|
Antiviral activity as inhibition of human liver microsomal Cytochrome P450 3A4
|
Homo sapiens
|
250.0
nM
|
|
|
Inhibition of human cytochrome P450 3A4
|
None
|
30.0
nM
|
|
|
Binding affinity for HIV -1 Protease
|
Human immunodeficiency virus 1
|
0.37
nM
|
|
|
The activity against HIV multiply mutated strain M36M/I,V82V/A was determined from patient number 304
|
Human immunodeficiency virus 1
|
54.0
nM
|
|
|
The activity against HIV mutant strain V82F was determined from patient number 313
|
Human immunodeficiency virus 1
|
123.0
nM
|
|
|
The activity against HIV mutant strain V82S was determined from patient number 337
|
Human immunodeficiency virus 1
|
143.0
nM
|
|
|
The activity against HIV strain was determined from patient number 302
|
Human immunodeficiency virus 1
|
23.0
nM
|
|
|
The activity against HIV was determined from patient number 129
|
Human immunodeficiency virus 1
|
5.0
nM
|
|
|
The activity against HIV was determined from patient number 304
|
Human immunodeficiency virus 1
|
19.0
nM
|
|
|
The activity against HIV was determined from patient number 313
|
Human immunodeficiency virus 1
|
35.0
nM
|
|
|
The activity against HIV was determined from patient number 337
|
Human immunodeficiency virus 1
|
35.0
nM
|
|
|
The activity against multiply mutated strain M36I,I54V,A71V,V82T was determined from patient number 129
|
Human immunodeficiency virus 1
|
65.0
nM
|
|
|
The activity against mutant HIV molecular clone V82A was determined
|
Human immunodeficiency virus 1
|
0.23
nM
|
|
|
The activity against mutant HIV molecular clone V82F was determined
|
Human immunodeficiency virus 1
|
0.308
nM
|
|
|
The activity against mutant HIV molecular clone V82T was determined
|
Human immunodeficiency virus 1
|
0.316
nM
|
|
|
The activity against mutant HIV molecular clone wt (pNL4-3) was determined
|
Human immunodeficiency virus 1
|
0.055
nM
|
|
|
Fold increase in EC50 for antiviral activity against HIV Protease-Resistant strains with A protease amino acid substitutions
|
Human immunodeficiency virus 1
|
38.0
|
|
|
Fold increase in EC50 for antiviral activity against HIV Protease-Resistant strains with B protease amino acid substitutions
|
Human immunodeficiency virus 1
|
9.0
|
|
|
Fold increase in EC50 for antiviral activity against HIV Protease-Resistant strains with C protease amino acid substitutions
|
Human immunodeficiency virus 1
|
39.0
|
|
|
Fold increase in EC50 for antiviral activity against HIV Protease-Resistant strains with D protease amino acid substitutions
|
Human immunodeficiency virus 1
|
23.0
|
|
|
Fold increase in EC50 for antiviral activity against HIV Protease-Resistant strains with E protease amino acid substitutions
|
Human immunodeficiency virus 1
|
44.0
|
|
|
The activity against HIV mutant strain V82A was determined from patient number 302
|
Human immunodeficiency virus 1
|
32.0
nM
|
|
|
Inhibitory activity against purified HIV protease
|
None
|
0.02
nM
|
|
|
Inhibitory potency towards recombinant HIV-1 protease using fluorogenic substrate was evaluated
|
None
|
74.4
%
|
|
|
Inhibition constant of ritonavir towards HIV protease was determined
|
None
|
0.015
nM
|
|
|
Tested for inhibitor binding of D25N/V82A mutant of HIV PR
|
human immunodeficiency virus type1
|
0.12
nM
|
|
|
Tested for inhibitor binding of wild-type HIV PR
|
human immunodeficiency virus type1
|
0.015
nM
|
|
|
Antiviral activity was assessed against I54I/V, A71V, V82A, L90L/M viral strains isolated from patient-235 pretreated with ritonavir (4 fold) at 36th week
|
Human immunodeficiency virus 1
|
87.0
nM
|
|
|
Antiviral activity was assessed against K20K/R, 36M/I, 154V, A71A/V, V82T viral strains isolated from patient-129 pretreated with ritonavir(33 fold) at 16th week
|
Human immunodeficiency virus 1
|
368.0
nM
|
|
|
Antiviral activity was assessed against K20K/R, M36M/I, 154V/I, L63L/P, V82/A viral strains isolated from patient-131 pretreated with ritonavir(20 fold) at 28th week
|
Human immunodeficiency virus 1
|
365.0
nM
|
|
|
Antiviral activity was assessed against M36I, I54V, A71V, V82T viral strains isolated from patient-129 pretreated with ritonavir(14 fold) at 8th week
|
Human immunodeficiency virus 1
|
149.0
nM
|
|
|
Antiviral activity was assessed against M36M/I, I54I/V, V82F/A/S/T viral strains isolated from patient-313 pretreated with ritonavir(14 fold) at 85th day
|
Human immunodeficiency virus 1
|
575.0
nM
|
|
|
Antiviral activity was assessed against M36M/I, V82F viral strains isolated from patient-313 pretreated with ritonavir(9 fold) at 57th day
|
Human immunodeficiency virus 1
|
340.0
nM
|
|
|
Antiviral activity was tested in absence of human serum in MT-4 cells (in vitro)
|
Human immunodeficiency virus 1
|
70.0
nM
|
|
|
Antiviral activity was tested in presence of 50% human serum in MT-4 cells (in vitro)
|
Human immunodeficiency virus 1
|
810.0
nM
|
|
|
Tested for its anti-HIV activity in MT-4 cells in the presence of 50% human serum.
|
None
|
810.0
nM
|
|
|
Tested for its anti-HIV activity in MT-4 cells.
|
None
|
70.0
nM
|
|
|
Anti-HIV activity against MT-4 cells using a cytopathicity assay
|
Human immunodeficiency virus 1
|
22.0
nM
|
|
|
Inhibitory potency towards recombinant HIV-1 3B in MT-4 cell was evaluated in 0% human plasma
|
Homo sapiens
|
90.0
nM
|
|
|
Anti-HIV activity was determined in MT-4 cells in the presence of 0% human serum using cytopathic effect assay
|
Human immunodeficiency virus 1
|
70.0
nM
|
|
|
Anti-HIV activity was determined in MT-4 cells in the presence of 50% human serum using cytopathic effect assay
|
Human immunodeficiency virus 1
|
810.0
nM
|
|
|
Compound was evaluated for its antiviral inhibition in MT-4 cell culture
|
Homo sapiens
|
210.0
nM
|
|
|
Inhibition of P-gp was determined using rhodamine-assay in human CaCo-2 cells
|
None
|
116.0
%
|
|
|
Inhibition of HIV protease
|
Human immunodeficiency virus 1
|
0.02
nM
|
|
|
Binding affinity to inhibit the purified wild-type HIV-1 Protease
|
Human immunodeficiency virus 1
|
0.37
nM
|
|
|
Inhibition constant against HIV-1 Protease
|
Human immunodeficiency virus 1
|
0.59
nM
|
|
|
Inhibitory concentration against HIV-1 protease
|
Human immunodeficiency virus 1
|
0.82
nM
|
|
|
Tested for its inhibition against HIV protease at a concentration of 0.5 nM.
|
Human immunodeficiency virus 1
|
78.0
%
|
|
|
Inhibition of HIV protease at 0.5 nM
|
Human immunodeficiency virus 1
|
78.0
%
|
|
|
Inhibitory activity against HIV protease at a compound concentration of 0.5 nM in MT-4 cells
|
Human immunodeficiency virus 1
|
78.0
%
|
|
|
Equilibrium constant for the interaction between inhibitor and HIV-1 Protease
|
Human immunodeficiency virus 1
|
0.608
nM
|
|
|
Affinity against HIV protease
|
Human immunodeficiency virus 1
|
0.37
nM
|
|
|
Inhibitory activity against HIV-1 protease
|
Human immunodeficiency virus 1
|
0.37
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
|
60.0
nM
|
|
|
Dissociation constant obtained by inhibition of mutant HIV-protease (K-60)
|
None
|
40.0
nM
|
|
|
Dissociation constant obtained by inhibition of mutant HIV-protease (V-18)
|
None
|
23.0
nM
|
|
|
Binding affinity for human immunodeficiency virus type 1 protease
|
Human immunodeficiency virus 1
|
0.6
nM
|
|
|
Inhibition constant for human immunodeficiency virus type 1 protease
|
Human immunodeficiency virus 1
|
0.59
nM
|
|
|
Percent inhibition of human immunodeficiency virus type I (HIV-1) protease was determined at 50 uM concentration
|
Human immunodeficiency virus 1
|
100.0
%
|
|
|
Percent inhibition of recombinant human T-cell leukemia virus type I (HTLV-1) protease was determined at 100 uM concentration
|
human T-cell leukemia virus type 1
|
20.0
%
|
|
|
Percent inhibition of synthesized human T-cell leukemia virus type I (HTLV-1) protease was determined at 100 uM concentration
|
human T-cell leukemia virus type 1
|
20.0
%
|
|
|
Inhibitory concentration against wild type human immunodeficiency virus
|
Human immunodeficiency virus 1
|
67.0
nM
|
|
|
Inhibitory concentration of compound against HIV LAI in MT-2 cells when tested at a range of 0.001-10 uM concentration
|
Homo sapiens
|
10.0
nM
|
|
|
Inhibitory concentration of compound against HIV LAI in MT-4 cells when tested at a range of 0.001-10 uM concentration
|
Homo sapiens
|
10.0
nM
|
|
|
Inhibitory activity against HIV1 protease at 0.5 uM
|
Human immunodeficiency virus 1
|
79.0
%
|
|
|
Antiviral activity against HIV1 in the absence of human serum
|
Human immunodeficiency virus 1
|
22.0
nM
|
|
|
Antiviral activity against HIV1 in the presence of 50% human serum
|
Human immunodeficiency virus 1
|
483.0
nM
|
|
|
Antiviral activity against HIV1 HXB2 in MT4 cells
|
None
|
268.0
nM
|
|
|
Antiviral activity against HIV1 LAI isolate in human MT2 cells
|
Human immunodeficiency virus 1
|
34.0
nM
|
|
|
Antiviral activity against HIV1 LAI isolate in human PHA-PBMC cells
|
Human immunodeficiency virus 1
|
43.0
nM
|
|
|
Antiviral activity against HIV1 BA-L isolate in human PHA-PBMC cells
|
Human immunodeficiency virus 1
|
36.0
nM
|
|
|
Antiviral activity against HIV2 EHO isolate in human MT2 cells
|
Human immunodeficiency virus 2
|
290.0
nM
|
|
|
Antiviral activity against multi drug-resistant HIV1 ET variant in human PHA-PBMC cells
|
Human immunodeficiency virus 1
|
15.0
nM
|
|
|
Antiviral activity against multi drug-resistant HIV1 K variant in human PHA-PBMC cells
|
Human immunodeficiency virus 1
|
57.0
nM
|
|
|
Antimalarial activity against Plasmodium falciparum Dd2
|
Plasmodium falciparum
|
850.0
nM
|
|
|
Inhibition of HIV protease at 1 nM
|
Human immunodeficiency virus
|
90.0
%
|
|
|
Antiviral activity against HIV1 3B in MT4 cells by MTT assay
|
Human immunodeficiency virus 1
|
36.0
nM
|
|
|
Antiviral activity against HIV1 NL432
|
Human immunodeficiency virus 1
|
80.0
nM
|
|
|
Antiviral activity against ritonavir-resistant HIV1 NL432
|
Human immunodeficiency virus 1
|
220.0
nM
|
|
|
Antiviral activity against nelfinavir-resistant HIV1 NL432
|
Human immunodeficiency virus 1
|
16.0
nM
|
|
|
Antiviral activity against ritonavir and nelfinavir-resistant HIV1 NL432
|
Human immunodeficiency virus 1
|
162.0
nM
|
|
|
Inhibition of HIV1 Protease M1 variant by FRET based assay
|
Human immunodeficiency virus 1
|
3.025
nM
|
|
|
Inhibition of HIV1 Protease M2 variant by FRET based assay
|
Human immunodeficiency virus 1
|
0.46
nM
|
|
|
Inhibition of HIV1 Protease M3 variant by FRET based assay
|
Human immunodeficiency virus 1
|
2.81
nM
|
|
|
Inhibition of HIV1 protease
|
Human immunodeficiency virus 1
|
0.098
nM
|
|
|
Antiviral activity against HIV1 3B
|
Human immunodeficiency virus 1
|
2.0
nM
|
|
|
Antiviral activity against HIV1 3B in presence of 50% human serum
|
Human immunodeficiency virus 1
|
41.0
nM
|
|
|
Antiviral activity against wild type HIV1
|
Human immunodeficiency virus 1
|
16.0
nM
|
|
|
Antiviral activity against HIV1 LAI in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 1
|
54.0
nM
|
|
|
Antiviral activity against HIV2 EHO in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 2
|
210.0
nM
|
|
|
Antiviral activity against HIV2 ROD in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 2
|
260.0
nM
|
|
|
Antiviral activity against HIV1 NL4-3 in MT4 cells by MTT assay
|
Human immunodeficiency virus 1
|
33.0
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
|
51.0
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
|
290.0
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
|
120.0
nM
|
|
|
Antiviral activity against HIV1 GRL98065p20 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 1
|
130.0
nM
|
|
|
Antiviral activity against HIV1 GRL98065p30 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 1
|
300.0
nM
|
|
|
Antiviral activity against HIV1 GRL98065p40 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
Human immunodeficiency virus 1
|
380.0
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
|
25.0
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
|
71.0
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
|
41.0
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
|
23.0
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
|
39.0
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
|
30.0
nM
|
|
|
Antiviral activity against HIV1 in presence of 50% human serum
|
Human immunodeficiency virus 1
|
100.0
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
|
46.0
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
|
349.0
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
|
514.0
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
|
665.0
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
|
421.0
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
|
310.0
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
|
115.0
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
|
84.0
nM
|
|
|
Inhibition of HIV1 protease
|
Human immunodeficiency virus 1
|
0.034
nM
|
|
|
Antiviral activity against wild type HIV1 NL4-3 infected in MT4 cells after 6 days by MTT assay
|
Human immunodeficiency virus 1
|
61.0
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
|
34.0
nM
|
|
|
Inhibition of HIV1 protease at 1 nM
|
Human immunodeficiency virus 1
|
90.0
%
|
|
|
Antiviral activity against HIV1 3B in human MT4 cells assessed as inhibition of viral-induced cytopathic effect by MTT method
|
Human immunodeficiency virus 1
|
36.0
nM
|
|
|
Antiviral activity against wild type HIV1 NL432
|
Human immunodeficiency virus 1
|
80.0
nM
|
|
|
Antiviral activity against nelfinavir-resistant HIV1 NL432
|
Human immunodeficiency virus 1
|
16.0
nM
|
|
|
Antiviral activity against ritonavir-resistant HIV1 NL432
|
Human immunodeficiency virus 1
|
220.0
nM
|
|
|
Antiviral activity against ritonavir and nelfinavir-resistant HIV1 NL432
|
Human immunodeficiency virus 1
|
162.0
nM
|
|
|
Antiviral activity against HIV1 3B in presence of 10% fetal calf serum
|
Human immunodeficiency virus 1
|
24.0
nM
|
|
|
Antiviral activity against HIV1 3B in presence of 10% fetal calf serum and alpha1 acid glycoprotein
|
Human immunodeficiency virus 1
|
422.0
nM
|
|
|
Inhibition of HIV1 protease expressed in Escherichia coli by fluorometric assay
|
Human immunodeficiency virus 1
|
0.8
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
|
50.0
nM
|
|
|
Inhibition of human recombinant CYP3A4-mediated oxidation of 7-benzyloxyquinoline
|
Homo sapiens
|
50.0
nM
|
|
|
Intrinsic clearance in human liver microsomes
|
Homo sapiens
|
40.0
nM
|
|
|
Antimicrobial activity against Plasmodium yoelii 265 liver infected in mammalian hepatocytes after 48 hrs
|
Plasmodium yoelii yoelii
|
34.2
nM
|
|
|
Inhibition of human CYP3A4
|
Homo sapiens
|
100.0
nM
|
|
|
Antiviral activity against HIV 1 3B infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
|
Human immunodeficiency virus 1
|
55.0
nM
|
|
|
Antiviral activity against HIV 1 3B harboring integrase E92Q S230N double mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 20 passages in presence of compound
|
Human immunodeficiency virus 1
|
69.0
nM
|
|
|
Antiviral activity against HIV 1 3B harboring integrase L34M mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 40 passages in presence of compound
|
Human immunodeficiency virus 1
|
69.0
nM
|
|
|
Antiviral activity against HIV 1 3B harboring integrase E92Q, S230N and L34M triple mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 60 passages in presence of compound
|
Human immunodeficiency virus 1
|
60.0
nM
|
|
|
Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
|
Human immunodeficiency virus 1
|
43.0
nM
|
|
|
Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 20 passages selected in presence of compound
|
Human immunodeficiency virus 1
|
39.0
nM
|
|
|
Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 40 passages selected in presence of compound
|
Human immunodeficiency virus 1
|
42.0
nM
|
|
|
Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 60 passages selected in presence of compound
|
Human immunodeficiency virus 1
|
41.0
nM
|
|
|
Antiviral activity against HIV 1 NL4.3 assessed as inhibition of virus-induced cytopathic effect by MTT assay
|
Human immunodeficiency virus 1
|
130.0
nM
|
|
|
Antiviral activity against HIV 1 NL4.3 harboring integrase L74M mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
|
Human immunodeficiency virus 1
|
60.0
nM
|
|
|
Antiviral activity against HIV 1 NL4.3 integrase E92Q mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
|
Human immunodeficiency virus 1
|
58.0
nM
|
|
|
Antiviral activity against HIV 1 NL4.3 integrase S230N mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
|
Human immunodeficiency virus 1
|
90.0
nM
|
|
|
Antiviral activity against HIV1 LAI infected in human MT2 cells after 7 days by MTT assay
|
Human immunodeficiency virus
|
38.0
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
|
36.0
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
|
36.0
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
|
21.0
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
|
80.0
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
|
140.0
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
|
260.0
nM
|
|
|
Mechanism based inhibition of human cytochrome P450 3A4
|
Homo sapiens
|
100.0
nM
|
|
|
Mechanism based inhibition of human cytochrome P450 3A5
|
Homo sapiens
|
120.0
nM
|
|
|
DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968)
|
None
|
874.0
nM
|
|
|
DRUGMATRIX: Thromboxane Synthetase enzyme inhibition (substrate: PGH2)
|
Homo sapiens
|
76.0
nM
|
|
|
DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
|
None
|
16.0
nM
|
|
|
DRUGMATRIX: CYP450, 3A4 enzyme inhibition (substrate: 7-Benzyloxy-4-(trifluoromethyl)-coumarin)
|
None
|
16.0
nM
|
|
|
Inhibition of human CYP3A4 in liver microsomes
|
Homo sapiens
|
100.0
nM
|
|
|
Antiviral activity against wild type HIV1 3B infected in human MT4 LTR-EGFP cells by EGFP reporter gene assay
|
Human immunodeficiency virus 1
|
1.5
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
|
92.3
%
|
|
|
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
|
85.1
%
|
|
|
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
|
93.6
%
|
|
|
Time dependent inhibition of CYP3A4-mediated testosterone-6-beta hydroxylation in human liver microsome
|
Homo sapiens
|
170.0
nM
|
|
|
Inhibition of human MATE1-mediated [14]-metformin uptake expressed in HEK293 cells after 1.5 mins by scintillation counting analysis
|
Homo sapiens
|
80.0
nM
|
|
|
Inhibition of C-terminal His-tagged wild type CYP3A4 (unknown origin)-mediated hydroxylation of 7-benzyloxy-4-trifluoromethylcoumarin expressed in Escherichia coli after 5 mins by fluorimetric analysis
|
Homo sapiens
|
550.0
nM
|
|
|
Inhibition of HIV1 protease at 50 uM relative to control
|
Human immunodeficiency virus 1
|
72.0
%
|
|
|
Inhibition of HIV-1 protease
|
Human immunodeficiency virus 1
|
0.6
nM
|
|
|
Antiviral activity against HIV1 by cell based assay
|
Human immunodeficiency virus 1
|
50.0
nM
|
|
|
Antiviral activity against HIV1 by cell based assay
|
Human immunodeficiency virus 1
|
15.0
nM
|
|
|
Inhibition of human CYP3A4-mediated midazolam 1'-hydroxylase activity
|
Homo sapiens
|
110.0
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
|
0.314
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
|
32.2
nM
|
|
|
Inhibition of CYP3A4-mediated lopinavir bioactivation in human liver microsomes assessed as inhibition of lopinavir-GSH adduct I and II formation at 2 uM after after 50 mins by UPLC-TOFMS analysis
|
Homo sapiens
|
80.0
%
|
|
|
Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate
|
Homo sapiens
|
700.0
nM
|
|
|
Time dependent inhibition of CYP1A2 (unknown origin) at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Time dependent inhibition of CYP2C8 (unknown origin) at 10 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Time dependent inhibition of CYP2C9 (unknown origin) at 3 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Time dependent inhibition of CYP2C19 in human liver microsomes at 10 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Time dependent inhibition of CYP2D6 (unknown origin) at 10 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Time dependent inhibition of CYP3A4 (unknown origin) at 1 uM by LC/MS system
|
Homo sapiens
|
75.0
%
|
|
|
Time dependent inhibition of CYP2B6 (unknown origin) at 0.3 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay
|
Human immunodeficiency virus 1
|
90.0
nM
|
|
|
Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay
|
Human immunodeficiency virus type 2 (ISOLATE ROD)
|
140.0
nM
|
|
|
Antiviral activity against nevirapine-resistant SIV mac251 infected in human MT4 cells
|
Simian immunodeficiency virus - mac251
|
140.0
nM
|
|
|
Inhibition of HIV1 3B protease infected in human MT4 cells assessed as protection from virus induced cytopathogenicity measured after 5 days post infection by MTT assay
|
Human immunodeficiency virus 1
|
150.0
nM
|
|
|
Antibacterial activity against Staphylococcus aureus MRSA ATCC 43300 (CO-ADD:GP_020); MIC in CAMBH media, using NBS plates, by OD(600)
|
Staphylococcus aureus subsp. aureus
|
13.2
%
|
|
|
Antibacterial activity against Escherichia coli ATCC 25922 (CO-ADD:GN_001); MIC in CAMBH media using NBS plates, by OD(600)
|
Escherichia coli
|
-0.63
%
|
|
|
Antibacterial activity against Klebsiella pneumoniae MDR ATCC 70063 (CO-ADD:GN_003); MIC in CAMBH media using NBS plates, by OD(600)
|
Klebsiella pneumoniae
|
14.84
%
|
|
|
Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 (CO-ADD:GN_042); MIC in CAMBH media using NBS plates, by OD(600)
|
Pseudomonas aeruginosa
|
15.52
%
|
|
|
Antibacterial activity against Acinetobacter baumannii ATCC 19606 (CO-ADD:GN_034); MIC in CAMBH media using NBS plates, by OD600
|
Acinetobacter baumannii
|
28.09
%
|
|
|
Antifungal activity against Candida albicans ATCC 90028 (CO-ADD:FG_001); MIC in YNB media using NBS plates, by OD630
|
Candida albicans
|
1.82
%
|
|
|
Antifungal activity against Cryptococcus neoformans H99 ATCC 208821 (CO-ADD:FG_002); MIC in YNB media using NBS plates, by Resazurin OD(600-570)
|
Cryptococcus neoformans
|
-5.87
%
|
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells at 10 uM after 48 hours by high content imaging
|
Homo sapiens
|
4.58
%
|
|
|
Antiviral activity against Human immunodeficiency virus 1
|
Human immunodeficiency virus 1
|
25.0
nM
|
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
15.19
%
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
-1.934
%
|
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
-0.1
%
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
-0.2
%
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
-0.1
%
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
-0.2
%
|
|
|
Inhibition of human full length CYP3A4 assessed using 7-benzyloxy-4 (trifluoromethyl)coumarin as substrate preincubated for 20 mins in presence of NADPH followed by substrate addition and measured for 2 mins by fluorometric analysis
|
Homo sapiens
|
130.0
nM
|
|
|
Inhibition of HIV-1 protease at 20 uM relative to control
|
Human immunodeficiency virus 1
|
99.8
%
|
|
|
Binding affinity to recombinant Cryptococcus neoformans var. grubii H99 major aspartyl peptidase 1 assessed as inhibition constant
|
Cryptococcus neoformans var. grubii H99
|
1.8
nM
|
|
