|
Inhibition of [3H]D-cis-diltiazem binding to calcium channel of isolated guinea pig skeletal muscle microsomal preparation
|
Cavia porcellus
|
380.0
nM
|
|
|
Displacement of [3H]diltiazem from L-type calcium channel of guinea pig striated muscle
|
Cavia porcellus
|
380.0
nM
|
|
|
Ability to inhibit [3H]nitrendipine binding to the L-type calcium channel receptor(CCR) in rat heart homogenate.
|
Rattus norvegicus
|
54.0
nM
|
|
|
Ability to inhibit [3H]nitrendipine binding to the calcium channel receptor(CCR) in rat cerebral cortex homogenate.
|
None
|
46.0
nM
|
|
|
Displacement of [3H]nitrendipine from calcium channel receptor
|
Rattus norvegicus
|
42.0
nM
|
|
|
Inhibition of [3H]nitrendipine binding to L-type calcium channel receptor(CCR) in rat cerebral cortex homogenate
|
Rattus norvegicus
|
21.0
nM
|
|
|
Displacement of [3H]nitrendipine from calcium channel receptor
|
Rattus norvegicus
|
16.0
nM
|
|
|
In Vitro evaluation for the affinity for the diltiazem receptor in isolated guinea pig skeletal muscle microsomal preparations by inhibiting [3H]diltiazem binding
|
Cavia porcellus
|
200.0
nM
|
|
|
Percent inhibition of calcium-dependent potassium-polarized smooth muscle contraction in canine trachea
|
Canis lupus familiaris
|
96.0
%
|
|
|
Effective drug concentration for negative inotropic activity was determined; Range is from 0.70-0.85 (10e-6 M)
|
Cavia porcellus
|
790.0
nM
|
|
|
Displacement of [3H]nitrendipine binding to L-type calcium channel of Guinea pig cerebral cortex membranes
|
Cavia porcellus
|
59.0
nM
|
|
|
Percent inhibition of calcium-induced contraction on K+-depolarized guinea-pig aortic strip at 5 x 10 e-5M
|
Cavia porcellus
|
88.0
%
|
|
|
Calcium antagonist activity on K+ depolarized guinea pig aortic strips at 10E-4 mol/L concentration was determined
|
Cavia porcellus
|
88.0
%
|
|
|
In vitro molar concentration required to block [Ca2+] -induced contraction of K+-depolarized taenia cecum of guinea pigs
|
Cavia porcellus
|
170.0
nM
|
|
|
Molar concentration needed to increase e binding by 50% of maximal stimulation
|
Cavia porcellus
|
59.0
nM
|
|
|
Inhibitory concentration required to suppress the contractile force of guinea pig right atria
|
Cavia porcellus
|
95.0
nM
|
|
|
Inhibitory concentration required to suppress the rate of contraction of guinea pig right atria
|
Cavia porcellus
|
600.0
nM
|
|
|
Tested for the calcium antagonistic activity on K+-depolarized guinea pig aortic strips at 10e-4 M.
|
Cavia porcellus
|
88.0
%
|
|
|
[Ca2+] antagonistic activity on K+ depolarized guinea pig aortic strips at 10e-4 M
|
Cavia porcellus
|
88.0
%
|
|
|
In Vitro evaluation on percentage inhibition in Heme Oxygenase at concentration 100(uM) of Cell-free parasite Plasmodium yoelii
|
Plasmodium yoelii
|
29.0
%
|
|
|
In Vitro inhibition of Heme Oxygenase in Cell-free parasite Plasmodium yoelii at concentration 50 uM
|
Plasmodium yoelii
|
12.5
%
|
|
|
In Vitro evaluation on percentage inhibition in Heme Oxygenase at concentration 100 (uM) of infected host
|
None
|
84.0
%
|
|
|
In Vitro evaluation on percentage inhibition in Heme Oxygenase at concentration 50(uM) of infected host
|
None
|
41.0
%
|
|
|
Calcium channel-blocking effect was assessed in potassium ion depolarized guinea pig ileum strips by recording the contractile responses produced by varying concentrations of calcium chloride
|
Cavia porcellus
|
41.69
nM
|
|
|
Inhibition of [3H]nitrendipine binding at L-type [Ca2+] channel in rat cortex homogenate by 50%.
|
None
|
46.0
nM
|
|
|
Calcium antagonistic activity by measuring [3H]nitrendipine displacement at L-type [Ca2+] channel in rat cortex homogenate
|
None
|
21.0
nM
|
|
|
Calcium antagonistic activity by measuring [3H]nitrendipine displacement from rat heart L-type [Ca2+] channel
|
Rattus norvegicus
|
280.0
nM
|
|
|
Inhibition of [3H]nitrendipine binding to L-type [Ca2+] channel in rat cortex homogenate, activity expressed as pIC50
|
None
|
45.71
nM
|
|
|
In vitro vasorelaxant activity in circumferential strips of potassium-depolarized rabbit aorta.
|
Oryctolagus cuniculus
|
210.0
nM
|
|
|
Calcium channel-blocking activity by determined by ability to antagonize calcium-induced contractions of isolated rabbit aortic strips
|
Oryctolagus cuniculus
|
19.95
nM
|
|
|
Vasorelaxant effects in circumferential strips of potassium-depolarized rabbit aorta. (IC50 in rabbit aorta strips contracted with KCl(95% confidence interval))
|
Oryctolagus cuniculus
|
210.0
nM
|
|
|
In vitro evaluation for the vasorelaxant effects in circumferential strips of potassium-depolarized rabbit aorta. (IC50 in rabbit aorta strips contracted with KCl)
|
Oryctolagus cuniculus
|
210.0
nM
|
|
|
Molar concentration required to block [Ca2+] induced contraction of K+ depolarized rat aorta by 50%
|
Rattus norvegicus
|
303.0
nM
|
|
|
Tested in vitro on K+ -depolarized rat aorta strips to evaluate its ability to relax the initial contraction induced by K
|
Rattus norvegicus
|
48.0
nM
|
|
|
In vitro inhibition of K+ induced contractions of the isolated rat aorta.
|
Rattus norvegicus
|
100.0
nM
|
|
|
Compound was tested in vitro for [Ca2+] antagonistic activity in K+-depolarized isolated rat aorta
|
Rattus norvegicus
|
100.0
nM
|
|
|
Inhibitory effect of compound on calcium influx by high potassium in isolated rat aorta
|
Rattus norvegicus
|
352.0
nM
|
|
|
Inhibition of [Ca2+] induced contraction of K+ depolarized rat aorta by 50%
|
Rattus norvegicus
|
303.0
nM
|
|
|
inhibitory effect of compound on contraction induced by high potassium in isolated rat aorta
|
Rattus norvegicus
|
203.0
nM
|
|
|
Inhibition of calcium activation was assessed against calcium-induced constriction of potassium-depolarized rat aorta (Negative logarithm of the molar concentration)
|
Rattus norvegicus
|
38.02
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
|
36.2
%
|
|
|
Displacement of [3H]nitrendipine from calcium channel receptors (CCRs)
|
Rattus norvegicus
|
42.0
nM
|
|
|
Inhibitory constant against calcium channel receptors (CCRs)
|
Rattus norvegicus
|
16.0
nM
|
|
|
Concentration (10 e-6 M) required to block [Ca2+]-induced contraction of K+-depolarized hamster aorta
|
Cricetulus griseus
|
980.0
nM
|
|
|
Calcium antagonistic activity assessed against calcium-induced constriction of potassium-depolarized rat aorta.
|
Rattus norvegicus
|
38.02
nM
|
|
|
Negative inotropic potency as decrease in the developed tension in isolated guinea pig left artium
|
Cavia porcellus
|
790.0
nM
|
|
|
Negative inotropic potency as coronary perfusion pressure in isolated guinea pig atrium
|
Cavia porcellus
|
21.88
nM
|
|
|
Negative inotropic potency as maximal rate of the rise in left ventricular pressure in isolated guinea pig atrium
|
Cavia porcellus
|
9.333
nM
|
|
|
Negative inotropic activity in guinea pig left atrium
|
Cavia porcellus
|
790.0
nM
|
|
|
Antagonist activity against calcium channel assessed as inhibition of calcium-induced contraction of potassium ion-depolarized guinea pig ileum longitudinal smooth muscle
|
Cavia porcellus
|
110.0
nM
|
|
|
Antagonist activity against calcium channel assessed as inhibition of carbachol-induced tonic contraction of guinea pig ileum longitudinal smooth muscle
|
Cavia porcellus
|
480.0
nM
|
|
|
Negative inotropic activity in guinea pig left atrium assessed as decrease in atrial tension relative to control
|
Cavia porcellus
|
790.0
nM
|
|
|
Vasorelaxant activity in K+-depolarized guinea pig aorta assessed as inhibition of calcium-induced contraction at 100 uM
|
Cavia porcellus
|
88.0
%
|
|
|
Vasorelaxant activity in K+-depolarized guinea pig ileum longitudinal smooth muscle assessed as inhibition of calcium-induced contraction at 1 uM
|
Cavia porcellus
|
98.0
%
|
|
|
Vasorelaxant activity in K+-depolarized guinea pig ileum longitudinal smooth muscle assessed as inhibition of calcium-induced contraction
|
Cavia porcellus
|
110.0
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
|
65.5
%
|
|
|
Inhibition of calcium channel
|
None
|
337.0
nM
|
|
|
Antiproliferative activity against human A2780 cells at 1.3 uM after 3 days by MTT assay
|
Homo sapiens
|
0.0
%
|
|
|
Blockade of L-type calcium channel
|
None
|
790.0
nM
|
|
|
Antiproliferative activity against human A2780/DX3 cells at 2.2 uM after 3 days by MTT assay
|
Homo sapiens
|
0.0
%
|
|
|
Effect on cardiac activity in guinea pig spontaneously beating heart assessed as change in left ventricular pressure
|
Cavia porcellus
|
9.333
nM
|
|
|
Effect on cardiac activity in guinea pig spontaneously beating heart assessed as change in coronary perfusion pressure
|
Cavia porcellus
|
21.88
nM
|
|
|
Negative inotropic activity in guinea pig left atrium assessed as decrease in atrial tension
|
Cavia porcellus
|
790.0
nM
|
|
|
Displacement of [3H]diltiazem from L-type calcium channel in Sprague-Dawley rat cardiac myocytes by liquid scintillation counting
|
Rattus norvegicus
|
85.0
nM
|
|
|
Negative inotropic activity in guinea pig left atrium assessed as decrease in atrial tension
|
Cavia porcellus
|
790.0
nM
|
|
|
Vasorelaxant activity in 80 mM K+-depolarized guinea pig thoracic aortic strip assessed as inhibition of calcium-induced contraction at 100 uM
|
Cavia porcellus
|
88.0
%
|
|
|
Muscle relaxant activity in 80 mM K+-depolarized guinea pig ileum longitudinal smooth muscle assessed as inhibition of calcium-induced contraction at 10 uM
|
Cavia porcellus
|
98.0
%
|
|
|
Muscle relaxant activity in 80 mM K+-depolarized guinea pig ileum longitudinal smooth muscle assessed as inhibition of calcium-induced contraction
|
Cavia porcellus
|
110.0
nM
|
|
|
Inhibition of rat L-type Ca2+ channel diltiazem site
|
Rattus norvegicus
|
52.0
nM
|
|
|
Mechanism based inhibition of human cytochrome P450 3A4 measured by testosterone 6-beta hydroxylation
|
Homo sapiens
|
500.0
nM
|
|
|
DRUGMATRIX: Calcium Channel Type L, Benzothiazepine radioligand binding (ligand: [3H] Diltiazem)
|
Rattus norvegicus
|
28.0
nM
|
|
DRUGMATRIX: Calcium Channel Type L, Benzothiazepine radioligand binding (ligand: [3H] Diltiazem)
|
Rattus norvegicus
|
25.0
nM
|
|
|
DRUGMATRIX: Calcium Channel Type L, Phenylalkylamine radioligand binding (ligand: [3H] (-)-Desmethoxyverapamil (D-888))
|
Rattus norvegicus
|
630.0
nM
|
|
DRUGMATRIX: Calcium Channel Type L, Phenylalkylamine radioligand binding (ligand: [3H] (-)-Desmethoxyverapamil (D-888))
|
Rattus norvegicus
|
612.0
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
|
3.2
%
|
|
|
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
|
4.1
%
|
|
|
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
|
-9.1
%
|
|
|
Inhibition of CYP3A4-mediated N-demethylation in human liver microsomes
|
Homo sapiens
|
100.0
nM
|
|
|
Displacement of [3H]Diltiazem from L-type calcium channel benzothiazepine binding site in Wistar rat brain after 3 hrs
|
Rattus norvegicus
|
32.0
nM
|
|
Displacement of [3H]Diltiazem from L-type calcium channel benzothiazepine binding site in Wistar rat brain after 3 hrs
|
Rattus norvegicus
|
36.0
nM
|
|
|
Displacement of [3H]Diltiazem from L-type calcium channel benzothiazepine binding site in Wistar rat brain at 10 uM after 3 hrs relative to control
|
Rattus norvegicus
|
16.0
%
|
|
|
Negative ionotropic activity in guinea pig left atrium assessed as decrease in developed tension driven at 1 Hz
|
Cavia porcellus
|
790.0
nM
|
|
|
Antagonist activity at Cav1.2b in K+-depolarized guinea pig ileum longitudinal smooth muscle assessed as inhibition of calcium-induced contraction
|
Cavia porcellus
|
110.0
nM
|
|
|
Inhibition of voltage-gated L-type Ca channel (species unknown)
|
None
|
450.0
nM
|
|
|
Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
|
Cavia porcellus
|
630.0
nM
|
|
|
Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
|
Cricetulus griseus
|
760.0
nM
|
|
|
Time dependent inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 90 mins followed by 10-fold dilution and substrate addition by LC-MS/MS analysis in presence of NADPH
|
Homo sapiens
|
100.0
nM
|
|
|
Time dependent inhibition of CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 90 mins followed by 10-fold dilution and substrate addition by LC-MS/MS analysis in presence of NADPH
|
Homo sapiens
|
100.0
nM
|
|
|
Negative inotropic activity in potassium depolarized guinea pig left atrium assessed as reduction in developed tension
|
Cavia porcellus
|
790.0
nM
|
|
|
Negative inotropic activity in potassium depolarized guinea pig left atrium assessed as reduction in developed tension after 30 mins
|
Cavia porcellus
|
790.0
nM
|
|
|
Negative chronotropic activity in potassium depolarized guinea pig right atrium assessed as reduction in atrial rate after 30 mins
|
Cavia porcellus
|
70.0
nM
|
|
|
Relaxant activity in potassium depolarized guinea pig ileum longitudinal smooth muscle assessed as inhibition of calcium-induced contraction after 30 mins
|
Cavia porcellus
|
110.0
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
|
1.94
%
|
|
|
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
|
0.05
%
|
|
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
|
0.05
%
|
|
