|
Displacement of [3H]clonidine from Alpha-2 adrenergic receptor of rat brain membranes
|
Rattus norvegicus
|
150.0
nM
|
|
|
Inhibition of [3H]prazosin binding to human Alpha-1D adrenergic receptor expressed in CHO cells
|
Homo sapiens
|
289.0
nM
|
|
|
Binding affinity against Alpha-1D adrenergic receptor, from human clones.
|
Homo sapiens
|
1.6
nM
|
|
|
Antagonistic activity against Alpha-2 adrenergic receptor in the prostatic portion of the rat vas deferens
|
None
|
19.5
nM
|
|
|
Antagonistic activity against alpha-2 adrenergic receptor in rat vas deferens
|
None
|
26.3
nM
|
|
|
Antagonistic activity against presynaptic alpha-2 adrenergic receptor in isolated rat vas deferens using xylazine as agonist
|
None
|
19.05
nM
|
|
|
Antagonistic activity against clonidine-stimulated rat vas deferens presynaptic alpha-2 adrenergic receptor
|
Rattus norvegicus
|
22.39
nM
|
|
|
Antagonistic potency of compound for Alpha-2 adrenergic receptor
|
None
|
19.95
nM
|
|
|
In vitro binding affinity was measured as the inhibition of [3H]WB-4101 binding to alpha-1 adrenergic receptor of rat cortical membranes
|
None
|
360.0
nM
|
|
|
Presynaptic antagonistic activity against alpha-2 adrenergic receptor from rat, isolated, field-stimulated vas deferens, using clonidine as the agonist
|
None
|
22.39
nM
|
|
|
Alpha-2 adrenergic receptor antagonistic activity in rat vas deferens vs clonidine
|
None
|
12.3
nM
|
|
|
The compound was evaluated for the alpha-2 adrenergic receptor antagonistic activity in rat vas deferens vs methoxamine alpha1 adrenoceptor antagonism
|
None
|
123.03
nM
|
|
|
Binding affinity against Alpha-2 adrenergic receptor in rat cerebral cortical membrane, determined using [3H]- yohimbine as the radioligand
|
None
|
12.59
nM
|
|
|
Binding affinity against Alpha-1D adrenergic receptor, from rat clones.
|
Rattus norvegicus
|
52.0
nM
|
|
|
Binding affinity to alpha-2 adrenergic receptor determined by measurement of [3H]yohimbine displacement from rat cortical membrane
|
None
|
12.59
nM
|
|
|
Binding affinity to the alpha-2 adrenergic receptor of rat cerebral cortex assayed using [3H]idazoxan as radioligand
|
None
|
56.23
nM
|
|
|
Binding affinity to alpha-2 adrenergic receptor of rat cerebral cortex assayed using [3H]yohimbine as radioligand
|
None
|
12.59
nM
|
|
|
Compound was evaluated for the displacement of [3H]yohimbine in acetonitrile/acetic acid anti-corynanthine MIPs for Alpha-2 adrenergic receptor
|
None
|
170.0
nM
|
|
|
Dissociation constant in high affinity sites where the binding is in 50 mM phosphate buffer for Alpha-2 adrenergic receptor
|
None
|
120.0
nM
|
|
|
Dissociation constant in high affinity sites where the binding is in acetonitrile/acetic acid for Alpha-2 adrenergic receptor
|
None
|
60.0
nM
|
|
|
Alpha-1 adrenergic receptor pA2 value against norepinephrine in vitro experiment in rat anococcygeus.
|
None
|
323.59
nM
|
|
|
Antagonistic activity against Alpha-1 adrenergic receptor in the epidermal portion of the rat vas deferens
|
None
|
616.6
nM
|
|
|
Antagonistic activity against alpha-1 adrenergic receptor in isolated rat anococcygeus muscle
|
None
|
263.03
nM
|
|
|
Antagonistic activity against postsynaptic Alpha-1 adrenergic receptor in isolated rat vas deferens using (-)-phenylephrine as agonist
|
None
|
89.13
nM
|
|
|
Antagonistic activity upon postsynaptic alpha-1 adrenergic receptor was determined in the rat isolated, field stimulated vas deferens using methoxamine
|
None
|
302.0
nM
|
|
|
Antagonistic potency of compound for Alpha-1 adrenergic receptor
|
None
|
630.96
nM
|
|
|
Presynaptic antagonistic activity against alpha-1 adrenergic receptor from rat, isolated, field-stimulated vas deferens, using methoxamine as the agonist
|
None
|
302.0
nM
|
|
|
Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand
|
None
|
49.0
nM
|
|
|
Displacement of [3H]clonidine from calf cerebral cortex alpha-2 adrenergic receptor
|
Bos taurus
|
49.0
nM
|
|
|
Evaluated for its ability to displace [3H]clonidine from alpha-2 adrenergic receptor of calf cerebral cortex
|
None
|
49.0
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in bovine pineal
|
None
|
3.6
nM
|
|
|
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
|
Homo sapiens
|
0.42
nM
|
|
|
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor
|
None
|
7.5
nM
|
|
|
Inhibition of [3H]- MK-912 binding against human recombinant Alpha-2A adrenergic receptor
|
None
|
3.1
nM
|
|
|
Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand
|
None
|
220.0
nM
|
|
|
Displacement of [3H]prazosin from calf cerebral cortex alpha-1 adrenergic receptor
|
Bos taurus
|
200.0
nM
|
|
|
Evaluated for its ability to displace [3H]prazosin from alpha-1-Adrenoceptor of calf cerebral cortex
|
None
|
220.0
nM
|
|
|
Binding affinity against Alpha-1 adrenergic receptor in rat cerebral cortical membrane, determined using [3H]-prazosin as the radioligand
|
None
|
398.11
nM
|
|
|
Binding affinity to alpha-1 adrenergic receptor determined by measurement of [3H]prazosin displacement from rat cortical membrane
|
None
|
398.11
nM
|
|
|
Binding affinity determined to alpha-1 adrenergic receptor of rat cerebral cortex using [3H]prazosin as radioligand
|
None
|
398.11
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in canine adipocyte
|
Canis lupus familiaris
|
4.0
nM
|
|
|
Alpha-2 adrenergic receptor activity was assessed in vitro from the ability to inhibit norepinephrine binding to guinea pig vas deferens
|
Cavia porcellus
|
25.7
nM
|
|
|
Antagonistic activity against adrenergic alpha-2 receptor in longitudinal muscle strip of the guinea pig ileum using l-norepinephrine as agonist
|
Rattus norvegicus
|
25.7
nM
|
|
|
Antagonistic activity against longitudinal muscle strip of the guinea pig ileum using xylazine as agonist
|
Cavia porcellus
|
43.65
nM
|
|
|
Alpha-1 adrenergic receptor agonist activity in rat anococcygeus assay
|
Rattus norvegicus
|
302.0
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in hamster adipocyte
|
Cricetulus griseus
|
33.0
nM
|
|
|
Inhibition of [3H]p-aminoclonidine (PAC) binding to alpha-2 adrenergic receptor of purified human platelet plasma membranes
|
None
|
8.0
nM
|
|
|
Binding affinity against human alpha 2b-adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
|
Homo sapiens
|
2.01
nM
|
|
|
Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2B adrenergic receptor
|
None
|
4.6
nM
|
|
|
Antagonistic activity against postsynaptic alpha-1 adrenergic receptor in rabbit pulmonary artery using l-norepinephrine as agonist
|
Oryctolagus cuniculus
|
147.91
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in HT-29 cell
|
None
|
1.8
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in alpha2C10
|
None
|
3.8
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in alpha2C2
|
None
|
4.1
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in human adipocyte
|
None
|
3.0
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in human platelet
|
None
|
0.9
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in rat adipocyte
|
None
|
70.0
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in Malpha-10H (mouse)
|
None
|
54.0
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in Malpha2-4H (mouse)
|
None
|
3.8
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in NG-108 cell
|
None
|
0.6
nM
|
|
|
Inhibition of [3H]- Yohimbine binding against rat kidney cortex Alpha-2B adrenergic receptor
|
None
|
2.0
nM
|
|
|
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptor
|
None
|
2.3
nM
|
|
|
Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor
|
Oryctolagus cuniculus
|
398.11
nM
|
|
|
Inhibition of phenylephrine-induced contraction of the rabbit aorta as a measure of functional alpha-1-adrenoceptor antagonism
|
Oryctolagus cuniculus
|
794.33
nM
|
|
|
Alpha-2 adrenergic receptor agonist activity in mouse vas deferens relative to clonidine
|
Mus musculus
|
10.47
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in OK cell
|
opossum
|
0.6
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in opossum kidney
|
opossum
|
0.4
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in porcine alpha2-clone
|
None
|
4.4
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]-yohimbine to Alpha-2 adrenergic receptor in rabbit adipocyte
|
Oryctolagus cuniculus
|
35.0
nM
|
|
|
Alpha-2 adrenergic receptor pA2 value against clonidine in vitro experiment in rat vas deferens
|
None
|
7.244
nM
|
|
|
Alpha-1-adrenolytic activity was assessed in vitro from the ability to inhibit clonidine binding to rat aorta preparation
|
None
|
346.74
nM
|
|
|
Alpha-2 adrenergic receptor activity was assessed from the ability to inhibit [3H]yohimbine binding to rat cerebral cortex preparation
|
None
|
9.1
nM
|
|
|
Binding affinity towards rat Alpha-2 adrenergic receptor was evaluated using [3H]- yohimbine as radioligand
|
None
|
30.0
nM
|
|
|
Binding affinity against Alpha-2 adrenergic receptor in rat brain membrane using [3H]yohimbine as radioligand
|
None
|
30.0
nM
|
|
|
In vitro inhibition of binding of [3H]-RX-821002 to alpha-2 adrenergic receptor site in rat brain membranes.
|
None
|
67.0
nM
|
|
|
Binding affinity against alpha-2 adrenergic receptor was determined by the displacement of [3H]prazosin from rat brain cortical membranes
|
None
|
190.0
nM
|
|
|
Binding affinity against Alpha-1B adrenergic receptor from hamster clones.
|
hamster
|
1.1
nM
|
|
|
Inhibition of [3H]prazosin binding to human Alpha-1B adrenergic receptor expressed in CHO cells
|
Homo sapiens
|
966.0
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in RG20 (rat)
|
None
|
52.0
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in RGlO (rat)
|
None
|
2.4
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in RIN-m5F cell
|
None
|
104.0
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in RNG (rat)
|
None
|
8.7
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]-yohimbine to Alpha-2 adrenergic receptor in alpha-2 C4
|
None
|
0.6
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in neonatal rat lung
|
None
|
1.0
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in rat enterocyte
|
None
|
54.0
nM
|
|
|
Compound was evaluated for inhibition of binding of [3H]yohimbine to Alpha-2 adrenergic receptor in rat kidney
|
None
|
5.0
nM
|
|
|
Binding affinity against Alpha-1B adrenergic receptor from human clone
|
Homo sapiens
|
7.2
nM
|
|
|
Evaluated for its ability to displace [3H]rauwolscine from alpha-2 adrenergic receptor of rat cerebral cortex
|
None
|
10.0
nM
|
|
|
In vitro binding affinity was measured as the inhibition of [3H]clonidine binding to alpha-2 adrenergic receptor of rat cortical membranes
|
None
|
45.0
nM
|
|
|
Inhibition of [3H]idazoxan binding to alpha-2 adrenergic receptor of rat cortical membranes
|
Rattus norvegicus
|
48.0
nM
|
|
|
In Vitro reversal of inhibitory effect of UK - 14304 on the contractile response of guinea pig ileum to field stimulation.
|
Cavia porcellus
|
12.59
nM
|
|
|
Inhibition of 1'-hydroxybufuralol formation by human liver microsomes
|
Homo sapiens
|
230.0
nM
|
|
|
Inhibition of 1'-hydroxybufuralol formation by human liver microsomes
|
Homo sapiens
|
140.0
nM
|
|
|
Inhibition of 1'-hydroxybufuralol formation by human liver microsomes
|
Homo sapiens
|
180.0
nM
|
|
|
Inhibition of 1'-hydroxybufuralol formation by human liver microsomes
|
Homo sapiens
|
190.0
nM
|
|
|
Inhibitory effect on Bufuralol 1'-hydroxylation by human liver microsomes (Ki = apparent inhibition constant)
|
Homo sapiens
|
180.0
nM
|
|
|
Inhibition of partially purified cytochrome P450 2D6 1'-hydroxybufuralol formation
|
Homo sapiens
|
520.0
nM
|
|
|
Inhibition of specific [3H]clonidine binding (0.4 nM) to rat brain membranes alpha2 adrenoceptor
|
None
|
165.0
nM
|
|
|
Inhibition constant on radiolabeled [125 I] FIDA2 binding to rat striatal membranes
|
Rattus norvegicus
|
505.0
nM
|
|
|
In vivo antagonist activity against B-HT 933-induced Alpha-2 adrenergic receptor-mediated vasoconstriction in pithed normotensive rats
|
Rattus norvegicus
|
147.91
nM
|
|
|
Tested for antagonism of clonidine in the field-stimulated rat vas deferens.
|
Rattus norvegicus
|
22.39
nM
|
|
|
Tested for antagonism of methoxamine in the field-stimulated rat vas deferens.
|
Rattus norvegicus
|
302.0
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
|
25.6
%
|
|
|
Inhibition of [3H]nitrendipine binding to membrane homogenates of rat cardiac muscle.
|
Rattus norvegicus
|
45.0
nM
|
|
|
Ability to displace [3H]clonidine from alpha-2 adrenergic receptor in rat brain homogenates in vitro
|
None
|
78.0
nM
|
|
|
In vitro antagonistic activity against alpha-2 adrenergic receptor in isolated electrically stimulated rat vas deferens (clonidine-induced decrease in twitch height)
|
None
|
12.3
nM
|
|
|
Ability to reversal of inhibitory effects of UK-14304 on the contraction of guinea pig ileum as a measure of alpha-2-adrenoceptor antagonism
|
Cavia porcellus
|
31.62
nM
|
|
|
Binding affinity against alpha-2 adrenergic receptor was determined by the displacement of [3H]clonidine from rat brain cortical membranes
|
None
|
84.0
nM
|
|
|
Binding affinity for cytochrome P450 2D6
|
None
|
180.0
nM
|
|
|
In vitro binding affinity towards alpha-2a adrenergic receptor
|
Homo sapiens
|
1.4
nM
|
|
|
In vitro binding affinity towards alpha-2b adrenergic receptor
|
Homo sapiens
|
7.1
nM
|
|
|
In vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamine
|
Homo sapiens
|
0.88
nM
|
|
|
Inhibitory concentration against cytochrome P450 2D6
|
None
|
8.4
nM
|
|
|
Percent inhibition against Alpha-2 adrenergic receptor at 1 uM
|
Homo sapiens
|
95.0
nM
|
|
|
Inhibition of alpha 2 adrenergic receptor
|
None
|
38.0
nM
|
|
|
Displacement of radiolabeled yohimbine from adrenergic alpha2 receptor
|
None
|
100.0
nM
|
|
Displacement of radiolabeled yohimbine from adrenergic alpha2 receptor
|
None
|
43.0
nM
|
|
|
Displacement of [3H]MK912 from human recombinant adrenergic alpha2A receptor expressed in Sf9 cells
|
Homo sapiens
|
8.5
nM
|
|
|
Inhibition of rat alpha2 adrenoceptor
|
Rattus norvegicus
|
58.0
nM
|
|
|
Displacement of [3H]RX821002 from adrenergic alpha2 receptor
|
None
|
33.0
nM
|
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
|
None
|
126.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
|
None
|
72.0
nM
|
|
|
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
|
Rattus norvegicus
|
500.0
nM
|
|
|
DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
|
Rattus norvegicus
|
658.0
nM
|
|
|
DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
|
None
|
498.0
nM
|
|
|
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
|
None
|
6.151
nM
|
|
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
|
None
|
2.307
nM
|
|
|
DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
|
None
|
17.0
nM
|
|
DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
|
None
|
7.947
nM
|
|
|
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
|
None
|
36.0
nM
|
|
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
|
None
|
5.162
nM
|
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
None
|
74.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
None
|
47.0
nM
|
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
None
|
784.0
nM
|
|
|
DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)
|
None
|
687.0
nM
|
|
|
DRUGMATRIX: Imidazoline I2, Central radioligand binding (ligand: [3H] Idazoxan)
|
Rattus norvegicus
|
157.0
nM
|
|
DRUGMATRIX: Imidazoline I2, Central radioligand binding (ligand: [3H] Idazoxan)
|
Rattus norvegicus
|
105.0
nM
|
|
|
Binding affinity to adrenergic alpha2 receptor (unknown origin) by radioligand displacement assay
|
Homo sapiens
|
36.0
nM
|
|
|
Displacement of [3H]MK912 from human recombinant alpha2A adrenergic receptor expressed in Sf9 cells after 60 mins
|
Homo sapiens
|
3.1
nM
|
|
Displacement of [3H]MK912 from human recombinant alpha2A adrenergic receptor expressed in Sf9 cells after 60 mins
|
Homo sapiens
|
8.4
nM
|
|
|
Displacement of [3H]MK912 from human recombinant alpha2A adrenergic receptor expressed in Sf9 cells at 10 uM after 60 mins relative to control
|
Homo sapiens
|
-5.0
%
|
|
|
Binding affinity to adrenergic alpha2 receptor (unknown origin) by radioligand displacement assay
|
Homo sapiens
|
25.0
nM
|
|
Binding affinity to adrenergic alpha2 receptor (unknown origin) by radioligand displacement assay
|
Homo sapiens
|
58.0
nM
|
|
|
Displacement of [125I]Clonidine from adrenergic alpha2B receptor (unknown origin)
|
Homo sapiens
|
28.84
nM
|
|
Displacement of [125I]Clonidine from adrenergic alpha2B receptor (unknown origin)
|
Homo sapiens
|
3.2
nM
|
|
|
Displacement of [3H]RX821002 from human recombinant alpha2C adrenoceptor expressed in CHO cells
|
Homo sapiens
|
0.5
nM
|
|
|
Displacement of [3H]RX-821002 from human adrenergic alpha2C receptor expressed in CHO cells
|
Homo sapiens
|
0.5
nM
|
|
|
Displacement of [3H]RX 821002 from rat cerebral cortex Alpha-2 adrenergic receptor
|
Rattus norvegicus
|
96.0
nM
|
|
|
Displacement of [3H]RX 821002 from rat cerebral cortex alpha-2 adrenergic receptor measured after 60 mins by scintillation counting method
|
Rattus norvegicus
|
96.0
nM
|
|
|
Antagonist activity at human CCR8 expressed in CHOK1 cells assessed as inhibition in CCL1-induced beta-arrestin 2 recruitment at 20 uM incubated for 30 mins followed by CCL1 addition and measured after 90 or 180 mins by pathhunter beta-arrestin assay relative to control
|
Homo sapiens
|
5.0
%
|
|
|
Antagonist activity at human Gs/Gi/o-coupled CHRM4 expressed in CHOK1 cells assessed as inhibition in acetylcholine-induced beta-arrestin 2 recruitment at 20 uM incubated for 30 mins followed by acetylcholine addition and measured after 90 or 180 mins by pathhunter beta-arrestin assay relative to control
|
Homo sapiens
|
4.0
%
|
|
|
Antagonist activity at human Gi/o-coupled CNR1 expressed in CHOK1 cells assessed as inhibition in CP55940-induced beta-arrestin 2 recruitment at 20 uM incubated for 30 mins followed by CP55940 addition and measured after 90 or 180 mins by pathhunter beta-arrestin assay relative to control
|
Homo sapiens
|
35.0
%
|
|
|
Antagonist activity at human Gi/o-coupled CNR2 expressed in CHOK1 cells assessed as inhibition in CP55940-induced beta-arrestin 2 recruitment at 20 uM incubated for 30 mins followed by CP55940 addition and measured after 90 or 180 mins by pathhunter beta-arrestin assay relative to control
|
Homo sapiens
|
20.0
%
|
|
|
Antagonist activity at human Gi/o-coupled CXCR4 expressed in mouse C2C12 cells assessed as inhibition in CXCL12-induced beta-arrestin 2 recruitment at 20 uM incubated for 30 mins followed by CXCL12 addition and measured after 90 or 180 mins by pathhunter beta-arrestin assay relative to control
|
Homo sapiens
|
21.0
%
|
|
|
Antagonist activity at human Gi/o-coupled DRD2L expressed in CHOK1 cells assessed as inhibition in dopamine-induced beta-arrestin 2 recruitment at 20 uM incubated for 30 mins followed by dopamine addition and measured after 90 or 180 mins by pathhunter beta-arrestin assay relative to control
|
Homo sapiens
|
102.0
%
|
|
|
Antagonist activity at human Gi/o-coupled FPR1 expressed in CHOK1 cells assessed as inhibition in WKYMVm-NH2-induced beta-arrestin 2 recruitment at 20 uM incubated for 30 mins followed by WKYMVm-NH2 addition and measured after 90 or 180 mins by pathhunter beta-arrestin assay relative to control
|
Homo sapiens
|
-6.0
%
|
|
|
Antagonist activity at human GPR119 assessed as inhibition in oleoylethanolamide-induced beta-arrestin 2 recruitment at 20 uM incubated for 30 mins followed by oleoylethanolamide addition and measured after 90 or 180 mins by pathhunter beta-arrestin assay relative to control
|
Homo sapiens
|
8.0
%
|
|
|
Antagonist activity at human Gq-coupled HCRTR2 expressed in CHOK1 cells assessed as inhibition in Orexin A-induced beta-arrestin 2 recruitment at 20 uM incubated for 30 mins followed by Orexin A addition and measured after 90 or 180 mins by pathhunter beta-arrestin assay relative to control
|
Homo sapiens
|
9.0
%
|
|
|
Antagonist activity at human Gq-coupled HRH1 expressed in CHOK1 cells assessed as inhibition in histamine-induced beta-arrestin 2 recruitment at 20 uM incubated for 30 mins followed by histamine addition and measured after 90 or 180 mins by pathhunter beta-arrestin assay relative to control
|
Homo sapiens
|
30.0
%
|
|
|
Antagonist activity at human Gq-coupled NPSR1b expressed in human U2OS cells assessed as inhibition in neuropeptide S-induced beta-arrestin 2 recruitment at 20 uM incubated for 30 mins followed by neuropeptide S addition and measured after 90 or 180 mins by pathhunter beta-arrestin assay relative to control
|
Homo sapiens
|
-3.0
%
|
|
|
Antagonist activity at human Gq-coupled PRLHR expressed in CHOK1 cells assessed as inhibition in prolactin releasing peptide (1 to 31)-induced beta-arrestin 2 recruitment at 20 uM incubated for 30 mins followed by prolactin releasing peptide (1 to 31) addition and measured after 90 or 180 mins by pathhunter beta-arrestin assay relative to control
|
Homo sapiens
|
1.0
%
|
|
|
Antagonist activity at human Gs-coupled PTGIR assessed as inhibition in beraprost-induced beta-arrestin 2 recruitment at 20 uM incubated for 30 mins followed by beraprost- addition and measured after 90 or 180 mins by pathhunter beta-arrestin assay relative to control
|
Homo sapiens
|
8.0
%
|
|
|
Displacement of [3H]RX 821002 from human recombinant adrenergic alpha-2A receptor expressed in CHO cell membranes incubated for 60 mins
|
Homo sapiens
|
3.13
nM
|
|
|
Displacement of [3H]RX 821002 from human recombinant adrenergic alpha-2B receptor expressed in CHO cell membranes incubated for 60 mins
|
Homo sapiens
|
1.16
nM
|
|
|
Displacement of [3H]RX 821002 from human recombinant adrenergic alpha-2C receptor expressed in CHO cell membranes incubated for 60 mins
|
Homo sapiens
|
0.8
nM
|
|
|
Antagonist activity at human ADRA1B expressed in CHO-K1 cells at 20 uM by PathHunter beta-arrestin assay relative to control
|
Homo sapiens
|
90.0
%
|
|
|
Antagonist activity at human ADRA2B expressed in CHO-K1 cells at 20 uM by PathHunter beta-arrestin assay relative to control
|
Homo sapiens
|
107.0
%
|
|
|
Antagonist activity at human AVPR2 at 20 uM by PathHunter beta-arrestin assay relative to control
|
Homo sapiens
|
-1.0
%
|
|
|
Antagonist activity at human CCR3 expressed in CHO-K1 cells at 20 uM by PathHunter beta-arrestin assay relative to control
|
Homo sapiens
|
-13.0
%
|
|
|
Antagonist activity at human CCR8 expressed in CHO-K1 cells at 20 uM by PathHunter beta-arrestin assay relative to control
|
Homo sapiens
|
5.0
%
|
|
|
Antagonist activity at human CX3CR1 expressed in CHO-K1 cells at 20 uM by PathHunter beta-arrestin assay relative to control
|
Homo sapiens
|
22.0
%
|
|
|
Antagonist activity at human CXCR4 expressed in mouse C2C12 cells at 20 uM by PathHunter beta-arrestin assay relative to control
|
Homo sapiens
|
21.0
%
|
|
|
Antagonist activity at human DRD2L expressed in CHO-K1 cells at 20 uM by PathHunter beta-arrestin assay relative to control
|
Homo sapiens
|
102.0
%
|
|
|
Antagonist activity at human FSHR expressed in CHO-K1 cells at 20 uM by PathHunter beta-arrestin assay relative to control
|
Homo sapiens
|
4.0
%
|
|
|
Antagonist activity at HTR1B in human U2OS cells at 20 uM by PathHunter beta-arrestin assay relative to control
|
Homo sapiens
|
86.0
%
|
|
|
Antagonist activity at HTR2C in human U2OS cells at 20 uM by PathHunter beta-arrestin assay relative to control
|
Homo sapiens
|
1.0
%
|
|
|
Antagonist activity at NPSR1B in human U2OS cells at 20 uM by PathHunter beta-arrestin assay relative to control
|
Homo sapiens
|
-3.0
%
|
|
|
Antagonist activity at human OXTR expressed in CHO-K1 cells at 20 uM by PathHunter beta-arrestin assay relative to control
|
Homo sapiens
|
5.0
%
|
|
|
Antagonist activity at human PRLHR expressed in CHO-K1 cells at 20 uM by PathHunter beta-arrestin assay relative to control
|
Homo sapiens
|
1.0
%
|
|
|
Antagonist activity at human ADRA2A expressed in CHO-K1 cells at 20 uM by PathHunter beta-arrestin assay relative to control
|
Homo sapiens
|
92.0
%
|
|
