|
Compound was tested for inhibition of daunomycin efflux in the resistant human T-lymphoblast cell line CEM vcr1000.
|
None
|
320.0
nM
|
|
|
Inhibitory concentration against IKr potassium channel
|
None
|
800.0
nM
|
|
|
Inhibition of P-glycoprotein expressed in MDR CCRF vcr1000 cells by daunorubicin efflux assay
|
Homo sapiens
|
329.0
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
|
83.8
%
|
|
|
NOVARTIS: Inhibition of Plasmodium falciparum 3D7 (drug-susceptible) proliferation in erythrocyte-based infection assay
|
Plasmodium falciparum
|
252.1
nM
|
|
|
NOVARTIS: Inhibition of Plasmodium falciparum W2 (drug-resistant) proliferation in erythrocyte-based infection assay
|
Plasmodium falciparum
|
116.5
nM
|
|
|
Inhibition of CETP in rabbit serum at 10 uM after 1 hr by fluorescent cholesteryl esters transfer assay
|
Oryctolagus cuniculus
|
0.0
%
|
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
|
None
|
935.0
nM
|
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
|
None
|
654.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
|
None
|
187.0
nM
|
|
|
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
|
None
|
354.0
nM
|
|
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
|
None
|
205.0
nM
|
|
|
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
|
None
|
52.0
nM
|
|
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
|
None
|
36.0
nM
|
|
|
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
|
None
|
424.0
nM
|
|
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
|
None
|
318.0
nM
|
|
|
DRUGMATRIX: Calcium Channel Type L, Benzothiazepine radioligand binding (ligand: [3H] Diltiazem)
|
Rattus norvegicus
|
775.0
nM
|
|
DRUGMATRIX: Calcium Channel Type L, Benzothiazepine radioligand binding (ligand: [3H] Diltiazem)
|
Rattus norvegicus
|
689.0
nM
|
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
None
|
92.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
None
|
58.0
nM
|
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
|
None
|
384.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
|
None
|
201.0
nM
|
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
None
|
865.0
nM
|
|
|
Antimalarial activity against erythrocytic stage of chloroquine-resistant Plasmodium falciparum K1 after 72 hrs by FACS method
|
Plasmodium falciparum K1
|
200.0
nM
|
|
|
Antimalarial activity against erythrocytic stage of chloroquine-resistant Plasmodium falciparum K1 after 72 hrs by spectrophotometry
|
Plasmodium falciparum K1
|
920.0
nM
|
|
|
Inhibition of Cav1.2 at 10 uM after 5 mins by patch clamp assay
|
None
|
72.5
%
|
|
|
Inhibition of Cav3.2 at 10 uM after 5 mins by patch clamp assay
|
None
|
60.2
%
|
|
|
Inhibition of HCN2 at 10 uM after 5 mins by patch clamp assay
|
None
|
47.8
%
|
|
|
Inhibition of HCN4 at 10 uM after 5 mins by patch clamp assay
|
None
|
54.6
%
|
|
|
Inhibition of human ERG at 10 uM after 5 mins by patch clamp assay
|
Homo sapiens
|
96.9
%
|
|
|
Inhibition of Kir2.1 at 10 uM after 5 mins by patch clamp assay
|
None
|
0.2
%
|
|
|
Inhibition of Kir3.1/3.4 at 10 uM after 5 mins by patch clamp assay
|
None
|
46.4
%
|
|
|
Inhibition of Kir6.2/SUR2A at 10 uM after 5 mins by patch clamp assay
|
None
|
89.6
%
|
|
|
Inhibition of Kv1.5 at 10 uM after 5 mins by patch clamp assay
|
None
|
65.4
%
|
|
|
Inhibition of Kv4.3 at 10 uM after 5 mins by patch clamp assay
|
None
|
44.1
%
|
|
|
Inhibition of KvLQT/minK at 10 uM after 5 mins by patch clamp assay
|
None
|
33.0
%
|
|
|
Inhibition of Nav1.5 assessed as tonic inhibition at 10 uM after 5 mins by patch clamp assay
|
None
|
93.4
%
|
|
|
Inhibition of Nav1.5 assessed as phasic inhibition at 10 uM after 5 mins by patch clamp assay
|
None
|
97.1
%
|
|
|
Inhibition of P-glycoprotein-mediated daunorubicin efflux from human CCRF-CEM/VCR1000 cells after 240 secs by FACS flow cytometric analysis
|
Homo sapiens
|
331.13
nM
|
|
|
Inhibition of CYP2D6 in human liver microsomes at 1 uM after 20 mins by LC-MS/MS analysis relative to control
|
Homo sapiens
|
25.0
%
|
|
|
Inhibition of CYP2D6 in human liver microsomes at 10 uM after 20 mins by LC-MS/MS analysis relative to control
|
Homo sapiens
|
12.0
%
|
|
|
SUPPLEMENTARY: Inhibition of P-glycoprotein expressed in MDR CCRF vcr1000 cells by daunorubicin efflux assay. Same assay as CHEMBL914418
|
Homo sapiens
|
331.13
nM
|
|
|
Inhibition of hERG K channel
|
None
|
440.0
nM
|
|
|
Inhibition of GIRK-1/4 channel (unknown origin) expressed in HEK293 cells at 1 uM by automated patch clamp method relative to control
|
Homo sapiens
|
60.6
%
|
|
|
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
|
9.33
%
|
|
|
Antibacterial activity against Escherichia coli ATCC 25922 (CO-ADD:GN_001); MIC in CAMBH media using NBS plates, by OD(600)
|
Escherichia coli
|
8.72
%
|
|
|
Antibacterial activity against Klebsiella pneumoniae MDR ATCC 70063 (CO-ADD:GN_003); MIC in CAMBH media using NBS plates, by OD(600)
|
Klebsiella pneumoniae
|
6.97
%
|
|
|
Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 (CO-ADD:GN_042); MIC in CAMBH media using NBS plates, by OD(600)
|
Pseudomonas aeruginosa
|
13.87
%
|
|
|
Antibacterial activity against Acinetobacter baumannii ATCC 19606 (CO-ADD:GN_034); MIC in CAMBH media using NBS plates, by OD600
|
Acinetobacter baumannii
|
18.62
%
|
|
|
Antifungal activity against Candida albicans ATCC 90028 (CO-ADD:FG_001); MIC in YNB media using NBS plates, by OD630
|
Candida albicans
|
0.01
%
|
|
|
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
|
-5.76
%
|
|
