|
Inhibitory activity against HIV-1 protease
|
Human immunodeficiency virus 1
|
2.1
nM
|
|
|
Binding affinity against HIV-1 protease
|
Human immunodeficiency virus 1
|
0.0
nM
|
|
|
Inhibitory activity against human immunodeficiency virus 1 protease
|
Human immunodeficiency virus 1
|
0.015
nM
|
|
|
Effective concentration against PI-Resistant HIV strain (M1)
|
Human immunodeficiency virus 1
|
5.129
nM
|
|
|
Effective concentration against PI-Resistant HIV strain (M2)
|
Human immunodeficiency virus 1
|
190.55
nM
|
|
Effective concentration against PI-Resistant HIV strain (M2)
|
Human immunodeficiency virus 1
|
7.244
nM
|
|
|
Effective concentration against PI-Resistant HIV strain (M3)
|
Human immunodeficiency virus 1
|
173.78
nM
|
|
Effective concentration against PI-Resistant HIV strain (M3)
|
Human immunodeficiency virus 1
|
7.244
nM
|
|
|
Effective concentration against PI-Resistant HIV strain (M4)
|
Human immunodeficiency virus 1
|
144.54
nM
|
|
Effective concentration against PI-Resistant HIV strain (M4)
|
Human immunodeficiency virus 1
|
3.89
nM
|
|
|
Effective concentration against PI-Resistant HIV strain (M5)
|
Human immunodeficiency virus 1
|
125.89
nM
|
|
Effective concentration against PI-Resistant HIV strain (M5)
|
Human immunodeficiency virus 1
|
6.026
nM
|
|
|
Effective concentration of against HIV Wild Type (IIIB) strain
|
Human immunodeficiency virus 1
|
43.65
nM
|
|
Effective concentration of against HIV Wild Type (IIIB) strain
|
Human immunodeficiency virus 1
|
4.074
nM
|
|
|
Effective concentration as average activity on mutant HIV panel (AVMUT)
|
Human immunodeficiency virus 1
|
154.88
nM
|
|
Effective concentration as average activity on mutant HIV panel (AVMUT)
|
Human immunodeficiency virus 1
|
5.129
nM
|
|
|
Binding affinity to HIV1 protease
|
Human immunodeficiency virus 1
|
0.22
nM
|
|
|
Binding affinity to HIV1 protease D30N
|
Human immunodeficiency virus 1
|
6.6
nM
|
|
|
Binding affinity to HIV1 protease I50V
|
Human immunodeficiency virus 1
|
2.0
nM
|
|
|
Binding affinity to HIV1 protease V82A
|
Human immunodeficiency virus 1
|
0.8
nM
|
|
|
Binding affinity to HIV1 protease I84V
|
Human immunodeficiency virus 1
|
1.1
nM
|
|
|
Binding affinity to HIV1 protease L90M
|
Human immunodeficiency virus 1
|
0.03
nM
|
|
|
Antiviral activity against HIV1 HXB2 in MT4 cells
|
None
|
3.9
nM
|
|
|
Antiviral activity against HIV1 EP13 in MT4 cells
|
None
|
6.8
nM
|
|
|
Antiviral activity against HIV D545701 in MT4 cells
|
None
|
32.0
nM
|
|
|
Inhibition of HIV1 protease
|
Human immunodeficiency virus 1
|
0.014
nM
|
|
|
Antiviral activity against HIV1 LAI isolate in human MT2 cells
|
Human immunodeficiency virus 1
|
3.0
nM
|
|
|
Antiviral activity against multi drug-resistant HIV1 B variant in human PHA-PBMC cells
|
Human immunodeficiency virus 1
|
10.2
nM
|
|
|
Antiviral activity against multi drug-resistant HIV1 C variant in human PHA-PBMC cells
|
Human immunodeficiency virus 1
|
3.5
nM
|
|
|
Antiviral activity against multi drug-resistant HIV1 G variant in human PHA-PBMC cells
|
Human immunodeficiency virus 1
|
3.7
nM
|
|
|
Antiviral activity against multi drug-resistant HIV1 TM variant in human PHA-PBMC cells
|
Human immunodeficiency virus 1
|
3.5
nM
|
|
|
Antiviral activity against multi drug-resistant HIV1 K variant in human PHA-PBMC cells
|
Human immunodeficiency virus 1
|
3.0
nM
|
|
|
Inhibition of wild type HIV1 protease
|
Human immunodeficiency virus 1
|
0.34
nM
|
|
|
Inhibition of HIV1 protease D30N mutant
|
Human immunodeficiency virus 1
|
1.9
nM
|
|
|
Inhibition of HIV1 protease I50V mutant
|
Human immunodeficiency virus 1
|
1.3
nM
|
|
|
Inhibition of HIV1 protease V82A mutant
|
Human immunodeficiency virus 1
|
0.54
nM
|
|
|
Inhibition of HIV1 protease I84V mutant
|
Human immunodeficiency virus 1
|
0.56
nM
|
|
|
Inhibition of HIV1 protease
|
Human immunodeficiency virus 1
|
0.016
nM
|
|
|
Antiviral activity against HIV1 LAI in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 1
|
3.9
nM
|
|
|
Antiviral activity against HIV2 EHO in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 2
|
8.0
nM
|
|
|
Antiviral activity against HIV2 ROD in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 2
|
6.8
nM
|
|
|
Antiviral activity against HIV1 NL4-3 in MT4 cells by MTT assay
|
Human immunodeficiency virus 1
|
3.0
nM
|
|
|
Antiviral activity against saquinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 1
|
5.8
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
|
18.0
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
|
15.0
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
|
3.3
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
|
330.0
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
|
3.4
nM
|
|
|
Antiviral activity against HIV1 GRL98065p20 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 1
|
21.0
nM
|
|
|
Antiviral activity against HIV1 GRL98065p30 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 1
|
36.0
nM
|
|
|
Antiviral activity against HIV1 GRL98065p40 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 1
|
210.0
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
|
3.8
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
|
4.3
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
|
16.0
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
|
27.0
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
|
40.0
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
|
9.0
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
|
7.0
nM
|
|
|
Inhibition of HIV1 protease dimerization in MT2 cells
|
Human immunodeficiency virus 1
|
0.016
nM
|
|
|
Antiviral activity against HIV1 LAI in MT2 cells
|
Human immunodeficiency virus 1
|
3.4
nM
|
|
|
Inhibition of wild-type HIV1 BH10 protease expressed in Escherichia coli by spectrophotometric assay
|
Human immunodeficiency virus 1
|
0.0053
nM
|
|
|
Inhibition of HIV1 recombinant protease D30N/N88D mutant expressed in Escherichia coli by spectrophotometric assay
|
Human immunodeficiency virus 1
|
0.011
nM
|
|
|
Inhibition of HIV1 recombinant protease M46I/A71V/V82T/I84V mutant expressed in Escherichia coli by spectrophotometric assay
|
Human immunodeficiency virus 1
|
0.032
nM
|
|
|
Inhibition of HIV1 recombinant protease A71V/V82T/I84V mutant expressed in Escherichia coli by spectrophotometric assay
|
Human immunodeficiency virus 1
|
0.0043
nM
|
|
|
Inhibition of HIV1 recombinant protease V32I/I47A mutant expressed in Escherichia coli by spectrophotometric assay
|
Human immunodeficiency virus 1
|
0.31
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
|
0.015
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
|
0.02
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
|
0.001
nM
|
|
|
Ratio of Ki for HIV1 recombinant protease D30N/N88D mutant to Ki for wild-type HIV1 BH10 protease
|
Human immunodeficiency virus 1
|
2.0
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
|
6.0
nM
|
|
|
Ratio of Ki for HIV1 recombinant protease A71V/V82T/I84V mutant to Ki for wild-type HIV1 BH10 protease
|
Human immunodeficiency virus 1
|
0.8
nM
|
|
|
Ratio of Ki for HIV1 recombinant protease V32I/I47A mutant to Ki for wild-type HIV1 BH10 protease
|
Human immunodeficiency virus 1
|
58.0
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
|
2.8
nM
|
|
|
Ratio of Ki for HIV1 recombinant protease L10I/L24I/L33F/M46L/154V/L63P/A71V/V82A/I84V mutant to Ki for wild-type HIV1 BH10 protease expressed in Escherichia coli
|
Human immunodeficiency virus 1
|
3.7
nM
|
|
|
Ratio of Ki for HIV1 recombinant protease L10F/L19I/K20R/L33F/E35D/M36I/R41K/F53L/I54V/L63P/H69K/A71V/T74P/I84V/L89M/L90M/I93L mutant to Ki for wild-type HIV1 BH10 protease
|
Human immunodeficiency virus 1
|
0.2
nM
|
|
|
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 CBL-23 infected in human PBMC assessed as inhibition of virus production after 5 days by Lenti-RT activity assay
|
Human immunodeficiency virus 2
|
83.0
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
|
155.0
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
|
9.0
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
|
6.0
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
|
10.0
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
|
8.0
nM
|
|
|
Antiviral activity against wild type HIV1 isolate ERS104pre infected in PHA-stimulated PBMC assessed as inhibition of p24 gap protein
|
Human immunodeficiency virus 1
|
3.6
nM
|
|
|
Antiviral activity against multidrug-resistant HIV1 isolate TM infected in PHA-stimulated PBMC assessed as inhibition of p24 gap protein
|
Human immunodeficiency virus 1
|
3.6
nM
|
|
|
Antiviral activity against multidrug-resistant HIV1 isolate MM infected in PHA-stimulated PBMC assessed as inhibition of p24 gap protein
|
Human immunodeficiency virus 1
|
19.0
nM
|
|
|
Antiviral activity against multidrug-resistant HIV1 isolate C infected in PHA-stimulated PBMC assessed as inhibition of p24 gap protein
|
Human immunodeficiency virus 1
|
15.0
nM
|
|
|
Antiviral activity against multidrug-resistant HIV1 isolate G infected in PHA-stimulated PBMC assessed as inhibition of p24 gap protein
|
Human immunodeficiency virus 1
|
14.0
nM
|
|
|
Inhibition of wild type HIV1 protease by uncompetitive binding
|
Human immunodeficiency virus 1
|
18.0
nM
|
|
|
Inhibition of wild type HIV1 protease by enzyme inhibition
|
Human immunodeficiency virus 1
|
9.0
nM
|
|
|
Inhibition of wild type HIV1 protease by competitive binding
|
Human immunodeficiency virus 1
|
22.0
nM
|
|
|
Inhibition of HIV1 protease V32I mutant by uncompetitive binding
|
Human immunodeficiency virus 1
|
180.0
nM
|
|
|
Inhibition of HIV1 protease V32I mutant by enzyme inhibition
|
Human immunodeficiency virus 1
|
54.0
nM
|
|
|
Inhibition of HIV1 protease V32I mutant by competitive binding
|
Human immunodeficiency virus 1
|
300.0
nM
|
|
|
Inhibition of HIV1 protease
|
Human immunodeficiency virus 1
|
0.016
nM
|
|
|
Antiviral activity against multidrug-resistant HIV1 with protease L10I, K14R, R41K, M46L, I54V, L63P, A71V, V82A, L90M, I93L mutation in phytohemagglutininin-activated PBMC assessed as inhibition of p24Gag protein production
|
Human immunodeficiency virus 1
|
4.0
nM
|
|
|
Antiviral activity against multidrug-resistant HIV1 with protease L10I, K43T, M46L, I54V, L63P, A71V, V82A, L90M, Q92K mutation in phytohemagglutininin-activated PBMC assessed as inhibition of p24G protein production
|
Human immunodeficiency virus 1
|
17.0
nM
|
|
|
Antiviral activity against multidrug-resistant HIV1 with protease L10I, L24I, I33F, E35D, M36I, N37S, M46L, I54V, R57K, I62V, L63P, A71V, G73S, V82A mutation in phytohemagglutininin-activated PBMC assessed as inhibition of p24G protein production
|
Human immunodeficiency virus 1
|
26.0
nM
|
|
|
Antiviral activity against multidrug-resistant HIV1 with protease L10I, K14R, L33I, M36I, M46I, F53I, K55R, I62V, L63P, A71V, G73S, V82A, L90M, I93L mutation in phytohemagglutininin-activated PBMC assessed as inhibition of p24G protein production
|
Human immunodeficiency virus 1
|
26.0
nM
|
|
|
Antiviral activity against multidrug-resistant HIV1 with protease L10I, V11I, T12E, I15V, L19I, R41K, M46L, L63P, A71T, V82A, L90M mutation in phytohemagglutininin-activated PBMC assessed as inhibition of p24G protein production
|
Human immunodeficiency virus 1
|
7.0
nM
|
|
|
Antiviral activity against multidrug-resistant HIV1/C with protease mutation in phytohemagglutininin-activated PBMC assessed as inhibition of p24G protein production
|
Human immunodeficiency virus 1
|
7.0
nM
|
|
|
Antiviral activity against multidrug-resistant HIV1/A with protease mutation in phytohemagglutininin-activated PBMC assessed as inhibition of p24G protein production
|
Human immunodeficiency virus 1
|
3.0
nM
|
|
|
Antiviral activity against HIV1 ERS104 with protease L63P mutation in phytohemagglutininin-activated PBMC assessed as inhibition of p24G protein production
|
Human immunodeficiency virus 1
|
3.5
nM
|
|
|
Antiviral activity against HIV1 BaL in human PBMC assessed as blockade of reverse transcriptase activity
|
Human immunodeficiency virus 1
|
2.8
nM
|
|
|
Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum by MTS assay
|
Human immunodeficiency virus 1
|
5.6
nM
|
|
|
Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 40% fetal bovine serum by MTS assay
|
Human immunodeficiency virus 1
|
11.0
nM
|
|
|
Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 10% human serum by MTS assay
|
Human immunodeficiency virus 1
|
11.0
nM
|
|
|
Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 20% human serum by MTS assay
|
Human immunodeficiency virus 1
|
15.0
nM
|
|
|
Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 30% human serum by MTS assay
|
Human immunodeficiency virus 1
|
19.0
nM
|
|
|
Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 40% human serum by MTS assay
|
Human immunodeficiency virus 1
|
22.0
nM
|
|
|
Antiviral activity against HIV1 drug resistant mutant isolates from protease inhibitor treated HIV patient
|
Human immunodeficiency virus 1
|
4.6
nM
|
|
|
Antiviral activity against HIV1 NL4-3
|
Human immunodeficiency virus 1
|
0.78
nM
|
|
|
Inhibition of HIV1 protease
|
Human immunodeficiency virus 1
|
0.000147
nM
|
|
|
Inhibition of HIV1 protease
|
Human immunodeficiency virus 1
|
0.014
nM
|
|
|
Antiviral activity against HIV1 assessed as inhibition of viral replication
|
Human immunodeficiency virus 1
|
4.1
nM
|
|
|
Antiviral activity against protease inhibitor resistant HIV1 isolates
|
Human immunodeficiency virus 1
|
3.0
nM
|
|
|
Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells after 5 days by MTT assay
|
Human immunodeficiency virus 1
|
12.0
nM
|
|
|
Antiviral activity against HIV1 bearing protease gene with A17 mutation infected in human MT4 cells after 5 days by MTT assay
|
Human immunodeficiency virus 1
|
338.0
nM
|
|
|
Antiviral activity against HIV1 bearing protease gene with B26 mutation infected in human MT4 cells after 5 days by MTT assay
|
Human immunodeficiency virus 1
|
587.0
nM
|
|
|
Antiviral activity against HIV1 bearing protease gene with P25 mutation infected in human MT4 cells after 5 days by MTT assay
|
Human immunodeficiency virus 1
|
515.0
nM
|
|
|
Inhibition of esterase mediated-hydrolysis of tenofovir disoproxil fumarate in human intestinal sub cellular fraction S9 at 2 uM after 30 mins
|
Homo sapiens
|
40.0
%
|
|
|
Inhibition of HIV1 protease expressed in Escherichia coli by fluorometric assay
|
Human immunodeficiency virus 1
|
1.1
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
|
4.0
nM
|
|
|
Inhibition of HIV1 protease
|
Human immunodeficiency virus 1
|
0.016
nM
|
|
|
Antiviral activity against HIV1 LAI infected in human MT2 cells by MTT assay
|
HIV-1 M:B_Lai
|
1.6
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
|
3.0
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
|
19.0
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
|
8.0
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
|
23.0
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
|
4.0
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
|
11.0
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
|
27.0
nM
|
|
|
Inhibition of HIV1 protease
|
Human immunodeficiency virus 1
|
0.016
nM
|
|
|
Antiviral activity against multi drug-resistant HIV1 isolate of subtype C in PHA-stimulated human PBMC assessed as inhibition of p24 antigen production
|
Human immunodeficiency virus 1
|
10.0
nM
|
|
|
Antiviral activity against multi drug-resistant HIV1 isolate of subtype G in PHA-stimulated human PBMC assessed as inhibition of p24 antigen production
|
Human immunodeficiency virus 1
|
19.0
nM
|
|
|
Antiviral activity against multi drug-resistant HIV1 isolate of subtype TM in PHA-stimulated human PBMC assessed as inhibition of p24 antigen production
|
Human immunodeficiency virus 1
|
7.0
nM
|
|
|
Antiviral activity against multi drug-resistant HIV1 isolate of subtype MM in PHA-stimulated human PBMC assessed as inhibition of p24 antigen production
|
Human immunodeficiency virus 1
|
27.0
nM
|
|
|
Antiviral activity against multi drug-resistant HIV1 isolate of subtype JSL in PHA-stimulated human PBMC assessed as inhibition of p24 antigen production
|
Human immunodeficiency virus 1
|
28.0
nM
|
|
|
Antiviral activity against wild type HIV1 isolate ERS104pre in PHA-stimulated human PBMC assessed as inhibition of p24 antigen production
|
Human immunodeficiency virus 1
|
5.0
nM
|
|
|
Antiviral activity against HIV1
|
Human immunodeficiency virus 1
|
1.6
nM
|
|
|
Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days post infection in absence of human serum by MTT assay
|
Human immunodeficiency virus 1
|
12.0
nM
|
|
|
Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days post infection in presence of 50% human serum by MTT assay
|
Human immunodeficiency virus 1
|
40.0
nM
|
|
|
Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as reduction in viral cytopathogenicity after 5 days post dose by MTT assay
|
Human immunodeficiency virus 1
|
100.0
nM
|
|
|
Antiviral activity against HIV1 A17 infected in human MT4 cells harboring protease L10F, V32I, M46I, I47V, Q58E, and I84V mutation derived from viral passages with Lopinavir assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days post infection by MTT assay
|
Human immunodeficiency virus 1
|
338.0
nM
|
|
|
Antiviral activity against HIV1 B26 infected in human MT4 cells harboring protease L33F, K45I, M46I, I50V, I54V, A71V, and V82F mutation derived from viral passages with Lopinavir assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days post infection by MTT assay
|
Human immunodeficiency virus 1
|
587.0
nM
|
|
|
Antiviral activity against HIV1 P25 infected in human MT4 cells harboring protease L10F, G16E, V32I, M46I, I47A, H69Y, I84V, and T91S mutation derived from viral passages with Lopinavir assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days post infection by MTT assay
|
Human immunodeficiency virus 1
|
857.0
nM
|
|
|
Antiviral activity against HIV 2 subtype H expressing 10I-34E-40P-41Y-60H-63N-70T-73G-82F-89L-92E protease gene sequence from HIV2 infected patient plasma and PBMC obtained at T1 during compound treatment measured after 13 months
|
Human immunodeficiency virus 2
|
900.0
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
|
9.0
nM
|
|
|
Antiviral activity against HIV 2 subtype A clinical isolate expressing 5L/F-14Y/H-17G/D-43T-54I/M-62V/A-70R/K-71I protease gene sequence from HIV2 infected patient plasma and PBMC obtained at T1 during compound treatment measured after 13 months
|
Human immunodeficiency virus 2
|
600.0
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
|
10.0
nM
|
|
|
Antiviral activity against HIV 2 subtype A clinical isolate expressing 54M-65E-71I-74N-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
|
200.0
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
|
4.0
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
|
800.0
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
|
4.0
nM
|
|
|
Antiviral activity against HIV 2 subtype A clinical isolate expressing 10I-40D-43I-70K-82F-84V-85L-89V-90M-91T/L-98N/K protease gene sequence from HIV2 infected patient plasma and PBMC obtained at T1 during compound treatment measured after 13 months
|
Human immunodeficiency virus 2
|
500.0
nM
|
|
|
Antiviral activity against HIV 2 subtype B clinical isolate expressing 14Y-61N-99L 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 B clinical isolate expressing 14Y-19P-33I-61N-71I-75M-84V-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
|
500.0
nM
|
|
|
Antiviral activity against HIV 2 subtype B clinical isolate expressing 14Y-19P-61N-64V-71I-90M-95I protease gene sequence from HIV2 infected patient plasma and PBMC obtained at T2 during compound treatment measured after 3 months
|
Human immunodeficiency virus 2
|
700.0
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
|
4.0
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
|
10.0
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
|
100.0
nM
|
|
|
Antiviral activity against Human immunodeficiency virus type 2 (ISOLATE ROD) after 13 months
|
Human immunodeficiency virus type 2 (ISOLATE ROD)
|
5.0
nM
|
|
|
Antiviral activity against Human immunodeficiency virus type 1 (BRU ISOLATE) after 13 months
|
Human immunodeficiency virus type 1 (BRU ISOLATE)
|
4.0
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
|
4.0
nM
|
|
|
Cmin in HIV-infected patient
|
Homo sapiens
|
700.0
nM
|
|
|
Inhibition of wild type HIV1 protease by FRET
|
Human immunodeficiency virus 1
|
0.008
nM
|
|
|
Inhibition of multidrug resistant HIV1 protease L101I, L36P, A71V, G73S, I84V, L90M mutant by FRET
|
Human immunodeficiency virus 1
|
0.025
nM
|
|
|
Antiviral activity against wild type Human immunodeficiency virus 1
|
Human immunodeficiency virus 1
|
0.4
nM
|
|
|
Antiviral activity against Human immunodeficiency virus 1 clade A isolated from HIV-AIDS patient
|
Human immunodeficiency virus 1
|
0.6
nM
|
|
|
Antiviral activity against Human immunodeficiency virus 1 clade B isolated from HIV-AIDS patient
|
Human immunodeficiency virus 1
|
0.4
nM
|
|
|
Antiviral activity against Human immunodeficiency virus 1 clade C isolated from HIV-AIDS patient
|
Human immunodeficiency virus 1
|
0.4
nM
|
|
|
Antiviral activity against multidrug resistant Human immunodeficiency virus 1 harboring protease M46I, I54V, V82A and L90M mutant
|
Human immunodeficiency virus 1
|
0.5
nM
|
|
|
Antiviral activity against multidrug resistant Human immunodeficiency virus 1 MDRC4
|
Human immunodeficiency virus 1
|
1.0
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
|
3.5
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
|
3.0
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
|
4.0
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
|
17.0
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
|
26.0
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
|
3.0
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
|
26.0
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
|
7.0
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
|
7.0
nM
|
|
|
Antiviral activity against HIV1 LAI infected in human MT2 cells by MTT assay
|
Human immunodeficiency virus 1
|
3.0
nM
|
|
|
Antiviral activity against HIV2 EHO infected in human MT2 cells by MTT assay
|
Human immunodeficiency virus 2
|
8.0
nM
|
|
|
Antiviral activity against HIV2 ROD infected in human MT2 cells by MTT assay
|
Human immunodeficiency virus type 2 (ISOLATE ROD)
|
10.0
nM
|
|
|
Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells by MTT assay
|
Human immunodeficiency virus 1
|
3.0
nM
|
|
|
Antiviral activity against HIV1 expressing protease L10I/G48V/I54V/A71V/I84V/L90M mutant infected in human MT4 cells selected at 5 uM of saquinavir by MTT assay
|
Human immunodeficiency virus 1
|
3.0
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
|
6.0
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
|
290.0
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
|
25.0
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
|
9.0
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
|
3.0
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
|
19.0
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
|
8.0
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
|
23.0
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
|
4.0
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
|
11.0
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
|
27.0
nM
|
|
|
Antiviral activity against HIV1 expressing protease L10I/L24I/M46I/V82I/I84V mutant infected in human MT4 cells selected after 50 passages of GRL-216 by MTT assay
|
Human immunodeficiency virus 1
|
9.0
nM
|
|
|
Antiviral activity against HIV1 expressing protease L10F/M46I/T91S mutant infected in human MT4 cells selected at 1 uM of GRL-246 by MTT assay
|
Human immunodeficiency virus 1
|
29.0
nM
|
|
|
Antiviral activity against HIV1 expressing protease L10F/M46L/I50V/A71Vmutant infected in human MT4 cells selected at 1 uM of GRL-286 by MTT assay
|
Human immunodeficiency virus 1
|
200.0
nM
|
|
|
Antiviral activity against HIV1 expressing protease L10F/M46M,I/Q61Q mutant infected in human MT4 cells selected at 1 uM of GRL-396 by MTT assay
|
Human immunodeficiency virus 1
|
16.0
nM
|
|
|
Antiviral activity against wild type HIV-1 ERS104 pre infected in human PHA-PBM cells assessed as inhibition of p24 Gag protein production
|
Human immunodeficiency virus 1
|
4.0
nM
|
|
|
Antiviral activity against HIV-1 MDR/B infected in human PHA-PBM cells assessed as inhibition of p24 Gag protein production
|
Human immunodeficiency virus 1
|
34.0
nM
|
|
|
Antiviral activity against HIV-1 MDR/C infected in human PHA-PBM cells assessed as inhibition of p24 Gag protein production
|
Human immunodeficiency virus 1
|
9.0
nM
|
|
|
Antiviral activity against HIV-1 MDR/G infected in human PHA-PBM cells assessed as inhibition of p24 Gag protein production
|
Human immunodeficiency virus 1
|
26.0
nM
|
|
|
Antiviral activity against HIV-1 MDR/TM infected in human PHA-PBM cells assessed as inhibition of p24 Gag protein production
|
Human immunodeficiency virus 1
|
22.0
nM
|
|
|
Antiviral activity against HIV-1 MDR/MM infected in human PHA-PBM cells assessed as inhibition of p24 Gag protein production
|
Human immunodeficiency virus 1
|
17.0
nM
|
|
|
Antiviral activity against HIV-1 MDR/JSL infected in human PHA-PBM cells assessed as inhibition of p24 Gag protein production
|
Human immunodeficiency virus 1
|
23.0
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
|
3.0
nM
|
|
|
Antiviral activity against wild type Human immunodeficiency virus 1 ERS104pre infected in PHA-stimulated human PBMC assessed as inhibition of p24 Gag protein production
|
Human immunodeficiency virus 1
|
3.7
nM
|
|
|
Antiviral activity against multidrug-resistant Human immunodeficiency virus 1 subtype B harboring protease L10I, L33I, M36I, M46I, F53L, K55R, I62 V, L63P, A71 V, G73S, V82A, L90M, I93L mutation infected in PHA-stimulated human PBMC assessed as inhibition of p24 Gag protein production
|
Human immunodeficiency virus 1
|
36.0
nM
|
|
|
Antiviral activity against multidrug-resistant Human immunodeficiency virus 1 MDR/C harboring protease L10I, I15 V, K20R, L24I, M36I, M46L, I54V, I62 V, L63P, K70Q, V82A, L89 M mutation infected in PHA-stimulated human PBMC assessed as inhibition of p24 Gag protein production
|
Human immunodeficiency virus 1
|
13.0
nM
|
|
|
Antiviral activity against multidrug-resistant Human immunodeficiency virus 1 MDR/G harboring protease L10I, V11I, T12E, I15 V, L19I, R41K, M46L, L63P, A71T, V82A, L90 M mutation infected in PHA-stimulated human PBMC assessed as inhibition of p24 Gag protein production
|
Human immunodeficiency virus 1
|
2.3
nM
|
|
|
Antiviral activity against multidrug-resistant Human immunodeficiency virus 1 MDR/TM harboring protease L10I, K14R, R41K, M46L, I54V, L63P, A71V, V82A, L90M, I93L mutation infected in PHA-stimulated human PBMC assessed as inhibition of p24 Gag protein production
|
Human immunodeficiency virus 1
|
1.9
nM
|
|
|
Antiviral activity against wild type HIV1 ERS104 infected in PHA-PBM cells assessed as inhibition of p24 Gag protein production
|
Human immunodeficiency virus 1
|
4.0
nM
|
|
|
Antiviral activity against HIV1 MDR/B harboring protease L10I, K14R, L33I, M36I, M46I, F53I, K55R, I62V, L63P, A71V, G73S, V82A, L90M, I93L mutant infected in PHA-PBM cells assessed as inhibition of p24 Gag protein production
|
Human immunodeficiency virus 1
|
19.0
nM
|
|
|
Antiviral activity against HIV1 MDR/C harboring protease L10I, I15V, K20R, L24I, M36I, M46L, I54V, I62V, L63P, K70Q, V82A, and L89 mutant infected in PHA-PBM cells assessed as inhibition of p24 Gag protein production
|
Human immunodeficiency virus 1
|
11.0
nM
|
|
|
Antiviral activity against HIV1 MDR/G harboring protease L10I, V11I, T12E, I15V, L19I, R41K, M46L, L63P, A71T, V82A, and L90M mutant infected in PHA-PBM cells assessed as inhibition of p24 Gag protein production
|
Human immunodeficiency virus 1
|
11.0
nM
|
|
|
Antiviral activity against HIV1 MDR/TM harboring protease L10I, K14R, R41K, M46L, I54V, L63P, A71V, V82A, L90M, I93L mutant infected in PHA-PBM cells assessed as inhibition of p24 Gag protein production
|
Human immunodeficiency virus 1
|
28.0
nM
|
|
|
Inhibition of HIV1 protease
|
Human immunodeficiency virus 1
|
0.016
nM
|
|
|
Antiviral activity against Human immunodeficiency virus 1 3B expressing wild-type protease infected in human MT4 cells
|
Human immunodeficiency virus 1
|
6.6
nM
|
|
|
Antiviral activity against Human immunodeficiency virus 1 isolate M1 expressing protease L10I, M46I, I64V, I84V, L90M, I93L mutant infected in human MT4 cells
|
Human immunodeficiency virus 1
|
11.3
nM
|
|
|
Antiviral activity against Human immunodeficiency virus 1 isolate M2 expressing protease L10I, I13V, M46I, I50V, L63P, L76V mutant infected in human MT4 cells
|
Human immunodeficiency virus 1
|
51.0
nM
|
|
|
Antiviral activity against Human immunodeficiency virus 1 isolate M3 expressing protease L10I, K20R, M36I, G48V, I62V, A71V, V82A, I93L mutant infected in human MT4 cells
|
Human immunodeficiency virus 1
|
2.3
nM
|
|
|
Antiviral activity against Human immunodeficiency virus 1 3B expressing wild-type protease infected in human MT4 cells in presence of 50% human serum
|
Human immunodeficiency virus 1
|
17.2
nM
|
|
|
Inhibition of Human immunodeficiency virus 1 3B protease
|
Human immunodeficiency virus 1
|
3.8
nM
|
|
|
Inhibition of wild type Human immunodeficiency virus protease expressed in Escherichia coli using ArgGlu(EDANS)SerGlnAsnTyrProIleValGlnLys(DABCYL)Arg as substrate preincubated with compound for 0.5 to 1 min measured by fluorometric analysis at pH 6.5
|
Human immunodeficiency virus
|
0.1
nM
|
|
|
Inhibition of Human immunodeficiency virus protease M8 mutant expressed in Escherichia coli using ArgGlu(EDANS)SerGlnAsnTyrProIleValGlnLys(DABCYL)Arg as substrate preincubated with compound for 0.5 to 1 min measured by fluorometric analysis at pH 6.5
|
Human immunodeficiency virus
|
0.25
nM
|
|
|
Inhibition of Human immunodeficiency virus protease M9 mutant expressed in Escherichia coli using ArgGlu(EDANS)SerGlnAsnTyrProIleValGlnLys(DABCYL)Arg as substrate preincubated with compound for 0.5 to 1 min measured by fluorometric analysis at pH 6.5
|
Human immunodeficiency virus
|
0.3
nM
|
|
|
Inhibition of Human immunodeficiency virus protease M10 mutant expressed in Escherichia coli using ArgGlu(EDANS)SerGlnAsnTyrProIleValGlnLys(DABCYL)Arg as substrate preincubated with compound for 0.5 to 1 min measured by fluorometric analysis at pH 6.5
|
Human immunodeficiency virus
|
1.0
nM
|
|
|
Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing wild type protease infected in human MT4 cells after 5 days by MTT assay
|
Human immunodeficiency virus 1
|
3.0
nM
|
|
|
Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M8 mutant infected in human MT4 cells after 5 days by MTT assay
|
Human immunodeficiency virus 1
|
16.0
nM
|
|
|
Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M9 mutant infected in human MT4 cells after 5 days by MTT assay
|
Human immunodeficiency virus 1
|
25.0
nM
|
|
|
Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M10 mutant infected in human MT4 cells after 5 days by MTT assay
|
Human immunodeficiency virus 1
|
130.0
nM
|
|
|
Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M3 mutant infected in human MT4 cells after 5 days by MTT assay
|
Human immunodeficiency virus 1
|
11.0
nM
|
|
|
Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M4 mutant infected in human MT4 cells after 5 days by MTT assay
|
Human immunodeficiency virus 1
|
30.0
nM
|
|
|
Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M5 mutant infected in human MT4 cells after 5 days by MTT assay
|
Human immunodeficiency virus 1
|
22.0
nM
|
|
|
Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M6 mutant infected in human MT4 cells after 5 days by MTT assay
|
Human immunodeficiency virus 1
|
10.0
nM
|
|
|
Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M7 mutant infected in human MT4 cells after 5 days by MTT assay
|
Human immunodeficiency virus 1
|
3.2
nM
|
|
|
Inhibition of HIV1 recombinant protease using Lys-Ala-Arg-Val-Nle-Nph-Glu-Ala-Nle-NH2 as substrate by spectrophotometric analysis
|
Human immunodeficiency virus 1
|
0.5
nM
|
|
|
Inhibition of HIV1 protease
|
Human immunodeficiency virus 1
|
0.016
nM
|
|
|
Antiviral activity against multidrug resistant HIV1 MDR1 containing protease M46I, I54V, V82A and L90M mutant infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay
|
Human immunodeficiency virus 1
|
0.23
nM
|
|
|
Antiviral activity against multidrug resistant HIV1 MDRC4 infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay
|
Human immunodeficiency virus 1
|
0.6
nM
|
|
|
Antiviral activity against wild type HIV1 clade C isolated form HIV1 patient infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay
|
Human immunodeficiency virus 1
|
0.18
nM
|
|
|
Antiviral activity against wild type HIV1 clade B isolated form HIV1 patient infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay
|
Human immunodeficiency virus 1
|
0.15
nM
|
|
|
Antiviral activity against wild type HIV1 clade A isolated form HIV1 patient infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay
|
Human immunodeficiency virus 1
|
0.3
nM
|
|
|
Antiviral activity against wild type HIV1 infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay
|
Human immunodeficiency virus 1
|
0.25
nM
|
|
|
Inhibition of HIV1 protease I50V, A71V mutant by FRET assay
|
Human immunodeficiency virus 1
|
0.001
nM
|
|
|
Inhibition of HIV1 protease L10I, L63P, A71V, G73S, I84V, L90M mutant by FRET assay
|
Human immunodeficiency virus 1
|
0.027
nM
|
|
|
Inhibition of HIV1 protease L10I, G48V, I54V, L63P and V82A mutant by FRET assay
|
Human immunodeficiency virus 1
|
0.004
nM
|
|
|
Inhibition of wild type HIV1 protease by FRET assay
|
Human immunodeficiency virus 1
|
0.0002
nM
|
|
|
Inhibition of HIV protease
|
Human immunodeficiency virus
|
0.015
nM
|
|
|
Antiviral activity against Human immunodeficiency virus 1 3B clinical isolate harboring L10I/K20R/M36I/G48V/ I62V/A71V/V82A/I93L protease mutant infected in human MT4 cells assessed as inhibition of viral replication
|
Human immunodeficiency virus 1
|
2.4
nM
|
|
|
Antiviral activity against Human immunodeficiency virus 1 3B clinical isolate harboring L10I/I13V/M46I/I50V/L63P/L76V protease mutant infected in human MT4 cells assessed as inhibition of viral replication
|
Human immunodeficiency virus 1
|
51.0
nM
|
|
|
Antiviral activity against Human immunodeficiency virus 1 3B clinical isolate harboring L10I/M46I/I64V/I84V/L90M/I93L protease mutant infected in human MT4 cells assessed as inhibition of viral replication
|
Human immunodeficiency virus 1
|
12.0
nM
|
|
|
Antiviral activity against wild type Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of viral replication in presence of 50% human plasma
|
Human immunodeficiency virus 1
|
17.0
nM
|
|
|
Antiviral activity against wild type Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of viral replication
|
Human immunodeficiency virus 1
|
6.6
nM
|
|
|
Antiviral activity against multidrug-resistant HIV1 TM harboring L10I/K14R/R41K/M46L/I54V/L63P/A71V/V82A/L90M/I93L protease-encoding region mutant infected in human PHA-PBMC cells assessed as inhibition of p24 Gag protein production
|
Human immunodeficiency virus 1
|
24.0
nM
|
|
|
Antiviral activity against multidrug-resistant HIV1 G harboring L10I/V11I/T12E/I15V/L19I/R41K/M46L/L63P/A71T/V82A/L90M protease-encoding region mutant infected in human PHA-PBMC cells assessed as inhibition of p24 Gag protein production.
|
Human immunodeficiency virus 1
|
19.0
nM
|
|
|
Antiviral activity against multidrug-resistant HIV1 C harboring L10I/I15V/K20R/L24I/M36I/M46L/I54V/I62V/L63P/K70Q/V82A/L89M protease-encoding region mutant infected in human PHA-PBMC cells assessed as inhibition of p24 Gag protein production
|
Human immunodeficiency virus 1
|
10.0
nM
|
|
|
Antiviral activity against wild type HIV1 ERS104pre infected in human PHA-PBMC cells assessed as inhibition of p24 Gag protein production
|
Human immunodeficiency virus 1
|
3.7
nM
|
|
|
Antiviral activity against HIV1 LAI infected in human MT2 cells by MTT assay
|
Human immunodeficiency virus 1
|
3.0
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
|
0.0046
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
|
2.3
nM
|
|
|
Inhibition of HIV1 protease expressed in Escherichia coli incubated for 20 to 30 mins at room temperature using (Arg-Glu(EDANS)-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-Lys(DABCYL)-Arg) substrate by FRET method
|
Human immunodeficiency virus 1
|
0.061
nM
|
|
|
Inhibition of wild type HIV1 protease
|
Human immunodeficiency virus 1
|
0.005
nM
|
|
|
Binding affinity to HIV1 protease PR20 mutant expressed in Escherichia coli BL21 (DE3) assessed as ligand dissociation constant by ITC method
|
Human immunodeficiency virus 1
|
41.0
nM
|
|
|
Antiviral activity against wild type HIV1 ERS104P infected in human MT4 cells assessed as virus-induced cytopathic effect by MTT assay
|
Human immunodeficiency virus 1
|
3.5
nM
|
|
|
Antiviral activity against multidrug resistant HIV1 MDR/B containing protease mutant infected in human MT4 cells assessed as inhibition of p24 Gag protein production
|
Human immunodeficiency virus 1
|
28.0
nM
|
|
|
Antiviral activity against multidrug resistant HIV1 MDR/C containing protease mutant infected in human MT4 cells assessed as inhibition of p24 Gag protein production
|
Human immunodeficiency virus 1
|
19.0
nM
|
|
|
Antiviral activity against multidrug resistant HIV1 MDR/G containing protease mutant infected in human MT4 cells assessed as inhibition of p24 Gag protein production
|
Human immunodeficiency virus 1
|
23.0
nM
|
|
|
Inhibition of HIV1 protease
|
Human immunodeficiency virus 1
|
0.016
nM
|
|
|
Antiviral activity against HIV1 LAI infected in human MT2 cells
|
Human immunodeficiency virus 1
|
3.0
nM
|
|
|
Antiviral activity against HIV1 NL4-3 infected in human MT4 cells by XTT assay
|
Human immunodeficiency virus 1
|
2.6
nM
|
|
|
Antiviral activity against darunavir-resistant HIV1 P10 infected in human MT4 cells by XTT assay
|
Human immunodeficiency virus 1
|
31.0
nM
|
|
|
Antiviral activity against darunavir-resistant HIV1 P20 infected in human MT4 cells by XTT assay
|
Human immunodeficiency virus 1
|
97.0
nM
|
|
|
Inhibition of HIV-1 protease by fluorometric assay
|
Human immunodeficiency virus 1
|
0.016
nM
|
|
|
Antiviral activity against HIV-1 LAI infected in MT-2 cells measured after 7 days by MTT assay
|
Human immunodeficiency virus 1
|
3.0
nM
|
|
|
Binding affinity to wild type HIV1 protease
|
Human immunodeficiency virus 1
|
0.008
nM
|
|
|
Binding affinity to HIV1 protease L10I mutant
|
Human immunodeficiency virus 1
|
0.005
nM
|
|
|
Binding affinity to HIV1 protease G48V mutant
|
Human immunodeficiency virus 1
|
0.005
nM
|
|
|
Binding affinity to HIV1 protease L63P mutant
|
Human immunodeficiency virus 1
|
0.005
nM
|
|
|
Binding affinity to HIV1 protease D30N mutant
|
Human immunodeficiency virus 1
|
0.041
nM
|
|
|
Binding affinity to HIV1 protease V82A mutant
|
Human immunodeficiency virus 1
|
0.005
nM
|
|
|
Binding affinity to HIV1 protease N88D mutant
|
Human immunodeficiency virus 1
|
0.041
nM
|
|
|
Binding affinity to HIV1 protease A71V mutant
|
Human immunodeficiency virus 1
|
0.025
nM
|
|
|
Binding affinity to HIV1 protease G73S mutant
|
Human immunodeficiency virus 1
|
0.025
nM
|
|
|
Binding affinity to HIV1 protease I84V mutant
|
Human immunodeficiency virus 1
|
0.025
nM
|
|
|
Binding affinity to HIV1 protease L90M mutant
|
Human immunodeficiency virus 1
|
0.025
nM
|
|
|
Binding affinity to HIV1 protease I50V mutant
|
Human immunodeficiency virus 1
|
0.33
nM
|
|
|
Binding affinity to HIV1 protease I54V mutant
|
Human immunodeficiency virus 1
|
0.005
nM
|
|
|
Binding affinity to HIV1 protease
|
Human immunodeficiency virus 1
|
0.016
nM
|
|
|
Inhibition of HIV1 protease using fluorogenic substrate by continuous fluorometric assay
|
Human immunodeficiency virus 1
|
0.016
nM
|
|
|
Antiviral activity against HIV1 LAI infected in human MT2 cells assessed as reduction in p24 Gag protein production incubated for 6 days by automated chemiluminescent enzyme immunoassay
|
Human immunodeficiency virus 1
|
3.2
nM
|
|
|
Inhibition of HIV-1 protease using fluorogenic substrate by fluorescence assay
|
Human immunodeficiency virus 1
|
0.016
nM
|
|
|
Anti-viral activity against HIV-1 LAI infected in human MT2 cells assessed as reduction in p24 Gag protein production
|
HIV-1 M:B_Lai
|
3.0
nM
|
|
|
Antiviral activity against wild type HIV-1 NL4-3 infected in human MT4 cells assessed as reduction in p24 Gag protein production
|
Human immunodeficiency virus 1
|
1.8
nM
|
|
|
Antiviral activity against darunavir-resistant HIV1 harboring protease L10I/I15/K20R/L24I/V32I/M36I/M46L/L63P/V82A/L89M mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production
|
Human immunodeficiency virus 1
|
87.0
nM
|
|
|
Inhibition of wild-type HIV-1 protease
|
Human immunodeficiency virus 1
|
0.016
nM
|
|
|
Antiviral activity against HIV-1 harboring protease I50V mutant
|
Human immunodeficiency virus 1
|
1.6
nM
|
|
|
Antiviral activity against amprenavir-resistant HIV1 NL4-3 harboring protease L10F/V32I/L33F/M46L/I54M/A71V mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay
|
Human immunodeficiency virus 1
|
25.0
nM
|
|
|
Antiviral activity against tipranavir-resistant HIV1 NL4-3 harboring protease L10I/L33I/M36I/M46I/I54V/K55R/I62V/L63P/A71V/G73S/V82T/L90M/I93L mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay
|
Human immunodeficiency virus 1
|
39.0
nM
|
|
|
Antiviral activity against lopinavir-resistant HIV1 NL4-3 harboring protease L10F/V32I/M46I/I47A/A71V/I84V mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay
|
Human immunodeficiency virus 1
|
430.0
nM
|
|
|
Antiviral activity against HIV1 Lai infected in human MT2 cells
|
HIV-1 M:B_Lai
|
3.2
nM
|
|
|
Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay
|
Human immunodeficiency virus 1
|
3.8
nM
|
|
|
Antiviral activity against darunavir-resistant HIV1 derived from 20 passages harboring protease L10I/I15V/K20R/L24I/V32I/M36I/M46L/L63P/V82A/L89M mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay
|
Human immunodeficiency virus 1
|
34.0
nM
|
|
|
Antiviral activity against darunavir-resistant HIV1 derived from 30 passages harboring protease L10I/I15V/K20R/L24I/V32I/M36I/M46L/L63P/K70R/V82A/I84V/L89M mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay
|
Human immunodeficiency virus 1
|
360.0
nM
|
|
|
Antiviral activity against nelfinavir-resistant HIV1 NL4-3 harboring protease L10F/K20T/D30N/K45I/A71V/V77I mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay
|
Human immunodeficiency virus 1
|
8.2
nM
|
|
|
Antiviral activity against saquinavir-resistant HIV1 NL4-3 harboring protease L10I/N37D/G48V/I54V/L63P/G73C/I84V/L90M mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay
|
Human immunodeficiency virus 1
|
45.0
nM
|
|
|
Antiviral activity against indinavir-resistant HIV1 NL4-3 harboring protease L10F/L24I/M46I/I54V/L63P/A71V/G73S/V82T mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay
|
Human immunodeficiency virus 1
|
30.0
nM
|
|
|
Antiviral activity against atazanavir-resistant HIV1 NL4-3 harboring protease L23I/E34Q/K43I/M46I/I50L/G51A/L63P/A71V/V82A/T91A mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay
|
Human immunodeficiency virus 1
|
36.0
nM
|
|
|
Inhibition of HIV1 protease expressed in Escherichia coli using Arg-Glu (EDANS)-Ser-GlnAsn-Tyr-Pro-Ile-Val-Gln-Lys(DABCYL)-Arg as substrate preincubated for 20 to 30 mins followed by substrate addition measured for 10 mins by FRET method
|
Human immunodeficiency virus 1
|
0.06
nM
|
|
|
Inhibition of HIV1 protease expressed in Escherichia coli using Val-Ser-Gln-Asn-(beta-naphtyl)Ala-Pro-Ile-Val as substrate preincubated for 30 mins followed by substrate addition measured after 1 hr by mass spectrometric method
|
Human immunodeficiency virus 1
|
0.013
nM
|
|
|
Antiviral activity against HIV1 infected in GFP expressing human MT4 cells assessed as inhibition of viral replication after 24 hrs in presence of 50% normal human serum
|
Human immunodeficiency virus 1
|
7.0
nM
|
|
|
Inhibition of DRV-resistant protease V32I/L33F/I54M/V82I mutant in HIV1 transfected in 293T cells after 48 hrs by lentiviral vector-based luciferase reporter gene assay
|
Human immunodeficiency virus 1
|
12.66
nM
|
|
|
Antiviral activity against wild-type HIV1 pNL4-3 infected in CMVdeltaR8.91 transfected 293T cells after 48 hrs by lentiviral vector-based luciferase reporter gene assay
|
Human immunodeficiency virus 1
|
0.82
nM
|
|
|
Inhibition of DRV-resistant protease V32I/L33F/I54M/I84V mutant in HIV1 transfected in 293T cells after 48 hrs by lentiviral vector-based luciferase reporter gene assay
|
Human immunodeficiency virus 1
|
112.08
nM
|
|
|
Inhibition of wild type HIV-1 NL4-3 protease expressed in Escherichia coli Rosetta (DE3)pLysS using Ac-Thr-Ile-Nle-Nle-Gln-Arg-NH2 as substrate by fluorescence assay
|
Human immunodeficiency virus 1
|
0.016
nM
|
|
|
Antiviral activity against HIV-1 LAI infected in human MT2 cells
|
Human immunodeficiency virus 1
|
3.2
nM
|
|
|
Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay
|
Human immunodeficiency virus 1
|
3.0
nM
|
|
|
Antiviral activity against ATV resistant HIV1 harboring protease L23I/E34Q/K43I/M46I/I50L/G51A/L63P/A71V/V82A/T91A mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay
|
Human immunodeficiency virus 1
|
24.0
nM
|
|
|
Antiviral activity against LPV resistant HIV1 harboring protease L10F/M46/I54V/V82A mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay
|
Human immunodeficiency virus 1
|
26.0
nM
|
|
|
Antiviral activity against APV resistant HIV1 harboring protease L10F/M46I/I50V/I85V mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay
|
Human immunodeficiency virus 1
|
200.0
nM
|
|
|
Inhibition of HIV1 wild type NL4-3 protease expressed in Escherichia coli Rosetta (DE3) pLysS using Abz-Thr-Ile-Nle-Phe-(pNO2)-Gln-Arg-NH2 as substrate preincubated for 5 to 10 mins followed by substrate addition measured after 1 hr by fluorescence assay
|
Human immunodeficiency virus 1
|
0.016
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
|
3.2
nM
|
|
|
Antiviral activity against Atazanavir-resistant HIV1 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
|
19.0
nM
|
|
|
Antiviral activity against lopinavir-resistant HIV1 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
|
301.0
nM
|
|
|
Antiviral activity against amprenavir-resistant HIV1 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
|
129.0
nM
|
|
|
Antiviral activity against darunavir-resistant HIV1 at passage 21 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
|
169.0
nM
|
|
|
Antiviral activity against darunavir-resistant HIV1 at passage 30 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
|
426.0
nM
|
|
|
Inhibition of HIV1 NL4-3 protease I84V mutant expressed in Escherichia coli TAP-106 cells using EDANS/DABCYL-labelled 10-amino acid containing natural MA/CA cleavage site as substrate preincubated for 1 hr followed by substrate addition and measured for 60 mins by FRET assay
|
Human immunodeficiency virus 1
|
0.025
nM
|
|
|
Inhibition of HIV1 NL4-3 protease I50V/A71V mutant expressed in Escherichia coli TAP-106 cells using EDANS/DABCYL-labelled 10-amino acid containing natural MA/CA cleavage site as substrate preincubated for 1 hr followed by substrate addition and measured for 60 mins by FRET assay
|
Human immunodeficiency virus 1
|
0.075
nM
|
|
|
Antiviral activity against wild-type HIV1 NL4-3 infected in human TZM-bl cells preincubated for 18 hrs followed by viral infection and measured after 48 hrs by luciferase reporter gene assay
|
Human immunodeficiency virus 1
|
5.5
nM
|
|
|
Antiviral activity against multidrug-resistant HIV1 NL4-3 SLK19 infected in human TZM-bl cells preincubated for 18 hrs followed by viral infection and measured after 48 hrs by luciferase reporter gene assay
|
Human immunodeficiency virus 1
|
33.0
nM
|
|
|
Antiviral activity against multidrug-resistant HIV1 NL4-3 VSL20 infected in human TZM-bl cells preincubated for 18 hrs followed by viral infection and measured after 48 hrs by luciferase reporter gene assay
|
Human immunodeficiency virus 1
|
320.0
nM
|
|
|
Inhibition of HIV1 protease expressed in Escherichia coli using Arg-Glu (EDANS)-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-Lys(DABCYL)-Arg as substrate preincubated for 20 to 30 mins followed by substrate addition and measured for 10 mins by FRET assay
|
Human immunodeficiency virus 1
|
1.12
nM
|
|
|
Antiviral activity against VSV-G pseudotyped HIV1 transfected in human 293T cells co-transfected with NL4-3 HIV1 supernatant infected in human SupT1 cells treated with compound for 48 hrs assessed as inhibition of viral infection at 10 uM after 48 hrs by luciferase assay (Rvb = 0 %)
|
Human immunodeficiency virus 1
|
83.21
%
|
|
|
Antiviral activity against wild-type HIV1 NL4-3 infected in human SupT1 cells infected with supernatants from virus-infected human TZM-bl cells after 48 hrs by luciferase reporter assay
|
Human immunodeficiency virus 1
|
6.0
nM
|
|
|
Antiviral activity against darunavir-resistant HIV1 NL4-3 infected in human SupT1 cells infected with supernatants from virus-infected human TZM-bl cells after 48 hrs by luciferase reporter assay
|
Human immunodeficiency virus 1
|
100.0
nM
|
|
|
Inhibition of HIV1 protease using RE(Edans)SGIFLETSK(Dabcyl)R as substrate by fluorescence method
|
Human immunodeficiency virus 1
|
0.01
nM
|
|
|
Inhibition of wild type HIV1 protease expressed in Escherichia coli using Arg-Glu (EDANS)-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-Lys(DABCYL)-Arg as substrate preincubated for 20 to 30 mins followed by substrate addition and measured for 10 mins by FRET assay
|
Human immunodeficiency virus 1
|
4.01
nM
|
|
|
Inhibition of HIV1 protease expressed in Escherichia coli using Arg-Glu (EDANS)-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-Lys(DABCYL)-Arg as substrate preincubated for 20 to 30 mins followed by substrate addition and measured for 10 mins by FRET assay
|
Human immunodeficiency virus 1
|
0.46
nM
|
|
|
Antiviral activity against HIV1 NL4-3 infected in human MT4 cells after 7 days by MTT assay
|
Human immunodeficiency virus 1
|
3.0
nM
|
|
|
Inhibition of HIV1 protease using Ac-Thr-Ile-Nle-Nle-Gln-Arg-NH2 substrate by continuous fluorometric assay
|
Human immunodeficiency virus 1
|
0.016
nM
|
|
|
Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as reduction in p24 Gag protein production incubated for 6 days and measured on day 7 by chemiluminescent enzyme immunoassay
|
Human immunodeficiency virus 1
|
3.2
nM
|
|
|
Inhibition of HIV-1 protease
|
Human immunodeficiency virus 1
|
0.016
nM
|
|
|
Antiviral activity against HIV1 LAI infected in human MT2 cells
|
HIV-1 M:B_Lai
|
3.2
nM
|
|
|
Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as reduction in p24 Gag protein production
|
Human immunodeficiency virus 1
|
4.2
nM
|
|
|
Antiviral activity against atazanavir resistant HIV1 harboring protease L23I/E34Q/K43I/M46I/I50L/G51A/L63P/A71V/V82A/T91A mutant infected in human MT4 cells assessed as reduction in p24 Gag production
|
Human immunodeficiency virus 1
|
26.0
nM
|
|
|
Antiviral activity against lopinavir resistant HIV1 harboring protease L10F/V32I/M46I/I47A/A71V/I84V mutant infected in human MT4 cells assessed as inhibition of p24 Gag production
|
Human immunodeficiency virus 1
|
360.0
nM
|
|
|
Antiviral activity against darunavir resistant HIV1 harboring protease P30 L10I/I15V/K20R/L24I/V32I/M36I/ M46L/L63P/K70Q/V82A/I84V/L89M mutant infected in human MT4 cells assessed as reduction in p24 Gag production
|
Human immunodeficiency virus 1
|
370.0
nM
|
|
|
Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells by p24 assay
|
Human immunodeficiency virus 1
|
1.8
nM
|
|
|
Antiviral activity against multi-drug resistant HIV1B harboring protease L10I/L33I/M36I/M46I/F53L/K55R/I62V/L63P/A71V/G73S/V82A/L90M/I93L mutant infected in human MT4 cells by p24 assay
|
Human immunodeficiency virus 1
|
43.0
nM
|
|
|
Antiviral activity against multi-drug resistant HIV1C harboring protease L10I/I15V/K20R/L24I/M36I/M46L/I54V/I62V/L63P/K70Q/V82A/L89M mutant infected in human MT4 cells by p24 assay
|
Human immunodeficiency virus 1
|
30.0
nM
|
|
|
Antiviral activity against darunavir resistant HIV1 harboring protease L10I/I15V/K20R/L24I/V32I/M36I/M46L/L63P/A71T/V82A/L89M mutant at 20 passages infected in human MT4 cells by p24 assay
|
Human immunodeficiency virus 1
|
87.0
nM
|
|
|
Inhibition of HIV1 protease by FRET assay
|
Human immunodeficiency virus 1
|
370.0
nM
|
|
|
Antiviral activity against wild type HIV-1
|
Human immunodeficiency virus 1
|
1.52
nM
|
|
|
Inhibition of wild type HIV1 protease expressed in Escherichia coli using Arg-Glu (EDANS)-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-Lys(DABCYL)-Arg as substrate preincubated for 20 to 30 mins followed by substrate addition and measured for 10 mins by FRET assay
|
Human immunodeficiency virus 1
|
0.34
nM
|
|
|
Antiviral activity against VSV-G pseudotyped HIV1 NL4-3 in human TZM-bl cells infected with virus particles extracted from human SupT1 cells infected with HIV1 NL4-3 at 10 uM incubated for 48 hrs assessed as inhibition of late stage viral infection by luciferase assay relative to control
|
Human immunodeficiency virus 1
|
100.0
%
|
|
|
Antiviral activity against VSV-G pseudotyped darunavir-resistant HIV1 NL4-3 in human SupT1 cells infected with supernatants of virus particles extracted from human 293T cells infected with darunavir-resistant HIV1 NL4-3 incubated for 48 hrs assessed as inhibition of late stage viral infection by single-round infection based luciferase reporter assay
|
Human immunodeficiency virus 1
|
240.0
nM
|
|
|
Antiviral activity against VSV-G pseudotyped wild type HIV1 NL4-3 in human SupT1 cells infected with supernatants of virus particles extracted from human 293T cells infected with wild type HIV1 NL4-3 incubated for 48 hrs assessed as inhibition of late stage viral infection by single-round infection based luciferase reporter assay
|
Human immunodeficiency virus 1
|
3.9
nM
|
|
|
Inhibition of HIV-1 protease expressed in Escherichia coli using Arg-Glu(EDANS)-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-Lys(DABCYL)-Arg as substrate preincubated for 20 to 30 mins followed by substrate addition by FRET based assay
|
Human immunodeficiency virus 1
|
2.92
nM
|
|
|
Antiviral activity against VSV-G pseudotyped darunavir-resistant HIV1 NL4-3 V32I, L33F,I54M and I84V mutant infected in human SUPT1 cells at 100 nM infected with supernatants from virus-infected human 293T cells after 48 hrs by luciferase assay relative to control
|
Human immunodeficiency virus 1
|
59.0
%
|
|
|
Antiviral activity against VSV-G pseudotyped wild type HIV1 NL4-3 infected in human TZM-b1 cells at 100 nM infected with supernatants from virus-infected human SUPT1 cells after 48 hrs by luciferase assay relative to control
|
Human immunodeficiency virus 1
|
95.0
%
|
|
|
Inhibition of HIV1 NL4-3 protease expressed in Escherichia coli TAP-106 cells using EDANS/DABCYL-labelled 10-amino acid containing protease cleavage site as substrate preincubated for 1 hr followed by substrate addition and measured for 60 mins by FRET assay
|
Human immunodeficiency virus 1
|
0.005
nM
|
|
|
Inhibition of HIV1 NL4-3 protease I84V mutant expressed in Escherichia coli TAP-106 cells using EDANS/DABCYL-labelled 10-amino acid containing protease cleavage site as substrate preincubated for 1 hr followed by substrate addition and measured for 60 mins by FRET assay
|
Human immunodeficiency virus 1
|
0.025
nM
|
|
|
Inhibition of HIV1 NL4-3 protease I50V/A71V mutant expressed in Escherichia coli TAP-106 cells using EDANS/DABCYL-labelled 10-amino acid containing protease cleavage site as substrate preincubated for 1 hr followed by substrate addition and measured for 60 mins by FRET assay
|
Human immunodeficiency virus 1
|
0.075
nM
|
|
|
Antiviral activity against wild-type HIV1 NL4-3 infected in human TZM-bl cells infected with supernatants from virus-infected human 293T cells treated with compound for 18 hrs assessed as reduction in viral replication by luciferase assay
|
Human immunodeficiency virus 1
|
5.0
nM
|
|
|
Antiviral activity against wild type HIV1 assessed as inhibitory effect on virus producing cells at 10 uM by cell based inhibition assay
|
Human immunodeficiency virus 1
|
30.77
%
|
|
|
Inhibition of recombinant HIV1 protease measured assessed as hydrolysis of fluorogenic substrate by FRET assay
|
Human immunodeficiency virus 1
|
1.72
nM
|
|
|
Antiviral activity against HIV1 NL4-3 infected in human MT4 cells incubated for 7 days by fully automated chemiluminescent enzyme immunoassay
|
Human immunodeficiency virus 1
|
4.6
nM
|
|
|
Antiviral activity against LPV-resistant HIV1 infected in human MT4 cells incubated for 7 days by fully automated chemiluminescent enzyme immunoassay
|
Human immunodeficiency virus 1
|
50.0
nM
|
|
|
Antiviral activity against ATV-resistant HIV1 infected in human MT4 cells incubated for 7 days by fully automated chemiluminescent enzyme immunoassay
|
Human immunodeficiency virus 1
|
11.0
nM
|
|
|
Antiviral activity against DRV resistant HIV1 infected in human MT4 cells incubated for 7 days by fully automated chemiluminescent enzyme immunoassay
|
Human immunodeficiency virus 1
|
316.0
nM
|
|
|
Antiviral activity against HIV1 DRVR P30 infected in human MT4 cells incubated for 7 days by fully automated chemiluminescent enzyme immunoassay
|
Human immunodeficiency virus 1
|
424.0
nM
|
|
|
Inhibition of wild type HIV1 protease expressed in Escherichia coli using Arg-Glu (EDANS)-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-Lys(DABCYL)-Arg as substrate preincubated for 20 to 30 mins followed by substrate addition and measured for 10 mins by FRET assay
|
Human immunodeficiency virus 1
|
1.52
nM
|
|
|
Antiviral activity against HIV1 NL4-3 Env-deficient VSV-G pseudotyped virus infected in human SUP-T1 cells assessed as inhibition of late stage viral production when host cells were infected with compound pretreated viral particles at 10 uM measured after 48 hrs by luciferase assay relative to control
|
Human immunodeficiency virus 1
|
99.0
%
|
|
|
Antiviral activity against HIV1 NL4-3 VSV-G pseudotyped virus infected in human SUP-T1 cells assessed as inhibition of early stage viral production at 10 uM measured after 48 hrs by luciferase assay relative to control
|
Human immunodeficiency virus 1
|
2.0
%
|
|
|
Inhibition of wild type HIV1 protease using Arg-Glu (EDANS)-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-Lys(DABCYL)-Arg as substrate preincubated for 20 to 30 mins followed by substrate addition and measured for 10 mins by FRET assay
|
Human immunodeficiency virus 1
|
0.18
nM
|
|
|
Antiviral activity against HIV1
|
Human immunodeficiency virus 1
|
0.82
nM
|
|
|
Antiviral activity against HIV1 Env-deficient VSV-G pseudotyped virus infected in human SUP-T1 cells infected with supernatant of compound treated virus-producing 293T cells assessed as inhibition of late stage viral production at 100 nM treated for 48 hrs with virus-producing 293T cells followed by SUP-T1 cells infection for 48 hrs by single-round infection luciferase assay relative to control
|
Human immunodeficiency virus 1
|
100.0
%
|
|
|
Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as reduction in viral replication by measuring reduction in p24 Gag production by chemiluminescent-EIA
|
Human immunodeficiency virus 1
|
3.9
nM
|
|
|
Antiviral activity against DRV resistant HIV1 infected in human MT4 cells assessed as reduction in viral replication by measuring reduction in p24 Gag production by chemiluminescent-EIA
|
Human immunodeficiency virus 1
|
240.0
nM
|
|
|
Antiviral activity against HIV1 subtype C isolate 11941
|
Human immunodeficiency virus 1
|
910.0
nM
|
|
