|
Inhibition of MAMC O-dealkylation mediated by human Cytochrome P450 2D6 expressed in human lymphoblastoid cell line
|
Homo sapiens
|
3.3
nM
|
|
|
Parasympatholytic activity and the % inhibition of guinea pig ileum contractile force at 4 mg/L of base was reported.
|
Cavia porcellus
|
62.0
%
|
|
|
Parasympatholytic activity was assessed from the ability to inhibit electrically stimulated contraction of isolated guinea pig ileum at 4 mg/L of base
|
Cavia porcellus
|
62.0
%
|
|
|
Inhibition of 1'-hydroxybufuralol formation by human liver microsomes
|
Homo sapiens
|
40.0
nM
|
|
|
Inhibitory effect on Bufuralol 1'-hydroxylation by human liver microsomes (Ki = apparent inhibition constant)
|
Homo sapiens
|
80.0
nM
|
|
|
The compound was tested for effective concentration (intradermal injection) that caused local anesthesia in 50% of mice by tail-clip method
|
Mus musculus
|
0.0098
ug.mL-1
|
|
|
Inhibition of partially purified cytochrome P450 2D6 1'-hydroxybufuralol formation
|
Homo sapiens
|
43.0
nM
|
|
|
Inhibitory constant for cytochrome P450 2D6
|
Homo sapiens
|
60.0
nM
|
|
|
Inhibition of P-gp was determined using rhodamine-assay in human CaCo-2 cells
|
None
|
36.0
%
|
|
|
In vitro antimalarial activity against Plasmodium falciparum W2 in human erythrocytes by [3H]hypoxanthine uptake
|
Plasmodium falciparum
|
160.0
nM
|
|
|
In vitro inhibition of parasite development of Plasmodium falciparum W2 in human erythrocytes
|
Plasmodium falciparum
|
4.0
nM
|
|
|
Percentage inhibition of specific binding of [3H]dofetilide (UK-68,798) from cardiac myocytes with blockade of delayed rectifier K+ channel
|
Cavia porcellus
|
40.0
%
|
|
|
Inhibition of human Potassium channel HERG expressed in mammalian cells
|
Homo sapiens
|
323.59
nM
|
|
|
Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 10 uM
|
Cavia porcellus
|
74.1
%
|
|
|
Percentage inhibition of specific binding of [3H]batrachotoxin [3H]BTX) in sodium channel from cardiac myocytes at 10 uM
|
Rattus norvegicus
|
68.0
%
|
|
|
Binding affinity for cytochrome P450 2D6
|
None
|
30.0
nM
|
|
|
Inhibitory concentration against cytochrome P450 2D6
|
None
|
10.0
nM
|
|
|
Inhibitory concentration against potassium channel HERG
|
None
|
323.59
nM
|
|
|
Inhibition of human CYP2D6
|
Homo sapiens
|
20.0
nM
|
|
|
Inhibition of calcium-induced contraction of potassium ion depolarized guinea pig aortic strips at 100 uM
|
Cavia porcellus
|
30.0
%
|
|
|
Inhibition of CYP2D6 in human liver microsomes
|
Homo sapiens
|
410.0
nM
|
|
|
Inhibition of human CYP2D6
|
Homo sapiens
|
11.0
nM
|
|
|
Inhibition of human recombinant CYP2D6 expressed in insect microsomes
|
Homo sapiens
|
14.0
nM
|
|
|
Inhibition of human recombinant CYP2D6 expressed in baculovirus-infected insect microsomes
|
Homo sapiens
|
14.0
nM
|
|
|
Inhibition of human CYP2D6 expressed in baculovirus-infected insect cell system
|
Homo sapiens
|
19.6
nM
|
|
|
Inhibition of human CYP2D6 by Lineweaver-Burke plot
|
Homo sapiens
|
9.8
nM
|
|
|
Inhibition of human liver microsome CYP2D6 in assessed as [14C]formaldehyde formation
|
Homo sapiens
|
82.0
nM
|
|
|
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy
|
Homo sapiens
|
62.9
%
|
|
|
Cardiotoxicity in iv dosed Dunkin-Hartley guinea pig assessed as drug level required to evoke 50 ms QTc prolongation administered as 3 fold cumulative doses measured every 10 seconds at end of every 20 mins follow up period of individual dose by ECG
|
Cavia porcellus
|
8.34
umol/Kg
|
|
|
Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 after 48 hrs by [G-3H]hypoxanthine uptake
|
Plasmodium falciparum K1
|
51.0
nM
|
|
|
Inhibition of human CYP2D6 by radiometric assay
|
Homo sapiens
|
78.0
nM
|
|
|
Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique
|
Homo sapiens
|
323.59
nM
|
|
|
Inhibition of human recombinant CYP2D6 at 5 uM assessed as blockade of O-demethylation of dextromethorphan in to dextrophan by nanoscale automated in-capillary assay
|
Homo sapiens
|
90.0
%
|
|
|
GSK_TCMDC: Inhibition of Plasmodium falciparum 3D7 in whole red blood cells, using parasite LDH activity as an index of growth. Test compounds present at 2uM
|
Plasmodium falciparum
|
98.0
%
|
|
|
GSK_TCMDC: Inhibition of Plasmodium falciparum Dd2 in whole red blood cells, using parasite LDH activity as an index of growth. Test compounds present at 2uM
|
Plasmodium falciparum
|
95.0
%
|
|
|
GSK_TCMDC: Inhibition of Plasmodium falciparum 3D7 LDH activity, using an LDH reporter assay. Test compounds present at 2uM
|
Plasmodium falciparum
|
0.0
%
|
|
|
GSK_TCMDC: Percent inhibition of human HepG2 cell line. Test compounds present at 10uM.
|
Homo sapiens
|
0.0
%
|
|
|
NOVARTIS: Inhibition of Plasmodium falciparum 3D7 (drug-susceptible) proliferation in erythrocyte-based infection assay
|
Plasmodium falciparum
|
9.59
nM
|
|
|
NOVARTIS: Inhibition of Plasmodium falciparum W2 (drug-resistant) proliferation in erythrocyte-based infection assay
|
Plasmodium falciparum
|
35.2
nM
|
|
|
Vasorelaxant activity in potassium depolarized guinea pig aortic strip assessed as inhibition of calcium-induced contraction at 50 uM
|
Cavia porcellus
|
30.0
%
|
|
|
Inhibition of human CYP2D6
|
Homo sapiens
|
10.0
nM
|
|
|
Inhibition of CYP2D6 after 30 mins by fluorometric assay
|
None
|
10.0
nM
|
|
|
Inhibition of human CYP2D6 expressed in baculovirus-infected insect microsomes
|
Homo sapiens
|
14.0
nM
|
|
|
Inhibition of human ERG expressed in HEK293 cells assessed as inhibition of tail current at holding potential of -70 mV at 20 uM after 10 mins by whole-cell patch clamp method
|
Homo sapiens
|
85.5
%
|
|
|
Antimalarial activity against chloroquine sensitive Plasmodium falciparum HB3 after 72 hrs by SYBP Green I dye staining
|
Plasmodium falciparum HB3
|
18.0
nM
|
|
|
Antimalarial activity against chloroquine resistant Plasmodium falciparum Dd2 after 72 hrs by SYBP Green I dye staining
|
Plasmodium falciparum
|
90.0
nM
|
|
|
Inhibition of norA-mediated ethidium bromide efflux in Staphylococcus aureus SA-1199B harboring grlA A116E mutant at 50 uM after 5 mins by fluorometric analysis
|
Staphylococcus aureus
|
31.5
%
|
|
|
Inhibition of human recombinant MDR1 expressed in mouse L5178Y cells assessed as inhibition of rhodamine-123 efflux at 10'-4 M preincubated for 10 mins measured after 20 mins by FACS analysis
|
Homo sapiens
|
21.1
%
|
|
|
TP_TRANSPORTER: transepithelial transport of digoxin (basal to apical) in Caco-2 cells
|
None
|
430.0
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
|
43.3
%
|
|
|
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
|
37.2
%
|
|
|
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
|
-10.0
%
|
|
|
Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 assessed as incorporation of [3H]hypoxanthine after 48 hr microdilution method
|
Plasmodium falciparum K1
|
51.0
nM
|
|
|
Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as incorporation of [3H]hypoxanthine after 48 hr microdilution method
|
Plasmodium falciparum 3D7
|
21.0
nM
|
|
|
Antiamoebic activity against Entamoeba histolytica
|
Entamoeba histolytica
|
16.6
ug.mL-1
|
|
|
Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells at 20 uM after 1.5 mins by fluorescence assay
|
Homo sapiens
|
28.0
%
|
|
|
Antiplasmodial activity against erythrocytic stage of chloroquine-sensitive Plasmodium falciparum 3D7 assessed as parasite LDH activity by three-fold serial dilution method
|
Plasmodium falciparum
|
0.06
ug.mL-1
|
|
|
Antileishmanial activity against Leishmania mexicana mexicana MHOM/BZ/84/BEL46 promastigotes assessed as parasite LDH activity by three-fold serial dilution method
|
Leishmania mexicana mexicana
|
20.0
ug.mL-1
|
|
|
Antitrypanosomal activity against Trypanosoma brucei brucei Lister 427 bloodstream form assessed as parasite LDH activity by three-fold serial dilution method
|
Trypanosoma brucei brucei
|
8.42
ug.mL-1
|
|
|
Cytotoxicity against human WI38 cells by MTT assay
|
Homo sapiens
|
11.28
ug.mL-1
|
|
|
Inhibition of human recombinant microsomal CYP2D6 using {3-[2-(N,N-diethyl-N-methylamino)ethyl]-7-methoxy-4-methylcoumarin} as substrate assessed as remaining activity at 10 uM after 30 mins by spectrofluorimetric analysis relative to control
|
Homo sapiens
|
2.0
nM
|
|
|
Inhibition of CYP3A4 in human liver microsomes assessed as midazolam hydroxylation to 1'-hydroxymidazolam at 10 uM after 10 mins relative to control
|
Homo sapiens
|
36.0
%
|
|
|
Inhibition of CYP2D6 in human liver microsomes assessed as bufuralol hydroxylation to 4'-hydroxybufuralol at 10 uM after 10 mins relative to control
|
Homo sapiens
|
90.0
%
|
|
|
Inhibition of CYP1A2 in human liver microsomes assessed as phenacetin demethylation to acetaminophen at 10 uM after 10 mins relative to control
|
Homo sapiens
|
23.0
%
|
|
|
Inhibition of CYP2C9 in human liver microsomes assessed as tolbutamide hydroxylation to hydroxytolbutamide at 10 uM after 10 mins relative to control
|
Homo sapiens
|
9.0
%
|
|
|
Inhibition of CYP2D6 (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
95.07
%
|
|
|
Inhibition of recombinant CYP2D6 (unknown origin) using 7-methoxy-4-trifluoromethylcoumarin as substrate
|
Homo sapiens
|
17.0
nM
|
|
|
Inhibition of human CYP2D6 at 10 uM
|
Homo sapiens
|
88.0
%
|
|
|
Inhibition of CYP2D6 (unknown origin) using AMMC by fluorescence assay
|
Homo sapiens
|
120.0
nM
|
|
|
Inhibition of recombinant human CYP2D6 preincubated at 10 uM for 5 mins before fluorescent substrate addition by fluorescence assay
|
Homo sapiens
|
21.2
%
|
|
|
Inhibition of CYP2D6 in human liver microsome
|
Homo sapiens
|
6.0
nM
|
|
|
Inhibition of human ERG expressed in CHL cells assessed as tail current at 10 uM after 7 mins by patch clamp assay relative to control
|
Homo sapiens
|
100.0
%
|
|
|
Inhibition of hERG K channel
|
None
|
300.0
nM
|
|
|
Inhibition of OCTN1 (unknown origin) expressed in HEK293 cells assessed as reduction of [3H]ergothioneine substrate uptake at 1500 uM by liquid scintillation counting
|
Homo sapiens
|
83.9
%
|
|
|
Inhibition of OCTN2 (unknown origin) expressed in HEK293 cells assessed as reduction of [3H]carnitine substrate uptake at 1500 uM by liquid scintillation counting
|
Homo sapiens
|
89.9
%
|
|
|
Antiplasmodial activity against Plasmodium falciparum 3D7 assessed as reduction in parasite viability by parasite lactate dehydrogenase assay
|
Plasmodium falciparum 3D7
|
194.4
nM
|
|
|
Inhibition of CYP2D6 (unknown origin) at 1 uM by luminescent readout-based method
|
Homo sapiens
|
96.25
%
|
|
|
Inhibition of CYP2D6 (unknown origin)
|
Homo sapiens
|
18.0
nM
|
|
|
Inhibition of CYP2D6 (unknown origin) using luciferin tagged substrate preincubated for 10 mins before substrate addition
|
Homo sapiens
|
30.0
nM
|
|
|
Inhibition of CYP2D6 (unknown origin) at 1 uM by P450-glo assay
|
Homo sapiens
|
96.25
%
|
|
|
Inhibition of human recombinant CYP2D6 using MFC as substrate incubated for 40 mins by fluorimetry
|
Homo sapiens
|
17.0
nM
|
|
|
Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate after 10 mins by LC-MS analysis
|
Homo sapiens
|
9.0
nM
|
|
|
Inhibition of CYP2D6 in human liver microsomes using bufuralol as substrate at 10 uM preincubated for 5 mins followed by NADPH addition measured after 10 mins by LC-MS/MS analysis relative to control
|
Homo sapiens
|
93.0
%
|
|
|
Inhibition of recombinant human CYP2D6 by P450-Glo luminescence assay
|
Homo sapiens
|
60.0
nM
|
|
|
Inhibition of CYP2D6 in pooled human hepatic microsomes using dextromethorphan substrate in presence of NADPH
|
Homo sapiens
|
41.3
nM
|
|
|
Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate preincubated for 10 mins followed by NADPH addition measured after 10 mins by LC/MS/MS method
|
Homo sapiens
|
151.0
nM
|
|
|
Inhibition of CYP2D6 in human liver microsomes using bufuralol as substrate after 5 to 15 mins
|
Homo sapiens
|
35.0
nM
|
|
|
Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate preincubated for 10 mins followed by NADPH addition measured after 10 mins by LC/MS/MS analysis
|
Homo sapiens
|
135.0
nM
|
|
|
Inhibition of CYP2D6 in human liver microsomes assessed as dextromethorphan O-demethylation after 4 to 40 mins in presence of NADPH by LCMS analysis
|
Homo sapiens
|
25.0
nM
|
|
|
Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate preincubated for 10 mins followed by NADPH addition measured after 10 mins by LC-MS/MS analysis
|
Homo sapiens
|
118.0
nM
|
|
|
Inhibition of CYP2D6 in human liver microsomes at 2 uM using dextromethorphan as substrate by LC-MS/MS analysis relative to control
|
Homo sapiens
|
93.28
%
|
|
|
Inhibition of recombinant human CYP2D6 expressed in insect cell microsomes at 1 uM using Luciferin-ME EGE as substrate preincubated for 30 mins followed by NADPH addition measured after 45 mins by luminometric method
|
Homo sapiens
|
91.0
%
|
|
|
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
|
10.07
%
|
|
|
Antibacterial activity against Escherichia coli ATCC 25922 (CO-ADD:GN_001); MIC in CAMBH media using NBS plates, by OD(600)
|
Escherichia coli
|
-1.55
%
|
|
|
Antibacterial activity against Klebsiella pneumoniae MDR ATCC 70063 (CO-ADD:GN_003); MIC in CAMBH media using NBS plates, by OD(600)
|
Klebsiella pneumoniae
|
12.62
%
|
|
|
Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 (CO-ADD:GN_042); MIC in CAMBH media using NBS plates, by OD(600)
|
Pseudomonas aeruginosa
|
8.31
%
|
|
|
Antibacterial activity against Acinetobacter baumannii ATCC 19606 (CO-ADD:GN_034); MIC in CAMBH media using NBS plates, by OD600
|
Acinetobacter baumannii
|
15.14
%
|
|
|
Antifungal activity against Candida albicans ATCC 90028 (CO-ADD:FG_001); MIC in YNB media using NBS plates, by OD630
|
Candida albicans
|
-0.46
%
|
|
|
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
|
2.25
%
|
|
|
Inhibition of human TASK3 expressed in Xenopus oocytes at 100 uM by whole cell patch clamp assay relative to control
|
Homo sapiens
|
42.2
%
|
|
|
Inhibition of rat TASK3 expressed in African green monkey COS7 cells at 100 uM by outside-out patches based electrophysiology assay relative to control
|
Rattus norvegicus
|
37.0
%
|
|
|
Inhibition of CYP2D6 in pooled human liver microsomes pre-incubated for 5 mins before NADPH addition and measured after 10 mins by UPLC-MS/MS analysis relative to control
|
Homo sapiens
|
78.0
nM
|
|
|
Inhibition of CYP2D6 in human liver microsomes using dextromethorphan substrate incubated for 10 mins in presence of NADPH
|
Homo sapiens
|
156.0
nM
|
|
|
Inhibition of CYP2D6 (unknown origin) using beetle D-luciferin as substrate by CYP450-Glo assay
|
Homo sapiens
|
10.0
nM
|
|
|
Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate after 10 mins in presence of NADPH
|
Homo sapiens
|
156.0
nM
|
|
|
Inhibition of human CYP2D6 in human liver microsomes at 50 times IC50 concentration relative to control
|
Homo sapiens
|
97.9
%
|
|
|
Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate after 20 mins in presence of NADP by LC-MS/MS analysis
|
Homo sapiens
|
263.0
nM
|
|
|
Inhibition of human ERG expressed in HEK cell at 1 uM at -70 mV holding potential by patch clamp method relative to control
|
Homo sapiens
|
50.2
%
|
|
|
Inhibition of CYP2D6 in human liver microsomes using dextromethorphan substrate in presence of NADPH incubated for 10 mins
|
Homo sapiens
|
134.0
nM
|
|
|
Inhibition of human CYP2D6 in presence of NADPH by luciferase reporter gene assay
|
Homo sapiens
|
10.0
nM
|
|
|
Inhibition of human CYP2D6 by fluorescence method
|
Homo sapiens
|
10.0
nM
|
|
|
Inhibition of human recombinant CYP2D6 using luciferin as substrate preincubated for 10 mins followed by substrate addition and measured after 50 mins in presence of NADPH by CYP450-Glo assay
|
Homo sapiens
|
6.9
nM
|
|
|
Inhibition of CYP2D6 (unknown origin) expressed in insect cell microsomes using dibenzylfluorescein substrate by fluorescence based assay
|
Homo sapiens
|
7.3
nM
|
|
|
Inhibition of CYP2D6 in human liver microsome using probe substrate measured after 20 mins in presence of NADPH by LC-MS/MS analysis
|
Homo sapiens
|
134.0
nM
|
|
|
Inhibition of CYP2D6 in human liver microsomes at 10 uM using dextromethorphan as substrate preincubated for 5 mins followed by NADPH addition and measured after 20 mins by LC-MS/MS analysis relative to control
|
Homo sapiens
|
89.0
%
|
|
|
Inhibition of human recombinant CYP2D6
|
Homo sapiens
|
8.1
nM
|
|
|
Inhibition of CYP2D6 in human liver microsomes after 20 mins by LC-MS/MS analysis
|
Homo sapiens
|
44.0
nM
|
|
|
Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate incubated for 5 mins followed by NADPH addition and measured after 20 mins by LC-MS/MS analysis
|
Homo sapiens
|
35.6
nM
|
|
|
Inhibition of CYP2D6 in human liver microsomes using Dextromethorphan as substrate measured after 20 mins by LC-MS/MS analysis
|
Homo sapiens
|
40.8
nM
|
|
|
Inhibition of CYP2D6 in human liver Microsome using dextromethorphan as substrate preincubated for 10 mins followed by NADPH addition and further incubated for 10 mins as substrate by LC-MS/MS analysis relative to control
|
Homo sapiens
|
96.2
%
|
|
|
Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate in presence of NADPH incubated for 10 mins by LC-MS/MS analysis
|
Homo sapiens
|
120.0
nM
|
|
|
Inhibition of CYP2D6 in human liver microsomes using bufuralol as substrate incubated for 10 mins in presence of NADPH by LC-MS/MS analysis
|
Homo sapiens
|
60.0
nM
|
|
|
Inhibition of CYP2D6 in human liver microsome using dextromethorphan as substrate
|
Homo sapiens
|
64.0
nM
|
|
|
Inhibition of CYP2D6 (unknown origin) at 1 uM using dextromethorphan as substrate relative to control
|
Homo sapiens
|
91.3
%
|
|
|
Inhibition of CYP2D6 (unknown origin) using quinidine as substrate
|
Homo sapiens
|
18.0
nM
|
|
