dihydrofolate reductase (S108N DHFR), relative to trimethoprim
|
ChEMBL.
|
14711307
|
Relative activity (binding)
|
= 0.4
|
Inhibitory activity against double mutant dihydrofolate reductase (C59R S108N DHFR), relative to trimethoprim
|
ChEMBL.
|
14711307
|
Relative activity (binding)
|
= 0.4
|
Inhibition of the wild-type dihydrofolate reductase (DHFR) relative to Tmp
|
ChEMBL.
|
11881993
|
Relative activity (binding)
|
= 0.4
|
Inhibition of S108N mutant dihydrofolate reductase (DHFR)relative to Tmp
|
ChEMBL.
|
11881993
|
Relative activity (binding)
|
= 0.4
|
Inhibition of the C59R+S108N mutant of dihydrofolate reductase (DHFR)relative to Tmp
|
ChEMBL.
|
11881993
|