Compound was tested for effective concentration against C8166 cell line
|
Homo sapiens
|
2.0
nM
|
|
Inhibitory effects on HIV-1 induced syncytium formation in C8166 cells
|
Human immunodeficiency virus 1
|
0.6
nM
|
|
Antiviral activity in HIV-infected CEM cells using whole cell assay
|
Homo sapiens
|
2.0
nM
|
|
Inhibitory concentration required for antiviral activity against HXB-2 infected CEM-SS cells
|
Homo sapiens
|
6.6
nM
|
|
Tested for the inhibitory activity against HIV-1 in H-9 cell lines assessed by syncytium formation and reverse transcriptase assay
|
Homo sapiens
|
20.0
nM
|
|
In vitro inhibition HIV-1 IIIB protease.
|
None
|
0.2
nM
|
|
In vitro antiviral activity against human immuno deficiency virus was determined
|
Human immunodeficiency virus 1
|
2.0
nM
|
|
Compound was tested for its inhibitory potency against human immunodeficiency virus -1 (HIV-1 protease); In house preparation
|
None
|
0.12
nM
|
|
Compound was tested for inhibitory activity against HIV-1 protease
|
None
|
270.0
nM
|
|
In vitro inhibition of HIV-1 protease.
|
None
|
1.0
nM
|
|
Inhibitory activity against HIV-1 protease using scintillation proximity assay (SPA assay)
|
None
|
45.0
nM
|
|
Inhibitory concentration required against HIV-1 protease
|
None
|
1.0
nM
|
|
Inhibitory activity against human immunodeficiency virus protease (HIVP) using protease inhibition assay
|
None
|
1.7
nM
|
|
Inhibitory activity against wild type strain,HIV104pre.
|
Human immunodeficiency virus
|
19.0
nM
|
|
Anti-HIV activity based on inhibition of HIV-1 induced cytopathogenicity in MT-2 cells.
|
Homo sapiens
|
17.0
nM
|
|
Concentration required for anti-viral activity (Anti-HIV-IIIB activity) against human T lymphoid (MT-2) cells that are infected with HIV-IIIB virus
|
Homo sapiens
|
3.0
nM
|
|
Inhibition of cytopathic effect of HIV-1 strain RF in MT-4 cell culture
|
None
|
4.0
nM
|
|
Compound was tested for effective concentration against MT-4 cell line
|
Homo sapiens
|
2.0
nM
|
|
Antiviral activity against HIV-1 resistant to 2-(2-Benzoyl-4-chloro-phenyl)-N-[4-(3-dimethylamino-propoxy)-2-methyl-phenyl]-acetamide in MT-4 cells
|
Homo sapiens
|
0.0038
ug.mL-1
|
|
Antiviral activity against HIV-1 (strain RF) infected MT-4 cells
|
Human immunodeficiency virus 1
|
0.028
ug.mL-1
|
|
Compound was evaluated for its antiviral inhibition in MT-4 cell culture
|
Homo sapiens
|
20.0
nM
|
|
Cytotoxicity against uninfected MT-4 cells
|
Homo sapiens
|
1.0
ug.mL-1
|
|
Cytotoxicity against uninfected MT-4 cells
|
Homo sapiens
|
1.0
ug.mL-1
|
|
Effective concentration against HIV infected MT-2 cell line
|
Homo sapiens
|
5.0
nM
|
|
Inhibition of P-gp was determined using rhodamine-assay in human CaCo-2 cells
|
None
|
43.0
%
|
|
Anti-HIV activity against multidrug resistant HIV JSL strain by inhibition of HIV p24 antigen expression in peripheral blood mononuclear cells(PBMC)
|
Homo sapiens
|
550.0
nM
|
|
Anti-HIV activity against multidrug resistant HIV MM strain by inhibition of HIV p24 antigen expression in peripheral blood mononuclear cells(PBMC)
|
Homo sapiens
|
320.0
nM
|
|
Anti-HIV activity against multidrug resistant HIV TM strain by inhibition of HIV p24 antigen expression in peripheral blood mononuclear cells(PBMC)
|
Homo sapiens
|
230.0
nM
|
|
Compound was evaluated for binding affinity against HIV protease
|
None
|
1.4
nM
|
|
Inhibition of HIV protease
|
Human immunodeficiency virus 1
|
0.04
nM
|
|
Binding affinity to inhibit the purified wild-type HIV-1 Protease
|
Human immunodeficiency virus 1
|
0.25
nM
|
|
Inhibition constant against HIV-1 Protease
|
Human immunodeficiency virus 1
|
0.23
nM
|
|
Inhibitory activity against HIV-1 protease
|
None
|
0.19
nM
|
|
Inhibitory concentration against HIV-1 protease
|
Human immunodeficiency virus 1
|
0.23
nM
|
|
Inhibitory activity against HIV-1 protease.
|
Human immunodeficiency virus 1
|
0.2291
nM
|
|
Inhibition of HIV-1 protease was determined in vitro
|
None
|
0.2291
nM
|
|
Inhibitory potency against HIV-1 protease
|
Human immunodeficiency virus 1
|
0.3999
nM
|
|
Binding affinity to HIV-1 protease
|
None
|
0.1202
nM
|
|
Compound was evaluated for inhibitory activity against HIV-2 protease
|
Human immunodeficiency virus 2
|
0.5
nM
|
|
Tested for inhibitory concentration against HIV-2 protease
|
Human immunodeficiency virus 2
|
0.5
nM
|
|
Inhibitory activity against HIV-1 Protease
|
Human immunodeficiency virus 1
|
11.2
nM
|
|
In vitro inhibition of HIV protease, using a peptide hydrolysis assay
|
None
|
0.34
nM
|
|
In vitro inhibitory activity against HIV proteinase
|
Human immunodeficiency virus 1
|
11.0
nM
|
|
In vivo antiviral activity (IC50) against HIV-1 protease.
|
Human immunodeficiency virus 1
|
6.3
nM
|
|
Concentration required for inhibitory activity against HIV-1 Protease
|
None
|
30.0
nM
|
|
Inhibitory activity against HIV-1 Protease was determined
|
None
|
0.4
nM
|
|
Inhibitory activity against HIV-1 protease
|
Human immunodeficiency virus 1
|
1.8
nM
|
|
Tested against S2-binding site of HIV-1 protease
|
Human immunodeficiency virus 1
|
0.23
nM
|
|
Tested for inhibitory concentration against HIV-1 protease
|
None
|
0.23
nM
|
|
Tested for inhibitory concentration against HIV-1 protease in experiment 2
|
None
|
0.4
nM
|
|
Equilibrium constant for the interaction between inhibitor and HIV-1 Protease
|
Human immunodeficiency virus 1
|
0.315
nM
|
|
Affinity against HIV protease
|
Human immunodeficiency virus 1
|
0.25
nM
|
|
Binding activity against HIV-1 Protease
|
Human immunodeficiency virus 1
|
0.4
nM
|
|
Binding activity against HIV-1 Protease
|
Human immunodeficiency virus 1
|
0.4
nM
|
|
Binding activity against HIV-1 Protease
|
human immunodeficiency virus type i
|
0.12
nM
|
|
The compound was tested for binding activity against HIV-1 protease
|
human immunodeficiency virus type i
|
0.12
nM
|
|
Inhibitory activity against P2 site in HIV protease.
|
Human immunodeficiency virus 1
|
0.452
nM
|
|
Inhibitory activity against HIV-1 protease
|
Human immunodeficiency virus 1
|
0.25
nM
|
|
Tested for the inhibitory activity against HIV-1 in Sup T1 cell lines assessed by syncytium formation and reverse transcriptase assay
|
Homo sapiens
|
20.0
nM
|
|
Dissociation constant obtained by inhibition of Wild-type protease
|
None
|
0.062
nM
|
|
Dissociation constant obtained by inhibition of mutant HIV-protease (A-44)
|
None
|
15.0
nM
|
|
Dissociation constant obtained by inhibition of mutant HIV-protease (K-60)
|
None
|
3.7
nM
|
|
Dissociation constant obtained by inhibition of mutant HIV-protease (V-18)
|
None
|
117.0
nM
|
|
Inhibitory activity in cell culture against both HIV-1 and HIV-2 viruses
|
None
|
30.0
nM
|
|
Binding affinity for human immunodeficiency virus type 1 protease
|
Human immunodeficiency virus 1
|
0.31
nM
|
|
Inhibition constant for human immunodeficiency virus type 1 protease
|
Human immunodeficiency virus 1
|
0.23
nM
|
|
Compound tested for the inhibition of HIV-induced cytopathogenicity in MT-2 cells
|
Homo sapiens
|
12.0
nM
|
|
Antiviral activity against HIV1 HXB2 in MT4 cells
|
None
|
60.0
nM
|
|
Antiviral activity against HIV1 EP13 in MT4 cells
|
None
|
80.0
nM
|
|
Antiviral activity against HIV D545701 in MT4 cells
|
None
|
603.0
nM
|
|
Antiviral activity against HIV1 IIIB strain in MT2 cells
|
None
|
5.0
nM
|
|
Antiviral activity against HIV1 LAI isolate in human MT2 cells
|
Human immunodeficiency virus 1
|
24.0
nM
|
|
Antiviral activity against HIV1 LAI isolate in human PHA-PBMC cells
|
Human immunodeficiency virus 1
|
14.0
nM
|
|
Antiviral activity against HIV1 BA-L isolate in human PHA-PBMC cells
|
Human immunodeficiency virus 1
|
18.0
nM
|
|
Antiviral activity against HIV2 EHO isolate in human MT2 cells
|
Human immunodeficiency virus 2
|
1.9
nM
|
|
Antiviral activity against multi drug-resistant HIV1 ET variant in human PHA-PBMC cells
|
Human immunodeficiency virus 1
|
17.0
nM
|
|
Antiviral activity against multi drug-resistant HIV1 B variant in human PHA-PBMC cells
|
Human immunodeficiency virus 1
|
230.0
nM
|
|
Antiviral activity against multi drug-resistant HIV1 C variant in human PHA-PBMC cells
|
Human immunodeficiency virus 1
|
100.0
nM
|
|
Antiviral activity against multi drug-resistant HIV1 G variant in human PHA-PBMC cells
|
Human immunodeficiency virus 1
|
59.0
nM
|
|
Antiviral activity against multi drug-resistant HIV1 TM variant in human PHA-PBMC cells
|
Human immunodeficiency virus 1
|
250.0
nM
|
|
Antiviral activity against multi drug-resistant HIV1 K variant in human PHA-PBMC cells
|
Human immunodeficiency virus 1
|
20.0
nM
|
|
Antimalarial activity against Plasmodium falciparum Dd2
|
Plasmodium falciparum
|
960.0
nM
|
|
Inhibition of HIV1 Protease M1 variant by FRET based assay
|
Human immunodeficiency virus 1
|
89.53
nM
|
|
Inhibition of HIV1 Protease M2 variant by FRET based assay
|
Human immunodeficiency virus 1
|
1.03
nM
|
|
Inhibition of HIV1 Protease M3 variant by FRET based assay
|
Human immunodeficiency virus 1
|
78.44
nM
|
|
Antiviral activity against HIV1 infected MT4 cells by MTT method
|
Human immunodeficiency virus 1
|
10.0
nM
|
|
Inhibition of wild type HIV1 recombinant aspartic protease
|
Human immunodeficiency virus 1
|
0.4
nM
|
|
Inhibition of HIV1 protease
|
Human immunodeficiency virus 1
|
0.138
nM
|
|
Antiviral activity against HIV1 3B
|
Human immunodeficiency virus 1
|
7.0
nM
|
|
Antiviral activity against HIV1 3B in presence of 50% human serum
|
Human immunodeficiency virus 1
|
50.0
nM
|
|
Antiviral activity against wild type HIV1
|
Human immunodeficiency virus 1
|
1.9
nM
|
|
Antiviral activity against HIV1 mutant strain 1
|
Human immunodeficiency virus 1
|
500.0
nM
|
|
Antiviral activity against HIV1 mutant strain 2
|
Human immunodeficiency virus 1
|
97.0
nM
|
|
Antiviral activity against HIV1 mutant strain 3
|
Human immunodeficiency virus 1
|
500.0
nM
|
|
Antiviral activity against HIV1 mutant strain 4
|
Human immunodeficiency virus 1
|
500.0
nM
|
|
Antiviral activity against HIV1 mutant strain 5
|
Human immunodeficiency virus 1
|
500.0
nM
|
|
Antiviral activity against HIV1 mutant strain 6
|
Human immunodeficiency virus 1
|
158.0
nM
|
|
Antiviral activity against HIV1 mutant strain 7
|
Human immunodeficiency virus 1
|
141.0
nM
|
|
Antiviral activity against HIV1 LAI in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 1
|
8.0
nM
|
|
Antiviral activity against HIV2 EHO in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 2
|
3.0
nM
|
|
Antiviral activity against HIV2 ROD in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 2
|
4.3
nM
|
|
Antiviral activity against HIV1 NL4-3 in MT4 cells by MTT assay
|
Human immunodeficiency virus 1
|
7.0
nM
|
|
Antiviral activity against ritonavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 1
|
10.0
nM
|
|
Antiviral activity against idinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 1
|
59.0
nM
|
|
Antiviral activity against nelfinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 1
|
24.0
nM
|
|
Antiviral activity against atazanavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 1
|
31.0
nM
|
|
Antiviral activity against lopinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 1
|
32.0
nM
|
|
Antiviral activity against amprenavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 1
|
37.0
nM
|
|
Antiviral activity against HIV1 GRL98065p20 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 1
|
12.0
nM
|
|
Antiviral activity against HIV1 GRL98065p30 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 1
|
22.0
nM
|
|
Antiviral activity against HIV1 GRL98065p40 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 1
|
32.0
nM
|
|
Antiviral activity against wild type HIV1 ERS104prc X4 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 1
|
8.0
nM
|
|
Antiviral activity against HIV1 MDR/TM X4 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 1
|
180.0
nM
|
|
Antiviral activity against HIV1 MDR/MM R5 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 1
|
140.0
nM
|
|
Antiviral activity against HIV1 MDR/JSL R5 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 1
|
290.0
nM
|
|
Antiviral activity against HIV1 MDR/B X4 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 1
|
270.0
nM
|
|
Antiviral activity against HIV1 MDR/C X4 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 1
|
35.0
nM
|
|
Antiviral activity against HIV1 MDR/G X4 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 1
|
33.0
nM
|
|
Antiviral activity against HIV1 92UG029 X4 subtype A in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 1
|
4.8
nM
|
|
Antiviral activity against HIV1 92UG037 subtype A R5 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 1
|
3.2
nM
|
|
Antiviral activity against HIV1 BaL R5 subtype B in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 1
|
8.3
nM
|
|
Antiviral activity against HIV1 97ZA003 R5 subtype C in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 1
|
6.7
nM
|
|
Antiviral activity against HIV1 92TH019 R5 subtype E in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 1
|
3.0
nM
|
|
Antiviral activity against R5-HIV1Ba-L assessed as inhibition of p24 Gag protein production in human PHA-PBMC by ELISA
|
Human immunodeficiency virus 1
|
8.0
nM
|
|
Antiviral activity against R5-HIV1MDR/MM assessed as inhibition of p24 Gag protein production in human PHA-PBMC by ELISA
|
Human immunodeficiency virus 1
|
220.0
nM
|
|
Antiviral activity against X4-HIV1 NL4-3 assessed as inhibition of p24 Gag protein production in human MT4 cells by MTT assay
|
Human immunodeficiency virus 1
|
10.0
nM
|
|
Antiviral activity against R5-HIV1MDR/C assessed as inhibition of p24 Gag protein production in human PHA-PBMC by ELISA
|
Human immunodeficiency virus 1
|
37.0
nM
|
|
Antiviral activity against R5-HIV1MDR/G assessed as inhibition of p24 Gag protein production in human PHA-PBMC by ELISA
|
Human immunodeficiency virus 1
|
26.0
nM
|
|
Inhibition of wild-type HIV1 BH10 protease expressed in Escherichia coli by spectrophotometric assay
|
Human immunodeficiency virus 1
|
0.04
nM
|
|
Inhibition of HIV1 recombinant protease D30N/N88D mutant expressed in Escherichia coli by spectrophotometric assay
|
Human immunodeficiency virus 1
|
0.51
nM
|
|
Inhibition of HIV1 recombinant protease M46I/A71V/V82T/I84V mutant expressed in Escherichia coli by spectrophotometric assay
|
Human immunodeficiency virus 1
|
13.0
nM
|
|
Inhibition of HIV1 recombinant protease A71V/V82T/I84V mutant expressed in Escherichia coli by spectrophotometric assay
|
Human immunodeficiency virus 1
|
12.0
nM
|
|
Inhibition of HIV1 recombinant protease V32I/I47A mutant expressed in Escherichia coli by spectrophotometric assay
|
Human immunodeficiency virus 1
|
0.22
nM
|
|
Inhibition of HIV1 recombinant protease L10I/I15V/E35D/N37S/R41K/I62V/L63P/A71V/G73S/L90M mutant expressed in Escherichia coli by spectrophotometric assay
|
Human immunodeficiency virus 1
|
2.9
nM
|
|
Inhibition of HIV1 recombinant protease L10I/L24I/L33F/M46L/154V/L63P/A71V/V82A/I84V mutant expressed in Escherichia coli by spectrophotometric assay
|
Human immunodeficiency virus 1
|
180.0
nM
|
|
Inhibition of HIV1 recombinant protease L10F/L19I/K20R/L33F/E35D/M36I/R41K/F53L/I54V/L63P/H69K/A71V/T74P/I84V/L89M/L90M/I93L mutant expressed in Escherichia coli by spectrophotometric assay
|
Human immunodeficiency virus 1
|
71.0
nM
|
|
Ratio of Ki for HIV1 recombinant protease D30N/N88D mutant to Ki for wild-type HIV1 BH10 protease
|
Human immunodeficiency virus 1
|
13.0
nM
|
|
Ratio of Ki for HIV1 recombinant protease M46I/A71V/V82T/I84V mutant to Ki for wild-type HIV1 BH10 protease
|
Human immunodeficiency virus 1
|
25.0
nM
|
|
Ratio of Ki for HIV1 recombinant protease A71V/V82T/I84V mutant to Ki for wild-type HIV1 BH10 protease
|
Human immunodeficiency virus 1
|
290.0
nM
|
|
Ratio of Ki for HIV1 recombinant protease V32I/I47A mutant to Ki for wild-type HIV1 BH10 protease
|
Human immunodeficiency virus 1
|
5.5
nM
|
|
Ratio of Ki for HIV1 recombinant protease L10I/I15V/E35D/N37S/R41K/I62V/L63P/A71V/G73S/L90M mutant to Ki for wild-type HIV1 BH10 protease
|
Human immunodeficiency virus 1
|
73.0
nM
|
|
Antimalarial activity after 24 hrs against chloroquine-resistant Plasmodium falciparum W2 by [3H]hypoxanthine uptake
|
Plasmodium falciparum
|
7.0
ug.mL-1
|
|
Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay
|
Human immunodeficiency virus 1
|
12.0
nM
|
|
Antiviral activity against HIV2 MS infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay
|
Human immunodeficiency virus 2
|
5.0
nM
|
|
Antiviral activity against HIV2 CBL-23 infected in human PBMC assessed as inhibition of virus production after 5 days by Lenti-RT activity assay
|
Human immunodeficiency virus 2
|
8.0
nM
|
|
Antiviral activity against HIV2 CDC310319 isolate infected in human PBMC assessed as inhibition of virus production after 5 days by Lenti-RT activity assay
|
Human immunodeficiency virus 2
|
68.0
nM
|
|
Antiviral activity against wild type HIV2 ROD infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay
|
Human immunodeficiency virus 2
|
3.6
nM
|
|
Antiviral activity against HIV2 ROD with protease G17N mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay
|
Human immunodeficiency virus 2
|
2.2
nM
|
|
Antiviral activity against HIV2 ROD with protease V47A mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay
|
Human immunodeficiency virus 2
|
0.2
nM
|
|
Antiviral activity against HIV2 ROD with protease G17N/V47A mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay
|
Human immunodeficiency virus 2
|
0.2
nM
|
|
Antiviral activity against HIV1 LAI infected in human CEM-SS cells assessed as reverse transcriptase activity after 5 days by MTT assay
|
Human immunodeficiency virus 1
|
9.0
nM
|
|
Antiviral activity against HTLV1 3B infected in human MT4 cells assessed as reverse transcriptase activity after 5 days by MTT assay
|
Human T-lymphotropic virus 1
|
18.0
nM
|
|
Inhibition of HIV1 protease
|
Human immunodeficiency virus 1
|
0.08
nM
|
|
Antiviral activity against wild type HIV1 NL4-3 infected in MT4 cells after 6 days by MTT assay
|
Human immunodeficiency virus 1
|
12.0
nM
|
|
Antiviral activity against wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay
|
Human immunodeficiency virus 1
|
1.8
nM
|
|
Inhibition of wild type HIV1 protease by competitive binding
|
Human immunodeficiency virus 1
|
0.42
nM
|
|
Inhibition of HIV1 protease V32I mutant by competitive binding
|
Human immunodeficiency virus 1
|
9.0
nM
|
|
Antiviral activity against HIV1 LAI in human MT2 cells assessed as inhibition of virus-induced cytopathic effect
|
Human immunodeficiency virus 1
|
16.0
nM
|
|
Inhibition of HIV1 protease
|
Human immunodeficiency virus 1
|
1.4
nM
|
|
Inhibition of HIV1 protease expressed in Escherichia coli by fluorometric assay
|
Human immunodeficiency virus 1
|
0.2
nM
|
|
Antiviral activity against HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 6 days by XTT assay
|
Human immunodeficiency virus 1
|
10.0
nM
|
|
Antiviral activity against wild type HIV1 isolate ERS104pre infected in PHA-stimulated human PBMC assessed as inhibition of p24 gap protein production
|
Human immunodeficiency virus 1
|
8.0
nM
|
|
Antiviral activity against multidrug-resistant HIV1 isolate B infected in PHA-stimulated human PBMC assessed as inhibition of p24 gap protein production
|
Human immunodeficiency virus 1
|
270.0
nM
|
|
Antiviral activity against multidrug-resistant HIV1 isolate C infected in PHA-stimulated human PBMC assessed as inhibition of p24 gap protein production
|
Human immunodeficiency virus 1
|
32.0
nM
|
|
Antiviral activity against multidrug-resistant HIV1 isolate G infected in PHA-stimulated human PBMC assessed as inhibition of p24 gap protein production
|
Human immunodeficiency virus 1
|
30.0
nM
|
|
Antiviral activity against multidrug-resistant HIV1 isolate TM infected in PHA-stimulated human PBMC assessed as inhibition of p24 gap protein production
|
Human immunodeficiency virus 1
|
260.0
nM
|
|
Antiviral activity against multidrug-resistant HIV1 isolate MM infected in PHA-stimulated human PBMC assessed as inhibition of p24 gap protein production
|
Human immunodeficiency virus 1
|
190.0
nM
|
|
Antiviral activity against multidrug-resistant HIV1 isolate JSL infected in PHA-stimulated human PBMC assessed as inhibition of p24 gap protein production
|
Human immunodeficiency virus 1
|
300.0
nM
|
|
Inhibition of recombinant wild type HIV1 protease assessed as hydrolysis of fluorogenic substrate
|
Human immunodeficiency virus 1
|
0.4
nM
|
|
Antimicrobial activity against Plasmodium yoelii 265 liver infected in mammalian hepatocytes after 48 hrs
|
Plasmodium yoelii yoelii
|
35.2
nM
|
|
Antiviral activity against HIV 2 subtype A clinical isolate expressing 14H-17D-43T-68N/D protease gene sequence from HIV2 infected patient plasma and PBMC obtained before compound treatment measured after 13 months
|
Human immunodeficiency virus 2
|
6.0
nM
|
|
Antiviral activity against HIV 2 subtype A clinical isolate expressing 14H-60K/N-65E protease gene sequence from HIV2 infected patient plasma and PBMC obtained before compound treatment measured after 13 months
|
Human immunodeficiency virus 2
|
5.0
nM
|
|
Antiviral activity against HIV 2 subtype A clinical isolate expressing 10I-17D-40D-43I-46V-66V/A-70R/K protease gene sequence from HIV2 infected patient plasma and PBMC obtained before compound treatment measured after 13 months
|
Human immunodeficiency virus 2
|
2.0
nM
|
|
Antiviral activity against HIV 2 subtype A clinical isolate expressing 10I-17D-40D-43I-45K/R-46V-54M-64I/V-69K/R-71V/I-90M protease gene sequence from HIV2 infected patient plasma and PBMC obtained at T1 during compound treatment measured after 13 months
|
Human immunodeficiency virus 2
|
90.0
nM
|
|
Antiviral activity against HIV 2 subtype A clinical isolate expressing 14H-40D-70K-72R/K-91T/S protease gene sequence from HIV2 infected patient plasma and PBMC obtained before compound treatment measured after 13 months
|
Human immunodeficiency virus 2
|
5.0
nM
|
|
Antiviral activity against HIV 2 subtype B clinical isolate expressing 12T-14Y-19P-40N-41D-61N-62I-96S-99L protease gene sequence from HIV2 infected patient plasma and PBMC obtained before compound treatment measured after 13 months
|
Human immunodeficiency virus 2
|
7.0
nM
|
|
Antiviral activity against HIV 2 subtype B clinical isolate expressing 12Q-14R-17G/D-19P-61N-62I-92A protease gene sequence from HIV2 infected patient plasma and PBMC obtained before compound treatment measured after 13 months
|
Human immunodeficiency virus 2
|
60.0
nM
|
|
Antiviral activity against HIV 2 subtype B clinical isolate expressing 41D protease gene sequence from HIV2 infected patient plasma and PBMC obtained before compound treatment measured after 13 months
|
Human immunodeficiency virus 2
|
20.0
nM
|
|
Antiviral activity against Human immunodeficiency virus type 2 (ISOLATE ROD) after 13 months
|
Human immunodeficiency virus type 2 (ISOLATE ROD)
|
10.0
nM
|
|
Antiviral activity against Human immunodeficiency virus type 1 (BRU ISOLATE) after 13 months
|
Human immunodeficiency virus type 1 (BRU ISOLATE)
|
10.0
nM
|
|
Antiviral activity against HIV 2 subtype H expressing 10I-40P-41Y-60H-63N-70T-73G-89L-92E protease gene sequence from HIV2 infected patient plasma and PBMC obtained before compound treatment measured after 13 months
|
Human immunodeficiency virus 2
|
30.0
nM
|
|
Antiviral activity against HIV1 LAI infected in human MT2 cells after 7 days by MTT assay
|
Human immunodeficiency virus
|
14.0
nM
|
|
Antiviral activity against HIV1 ERS104pre infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA
|
Human immunodeficiency virus 1
|
9.0
nM
|
|
Antiviral activity against HIV1 MOKW infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA
|
Human immunodeficiency virus 1
|
4.0
nM
|
|
Antiviral activity against HIV1 TM harboring L10I/K14R/R41K/M46L/I54V/L63P/A71V/V82A/L90M/I93L in protease encoding region infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA
|
Human immunodeficiency virus 1
|
270.0
nM
|
|
Antiviral activity against HIV1 MM harboring L10I/K43T/M46L/I54V/L63P/A71V/V82A/L90M/Q92K in protease encoding region infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA
|
Human immunodeficiency virus 1
|
270.0
nM
|
|
Antiviral activity against HIV1 JSL harboring L10I/L24I/L33F/E35D/M36I/N37S/M46L/I54V/R57K/I62V/L63P/A71V/G73S/82A in protease encoding region infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA
|
Human immunodeficiency virus 1
|
320.0
nM
|
|
Antiviral activity against HIV1 A harboring L10I/I15V/E35D/N37E/K45R/I54V/L63P/A71V/V82T/L90M/I93L/C95F in protease encoding region infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA
|
Human immunodeficiency virus 1
|
100.0
nM
|
|
Antiviral activity against HIV1 B harboring L10I/I15V/E35D/N37E/K45R/I54V/L63P/A71V/V82T/L90M/I93L/C95F in protease encoding region infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA
|
Human immunodeficiency virus 1
|
300.0
nM
|
|
Antiviral activity against HIV1 C harboring L10I/I15V/K20R/L24I/M36I/M46L/I54V/I62V/L63P/K70Q/V82A/L89M in protease encoding region infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA
|
Human immunodeficiency virus 1
|
33.0
nM
|
|
Antiviral activity against HIV1 G harboring L10I/V11I/T12E/I15V/L19I/R41K/M46L/L63P/A71T/V82A/L90M in protease encoding region infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA
|
Human immunodeficiency virus 1
|
27.0
nM
|
|
Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of p24 gag protein production by ELISA
|
Human immunodeficiency virus 1
|
8.0
nM
|
|
Antiviral activity against HIV1 NL4-3 harboring L10F/V32I/M46I/I54M//A71V/I84V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of amprenavir by ELISA
|
Human immunodeficiency virus 1
|
16.0
nM
|
|
Antiviral activity against HIV1 NL4-3 harboring L10F/L24I/M46I/L63P/A71V/G73S/V82T amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of indinavir by ELISA
|
Human immunodeficiency virus 1
|
22.0
nM
|
|
Antiviral activity against HIV1 NL4-3 harboring L10F/D30N/K45I/A71V/T74S amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of nelfinavir by ELISA
|
Human immunodeficiency virus 1
|
28.0
nM
|
|
Antiviral activity against HIV1 NL4-3 harboring M46I/V82F/I84V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of ritonavir by ELISA
|
Human immunodeficiency virus 1
|
10.0
nM
|
|
Antiviral activity against HIV1 NL4-3 harboring L10F/M46I/I54V/V82A amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 1 uM of Lopinavir by ELISA
|
Human immunodeficiency virus 1
|
33.0
nM
|
|
Antiviral activity against HIV1 NL4-3 harboring L23I/K43I/M46I/I50L/G51A/A71V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 1 uM of atazanavir by ELISA
|
Human immunodeficiency virus 1
|
34.0
nM
|
|
Antiviral activity against HIV1 NL4-3 harboring L10F/L33F/M46I/I47V/Q58E/V82I/I84V/I85V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of GRL-02031 by ELISA
|
Human immunodeficiency virus 1
|
8.0
nM
|
|
Antiviral activity against HIV1 NL4-3 infected in human PBMC assessed as inhibition of viral p24 antigen production after 7 to 10 days by ELISA
|
Human immunodeficiency virus 1
|
9.0
nM
|
|
Antiviral activity against HIV1 X4 infected in human PBMC assessed as inhibition of viral p24 antigen production after 7 to 10 days by ELISA
|
Human immunodeficiency virus 1
|
29.0
nM
|
|
Antiviral activity against HIV1 89.6 infected in human PBMC assessed as inhibition of viral p24 antigen production after 7 to 10 days by ELISA
|
Human immunodeficiency virus 1
|
9.9
nM
|
|
Antiviral activity against HIV1 JRCSF infected in human PBMC assessed as inhibition of viral p24 antigen production after 7 to 10 days by ELISA
|
Human immunodeficiency virus type 1 (JRCSF ISOLATE)
|
2.6
nM
|
|
Antiviral activity against HIV1 R5 infected in human PBMC assessed as inhibition of viral p24 antigen production after 7 to 10 days by ELISA
|
Human immunodeficiency virus 1
|
8.0
nM
|
|
Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells by MTT assay
|
Human immunodeficiency virus 1
|
5.0
nM
|
|
Antiviral activity against HIV1 expressing protease L10F/D30N/K45I/A71V/T74S mutant infected in human MT4 cells selected at 5 uM of nelfinavir by MTT assay
|
Human immunodeficiency virus 1
|
3.0
nM
|
|
Antiviral activity against HIV1 expressing protease L10F/M46I/I50V/A71V/I84V/L90M mutant infected in human MT4 cells selected at 5 uM of amprenavir by MTT assay
|
Human immunodeficiency virus 1
|
26.0
nM
|
|
Antiviral activity against HIV1 expressing protease L10F/M46I/I54V/V82A mutant infected in human MT4 cells selected at 5 uM of Lopinavir by MTT assay
|
Human immunodeficiency virus 1
|
28.0
nM
|
|
Antiviral activity against HIV1 expressing protease L23I/E34Q/K43I/M46I/I50L/G51A/L63P/A71V/V82A/T91A mutant infected in human MT4 cells selected at 5 uM of atazanavir by MTT assay
|
Human immunodeficiency virus 1
|
31.0
nM
|
|
Antiviral activity against wild type HIV1 ERS104 containing protease L36P mutant infected in human PHA-PBMC cells by MTT assay
|
Human immunodeficiency virus 1
|
8.0
nM
|
|
Antiviral activity against multidrug-resistant HIV1 isolate B containing protease L10I, K14R, L33I, M36I,M46I, F53I, K55R, I62V, L63P, A71V, G73S, V82A, L90M, and I93L mutant infected in human PHA-PBMC cells by MTT assay
|
Human immunodeficiency virus 1
|
270.0
nM
|
|
Antiviral activity against multidrug-resistant HIV1 isolate C containing protease L10I, I15V, K20R, L24I, M36I, M46L, I54V, I62V, L63P, K70Q, V82A, and L89M mutant infected in human PHA-PBMC cells by MTT assay
|
Human immunodeficiency virus 1
|
32.0
nM
|
|
Antiviral activity against multidrug-resistant HIV1 isolate G containing L10I, V11I, T12E, I15V, L19I,R41K, M46L, L63P, A71T, V82A, and L90M mutant infected in human PHA-PBMC cells by MTT assay
|
Human immunodeficiency virus 1
|
30.0
nM
|
|
Antiviral activity against multidrug-resistant HIV1 isolate TM containing L10I, K14R, R41K, M46L, I54V, L63P, A71V, V82A, L90M, and I93L mutant infected in human PHA-PBMC cells by MTT assay
|
Human immunodeficiency virus 1
|
260.0
nM
|
|
Antiviral activity against multidrug-resistant HIV1 isolate MM containing L10I, K43T, M46L, I54V, L63P, A71V, V82A, L90M, and Q92K mutant infected in human PHA-PBMC cells by MTT assay
|
Human immunodeficiency virus 1
|
190.0
nM
|
|
Antiviral activity against multidrug-resistant HIV1 isolate JSL containing L10I, L24I, I33F, E35D, M36I, N37S, M46L, I54V, R57K, I62V, L63P, A71V, G73S, and V82A mutant infected in human PHA-PBMC cells by MTT assay
|
Human immunodeficiency virus 1
|
300.0
nM
|
|
Antiviral activity against HIV1 LAI infected in human MT2 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
|
Human immunodeficiency virus 1
|
15.0
nM
|
|
Mechanism based inhibition of human cytochrome P450 3A4 measured by testosterone hydroxylation
|
Homo sapiens
|
170.0
nM
|
|
Antiviral activity against Human immunodeficiency virus 1 LAI infected in human MT2 cells assessed as inhibition of p24 Gag protein production
|
Human immunodeficiency virus 1
|
15.0
nM
|
|
DRUGMATRIX: Sodium Channel, Site 2 radioligand binding (ligand: [3H] Batrachotoxin)
|
Rattus norvegicus
|
755.0
nM
|
|
DRUGMATRIX: Sodium Channel, Site 2 radioligand binding (ligand: [3H] Batrachotoxin)
|
Rattus norvegicus
|
677.0
nM
|
|
Antimalarial activity against chloroquine resistant, mefloquine sensitive Plasmodium falciparum W2 infected in human erythrocytes by [3H]-hypoxanthine incorporation assay
|
Plasmodium falciparum
|
7.0
ug.mL-1
|
|
Antiviral activity against multidrug-resistant HIV1 106-PR infected in HEK293T cells assessed as inhibition of viral replication after 4 days by beta-galactosidase reporter gene assay
|
Human immunodeficiency virus 1
|
12.0
nM
|
|
Binding affinity to Human immunodeficiency virus 1 protease by SPR biosensor interaction analysis at pH 7.4
|
Human immunodeficiency virus 1
|
0.577
nM
|
|
Binding affinity to Human immunodeficiency virus 1 protease by SPR biosensor interaction analysis at pH 5.1
|
Human immunodeficiency virus 1
|
0.637
nM
|
|
Binding affinity to Human immunodeficiency virus 1 protease by SPR biosensor interaction analysis at pH 4.1
|
Human immunodeficiency virus 1
|
4.13
nM
|
|
Binding affinity to wild type HIV1 protease
|
Human immunodeficiency virus 1
|
0.65
nM
|
|
Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting
|
Homo sapiens
|
63.8
%
|
|
Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting
|
Homo sapiens
|
6.6
%
|
|
Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting
|
Homo sapiens
|
11.5
%
|
|
Time dependent inhibition of CYP3A4-mediated testosterone-6-beta hydroxylation in human liver microsome
|
Homo sapiens
|
650.0
nM
|
|
Antiviral activity against HIV1 LAI infected in human MT2 cells by MTT assay
|
Human immunodeficiency virus 1
|
15.0
nM
|
|
Inhibition of HIV1 protease using fluorogenic hexapeptide substrate (2-aminobenzoyl)Thr-Ile-Nle-(p-nitro)Phe-Gln-Arg by fluorimeter
|
Human immunodeficiency virus 1
|
0.221
nM
|
|
Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as virus-induced cytopathic effect after 5 days by XTT assay
|
Human immunodeficiency virus 1
|
13.6
nM
|
|
Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay
|
Human immunodeficiency virus 1
|
20.0
nM
|
|
Antiviral activity against efavirenz-resistant HIV1 harboring RT 100I, 103R, 179D, 225H mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay
|
Human immunodeficiency virus 1
|
10.0
nM
|
|
Antiviral activity against N119-sensitive HIV1 harboring Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay
|
Human immunodeficiency virus 1
|
20.0
nM
|
|
Antiviral activity against A17-sensitive HIV1 harboring 103N, 181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay
|
Human immunodeficiency virus 1
|
10.0
nM
|
|
Antiviral activity against zidovudine-resistant HIV1 harboring RT 67N, 70R, 215F, 219Q mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay
|
Human immunodeficiency virus 1
|
10.0
nM
|
|
Antiviral activity against MDR-resistant HIV1 harboring 41L, 74V, 106A, 215Y mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay
|
Human immunodeficiency virus 1
|
20.0
nM
|
|
Antiviral activity against saquinavir-resistant HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay
|
Human immunodeficiency virus 1
|
90.0
nM
|
|
Antiviral activity against 6-[(3,5-Dimethylphenyl)fluoromethyl]-5-ethyl-1-{[[4-(3-hydroxyprop-1-ynyl)benzyl]oxy]methyl}pyrimidine-2,4(1H,3H)-dione-resistant HIV1 harboring RT 106I, 181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay
|
Human immunodeficiency virus 1
|
20.0
nM
|
|
Antiviral activity against MC1220-resistant HIV1 harboring RT 100I, 179D, 181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay
|
Human immunodeficiency virus 1
|
10.0
nM
|
|
Antiviral activity against TMC120-resistant HIV1 harboring RT 100I, 138G mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay
|
Human immunodeficiency virus 1
|
20.0
nM
|
|
Antiviral activity against TMC125-resistant HIV1 harboring RT 109M, 138K, 190E mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay
|
Human immunodeficiency virus 1
|
10.0
nM
|
|
Antiviral activity against HIV1 Lai infected in human MT2 cells
|
HIV-1 M:B_Lai
|
21.0
nM
|
|
Antiviral activity against HIV-1 LAI infected in human MT2 cells
|
Human immunodeficiency virus 1
|
21.0
nM
|
|
Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by automated chemiluminescent enzyme immunoassay
|
Human immunodeficiency virus 1
|
21.0
nM
|
|
Binding affinity to HIV-1 Aspartic Protease
|
Human immunodeficiency virus 1
|
67.4
nM
|
|
Antiviral activity against HIV1 NL4-3 infected in human MT4 cells after 7 days by MTT assay
|
Human immunodeficiency virus 1
|
15.0
nM
|
|
Antiviral activity against HIV1 LAI infected in human MT2 cells
|
HIV-1 M:B_Lai
|
21.0
nM
|
|
Inhibition of HIV1 protease using H-Val-Ser-Gln-Am-(L-b-naphthyl-alanine)-Pro-Ile-Val-OH as substrate by HPLC method
|
Human immunodeficiency virus 1
|
0.23
nM
|
|
Inhibition of HIV2 protease
|
Human immunodeficiency virus 2
|
0.5
nM
|
|