|
Concentration that produces 50 % displacement of specific [3H]clonidine binding to Alpha adrenergic receptor in rat brain cortical membrane preparations.
|
None
|
61.0
nM
|
|
|
Compound was tested for its binding affinity against Alpha-2 adrenergic receptor
|
None
|
977.24
nM
|
|
|
Binding Affinity was tested on low Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.
|
None
|
650.0
nM
|
|
|
Binding Affinity was tested on high Affinity Site of Bovine Dopamine D2 Receptor. Tested for ability to displace the radioligand [3H]spiperone was tested
|
None
|
11.0
nM
|
|
|
Growth inhibition of Don-6 cell lines at 1.0 mM concentration
|
Cricetulus griseus
|
30.0
%
|
|
|
Tested for its ability to stimulate rat caudate adenylate cyclase (Dopamine receptor D1) at 10 uM
|
None
|
3.5
|
|
|
In vitro binding affinity towards Dopamine D1 receptor using [3H]-SCH- 23390 as radioligand
|
None
|
200.0
nM
|
|
|
The percentage stimulation of adenylate cyclase activity of compound was measured on dopamine receptor D1 of Rat Striatum at 0.01 uM
|
None
|
104.0
%
|
|
|
The percentage stimulation of adenylate cyclase activity of compound was measured on dopamine receptor D1 of Rat Striatum at 0.1 uM
|
None
|
113.0
%
|
|
|
The percentage stimulation of adenylate cyclase activity of compound was measured on dopamine receptor D1 of Rat Striatum at 10 uM
|
None
|
151.0
%
|
|
|
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D2 using FLIPR assay
|
None
|
8.0
nM
|
|
|
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D2 using FLIPR assay
|
None
|
1.1
nM
|
|
|
Percent stimulation of adenylate cyclase activity at dopamine receptor D1 of Rat Striatum at 1 uM
|
Rattus norvegicus
|
110.0
%
|
|
|
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
|
Rattus norvegicus
|
150.0
nM
|
|
|
Displacement of [3H]quinpirole from human dopamine D2A receptors expressed in LtK cells
|
Homo sapiens
|
1.89
nM
|
|
|
Displacement of [3H]raclopride from human dopamine D2A receptors expressed in LtK cells
|
Homo sapiens
|
759.0
nM
|
|
|
Inhibition of [35S]GTP-gamma-S, binding to cell membranes expressing dopamine D2A receptors at 100 uM
|
None
|
16.0
%
|
|
|
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
|
None
|
416.87
nM
|
|
|
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
|
Rattus norvegicus
|
309.03
nM
|
|
|
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
|
None
|
192.0
nM
|
|
|
Binding Affinity on high Affinity Site of Bovine dopamine receptor D2. Tested for ability to displace the radioligand [3H]pramipexole was tested
|
None
|
1.8
nM
|
|
|
Binding Affinity was tested on relative proportion of high Affinity Site of Bovine dopamine receptor D2. Tested for ability to displace the radioligand [3H]spiperone at the binding site.
|
None
|
51.0
nM
|
|
|
High binding affinity for dopamine D-2 receptor from bovine anterior pituitary membrane, using radioligand [3H]spiroperidol
|
None
|
34.0
nM
|
|
|
Inhibition of [3H]dopamine binding to Dopamine receptor in calf caudate nuclei.
|
None
|
64.0
nM
|
|
|
Inhibitory binding activity against dopamine receptor using [3H]ADTN as the radioligand in striatal tissue of calf brain.
|
None
|
510.0
nM
|
|
|
Tested for binding to dopamine receptor using [3H]- ADTN as radioligand in calf caudate nucleus homogenates.
|
None
|
3.7
nM
|
|
|
Tested for binding to dopamine receptor using [3H]apomorphine as radioligand in calf caudate nucleus homogenates.
|
None
|
4.5
nM
|
|
|
The IC50 value was reported as apparent, since [3H]NCA was purported to be irreversible. Result indicates the mean of two separate experiments, each performed in triplicate.
|
Canis lupus familiaris
|
15.0
nM
|
|
|
Agonist required to inhibit Dopamine receptor D2 photoinactivation by 50% with Iodazidoclebopride using [3H]-Spiperone
|
Canis lupus familiaris
|
8e-06
nM
|
|
|
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D2
|
None
|
170.0
nM
|
|
|
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D2 using FLIPR assay
|
None
|
18.0
nM
|
|
|
Binding affinity against cloned human Dopamine receptor D2 using [3H]spiperone as radioligand transfected in HEK cells
|
None
|
260.0
nM
|
|
|
Inhibition of [3H]dopamine uptake in HEK cells expressing human DAT
|
Homo sapiens
|
460.0
nM
|
|
|
Displacement of [3H]quinpirole from Dopamine receptor D2
|
None
|
1.89
nM
|
|
|
Inhibition of [3H]raclopride binding to Dopamine receptor D2
|
Homo sapiens
|
572.0
nM
|
|
|
Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390
|
None
|
7.0
nM
|
|
|
Binding Affinity was tested on relative proportion of High Affinity Site of Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.
|
None
|
36.0
nM
|
|
|
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
|
None
|
100.0
nM
|
|
|
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
|
None
|
130.0
nM
|
|
|
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
|
Rattus norvegicus
|
800.0
nM
|
|
|
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
|
None
|
2.7
nM
|
|
|
Binding Affinity was determined against Dopamine receptor D2 in rat striatal membranes using [3H]- spiperone radioligand.
|
None
|
724.44
nM
|
|
|
Binding affinity against Dopamine receptor D2 in rat striatal membranes using [3H]spiperone
|
Rattus norvegicus
|
104.71
nM
|
|
|
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
|
None
|
2.4
nM
|
|
|
Binding affinity for dopamine D4-like receptor labelled with [3H]YM-09151-2 in retina
|
Bos taurus
|
15.0
nM
|
|
|
Binding Affinity was determined in the presence of 100 micro M Gpp(NH)p for decoupling of the ternary complex of Compound to Dopamine receptor D4.4
|
None
|
97.0
nM
|
|
|
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
|
Homo sapiens
|
1.2
nM
|
|
|
Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4
|
None
|
62.0
nM
|
|
|
Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4
|
None
|
57.0
nM
|
|
|
Tested for binding affinity against Dopamine receptor D2 like from bovine striatum membranes by using [3H]YM-09151-2 radioligand
|
Bos taurus
|
617.0
nM
|
|
|
Inhibition of [3H]YM-09151-2 binding to bovine retina membrane Dopamine receptor D2, high affinity site
|
Bos taurus
|
14.9
nM
|
|
|
Binding affinity for dopamine D2-D3 like receptor labelled with [3H]YM-09151-2 in striatum
|
Bos taurus
|
130.0
nM
|
|
|
Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D2L
|
None
|
42.0
nM
|
|
|
Binding affinity on High Affinity Site of Dopamine receptor D2L
|
Homo sapiens
|
20.0
nM
|
|
|
Binding Affinity on High Affinity Site of Dopamine receptor D2S
|
Homo sapiens
|
17.0
nM
|
|
|
Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D2S
|
None
|
34.0
nM
|
|
|
The percentage inhibition of adenylate cyclase activity of compound was measured on dopamine receptor D2 of Rat Striatum at 0.01 micro M
|
None
|
95.0
%
|
|
|
The percentage inhibition of adenylate cyclase activity of compound was measured on dopamine receptor D2 of Rat Striatum at 0.1 micro M
|
None
|
92.0
%
|
|
|
The percentage inhibition of adenylate cyclase activity of compound was measured on dopamine receptor D2 of Rat Striatum at 10 micro M
|
None
|
83.0
%
|
|
|
The percentage inhibition of adenylate cyclase activity of compound was measured on dopamine receptor D2 of Rat Striatum at 1 micro M
|
None
|
87.0
%
|
|
|
Binding Affinity was determined in the presence of 100 micro M Gpp(NH)p for decoupling of the ternary complex of Compound to Dopamine receptor D3
|
None
|
290.0
nM
|
|
|
Binding Affinity was tested on the high affinity site of Dopamine receptor D3
|
Homo sapiens
|
50.0
nM
|
|
|
Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D3
|
None
|
52.0
nM
|
|
|
Displacement of [3H]raclopride from Dopamine receptor D3
|
Homo sapiens
|
13.2
nM
|
|
|
Binding affinity which represents concentration giving half-maximal inhibition of [3H]7-OH-DPAT binding to Dopamine receptor D3 in rat tissue homogenate
|
None
|
11.0
nM
|
|
|
Tested for binding affinity against dopamine receptor D3 expressed in Sf9 cells.
|
None
|
49.3
nM
|
|
|
In vitro affinity against Dopamine receptor D2 using [3H]DP-5,6-ADTN radioligand in rat striatal homogenate.
|
None
|
15.0
nM
|
|
|
Competitive binding assay against Dopamine receptor D2 in rat striatal membranes and [125I]-IBF radioligand
|
Rattus norvegicus
|
843.0
nM
|
|
|
Inhibitory constant against binding of [125I]- IBZM to rat striatal membrane
|
None
|
296.0
nM
|
|
|
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
|
None
|
2.2
nM
|
|
|
Inhibition of [3H]norepinephrine uptake in HEK cells expressing human NET
|
Homo sapiens
|
6.63
nM
|
|
|
Ability to relax the electrically stimulated rabbit ear artery was determined
|
Oryctolagus cuniculus
|
76.0
nM
|
|
|
Inhibition of the constrictor response to electrical stimulation in rabbit ear artery.
|
Oryctolagus cuniculus
|
38.0
nM
|
|
|
Ability to stimulate peripheral prejunctional dopaminergic receptors by 50% inhibition of vasoconstrictor response to field stimulation in isolated perfused rabbit ear artery
|
Oryctolagus cuniculus
|
73.0
nM
|
|
|
Compound concentration required to reduce specific binding of tritiated dopamine to rat brain striatal membrane by 50 % was reported
|
Rattus norvegicus
|
29.0
nM
|
|
|
Maximal degree of inhibition at 1 uM concentration was determined from displacement of [3H]dopamine binding to rat brain striatal membrane
|
Rattus norvegicus
|
32.0
%
|
|
|
Inhibitory concentration for half-maximal displacement of 1.0 nM [3H]ADTN specific binding from rat striatal membranes using 10E-5 sulpiride
|
Rattus norvegicus
|
2.1
nM
|
|
|
Inhibitory concentration half-maximal displacement of 1.0 nM [3H]NPA specific binding from rat striatal membranes using 10e-5 (+/-)ADTN
|
Rattus norvegicus
|
2.0
nM
|
|
|
Binding of [3H]clonidine to alpha-2-adrenergic receptor of rat cerebral cortical membranes
|
None
|
58.0
nM
|
|
|
Growth inhibition of YT-nu cell lines at 1.0 mM concentration
|
Homo sapiens
|
40.0
%
|
|
|
Inhibitory activity against tyrosinase at 100uM
|
Homo sapiens
|
10.0
%
|
|
|
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
|
Homo sapiens
|
120.0
nM
|
|
|
Activity at rat dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
|
Rattus norvegicus
|
5.0
nM
|
|
|
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
|
Homo sapiens
|
10.0
nM
|
|
|
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
|
Homo sapiens
|
2.2
nM
|
|
|
Agonist activity at ferret D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
|
Mustela putorius furo
|
2.7
nM
|
|
|
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
|
Rattus norvegicus
|
2.4
nM
|
|
|
Agonist activity at human D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
|
Homo sapiens
|
18.0
nM
|
|
|
Agonist activity at ferret D2 receptor in HEK293 cells coexpressing Galphaqo5 by FLIPR
|
Mustela putorius furo
|
8.0
nM
|
|
|
Agonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
|
Rattus norvegicus
|
1.1
nM
|
|
|
Agonist activity at human cloned dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
|
Homo sapiens
|
209.0
nM
|
|
|
Agonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S binding
|
Homo sapiens
|
8.53
nM
|
|
|
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
|
Homo sapiens
|
35.0
nM
|
|
|
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
|
Homo sapiens
|
43.0
nM
|
|
|
Inhibition of dopamine transporter-mediated [3H]dopamine uptake in Wistar rat striatal synaptosomes by liquid scintillation spectrometry
|
Rattus norvegicus
|
200.0
nM
|
|
|
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
|
Homo sapiens
|
209.0
nM
|
|
|
Agonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS binding
|
Homo sapiens
|
8.53
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
|
11.8
%
|
|
|
Displacement of [3H]spiperone from human D2long receptor expressed in CHO cells
|
Homo sapiens
|
450.0
nM
|
|
|
Displacement of [3H]spiperone from human D2short receptor expressed in CHO cells
|
Homo sapiens
|
360.0
nM
|
|
|
Displacement of [3H]spiperone from human D3 receptor expressed in CHO cells
|
Homo sapiens
|
240.0
nM
|
|
|
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cells
|
Homo sapiens
|
6.2
nM
|
|
|
Displacement of [3H]spiperone from human wild type D3 receptor expressed in human HEK293 cells
|
Homo sapiens
|
72.0
nM
|
|
|
Activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
|
Homo sapiens
|
209.0
nM
|
|
|
Activity at human dopamine D3 receptor expressed in AtT cells assessed as stimulation of [35S]GTPgammaS binding
|
Homo sapiens
|
8.53
nM
|
|
|
Displacement of [3H]raclopride from rat dopamine D2short receptor expressed in CHO-K1 cells by liquid scintillation counting
|
Rattus norvegicus
|
197.0
nM
|
|
|
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
|
None
|
124.0
nM
|
|
|
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma binding
|
Homo sapiens
|
209.0
nM
|
|
|
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
|
Homo sapiens
|
8.53
nM
|
|
|
Displacement of [3H]spiperone from human dopamine D2 receptor at high affinity state expressed in HEK293 cells
|
Homo sapiens
|
2.9
nM
|
|
|
Agonist activity at human dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
|
Homo sapiens
|
209.0
nM
|
|
|
Agonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
|
Homo sapiens
|
4.76
nM
|
|
|
Agonist activity at human D1 receptor assessed as cAMP accumulation
|
Homo sapiens
|
20.0
nM
|
|
|
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
|
Homo sapiens
|
209.0
nM
|
|
|
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
|
Homo sapiens
|
4.76
nM
|
|
|
Displacement of [3H]SCH23390 from dopamine D1-like receptor pig striatal membrane
|
Sus scrofa
|
1.33
nM
|
|
|
Antioxidant activity against AAPH-induced lipid peroxidation assessed as inhibition of conjugated diene hydroperoxide production at 0.1 mM by UV spectrophotometry
|
None
|
43.0
%
|
|
|
Antiinflammatory activity in Fisher rat assessed as inhibition of carrageenan-induced paw oedema at 0.01 mmol/kg, po measured after 3.5 hrs
|
Rattus norvegicus
|
13.0
%
|
|
|
Displacement of [3H]raclopride from human D3 receptor expressed in HEK293 cells
|
Homo sapiens
|
15.0
nM
|
|
|
Agonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
|
Homo sapiens
|
227.0
nM
|
|
|
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
|
Homo sapiens
|
8.57
nM
|
|
|
Agonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay
|
Homo sapiens
|
6.1
nM
|
|
|
Agonist activity at human dopamine D2 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay
|
Homo sapiens
|
65.0
nM
|
|
|
Displacement of [3H]YM-09151-2 from human dopamine D2 receptor expressed in CHOp cells
|
Homo sapiens
|
422.0
nM
|
|
|
Displacement of [3H]YM-09151-2 from human dopamine D3 receptor expressed in CHOp cells
|
Homo sapiens
|
20.0
nM
|
|
|
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assay
|
Homo sapiens
|
5.8
nM
|
|
|
Agonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTP gammaS binding assay
|
Homo sapiens
|
240.0
nM
|
|
|
Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D3 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
|
Rattus norvegicus
|
111.0
nM
|
|
|
Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D3 trunk/D3 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
|
Rattus norvegicus
|
124.0
nM
|
|
|
Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D3 trunk/D2 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
|
Rattus norvegicus
|
483.0
nM
|
|
|
Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D2 trunk/D3 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
|
Rattus norvegicus
|
582.0
nM
|
|
|
Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells
|
Homo sapiens
|
21.0
nM
|
|
|
Displacement of [3H]spiperone from human dopamine D2short receptor expressed in CHO cells
|
Homo sapiens
|
110.0
nM
|
|
|
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
|
Homo sapiens
|
8.9
nM
|
|
|
Displacement of [3H]spiperone from human dopamine D2long receptor expressed in CHO cells
|
Homo sapiens
|
190.0
nM
|
|
|
Displacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatum
|
Bos taurus
|
440.0
nM
|
|
|
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
|
Homo sapiens
|
7.64
nM
|
|
|
Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
|
Homo sapiens
|
227.0
nM
|
|
|
Agonist activity at dopamine D3 receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 by FLIPR assay
|
Homo sapiens
|
1.8
nM
|
|
|
Agonist activity at dopamine D2 receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 by FLIPR assay
|
Homo sapiens
|
6.7
nM
|
|
|
Displacement of [3H]raclopride from human dopamine D3 receptor expressed in HEK293 cells by scintillation counting analysis
|
Homo sapiens
|
15.0
nM
|
|
|
Displacement of [3H]-NPA from dopamine D2L receptor (unknown origin) expressed in CHO cell membranes
|
Homo sapiens
|
8.0
nM
|
|
|
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
|
Homo sapiens
|
36.0
nM
|
|
|
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
|
Homo sapiens
|
39.0
nM
|
|
|
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
|
Homo sapiens
|
10.6
nM
|
|
|
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
|
Homo sapiens
|
218.0
nM
|
|
|
Displacement of [3Hprazosin from adrenergic alpha1 receptor in pig cerebral cortex homogenates by competitive binding assay
|
Sus scrofa
|
309.03
nM
|
|
Displacement of [3Hprazosin from adrenergic alpha1 receptor in pig cerebral cortex homogenates by competitive binding assay
|
Sus scrofa
|
310.0
nM
|
|
|
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
|
Homo sapiens
|
467.74
nM
|
|
Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
|
Homo sapiens
|
470.0
nM
|
|
|
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
|
Homo sapiens
|
9.333
nM
|
|
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
|
Homo sapiens
|
9.3
nM
|
|
|
Antioxidant activity assessed as inhibition of AAPH-induced linoleic acid lipid peroxidation at 100 uM
|
None
|
43.0
%
|
|
|
Anti-inflammatory activity in Fisher 344 rat assessed as inhibition of carrageenan-induced paw edema at 0.01 mmol/kg, ip after 3.5 hrs
|
Rattus norvegicus
|
13.0
%
|
|
|
Agonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
|
Homo sapiens
|
5.34
nM
|
|
|
Displacement of [3H]Spiroperidol from cloned rat dopamine D2L receptor expressed in HEK293 cells by liquid scintillation counting analysis
|
Rattus norvegicus
|
990.0
nM
|
|
|
Displacement of [3H]Spiroperidol from cloned rat dopamine D3 receptor expressed in HEK293 cells by liquid scintillation counting analysis
|
Rattus norvegicus
|
101.0
nM
|
|
|
Agonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
|
Homo sapiens
|
183.0
nM
|
|
|
Displacement of [3H]spiperone from human D2S receptor expressed in CHO cells
|
Homo sapiens
|
48.0
nM
|
|
|
Displacement of [3H]N-methylspiperone from human D3 receptor transfected in HEK293 cells measured after 60 mins by liquid scintillation counter
|
Homo sapiens
|
293.0
nM
|
|
|
Displacement of [3H]7-OH-DPAT from human D2 receptor transfected in HEK293 cells measured after 60 mins by liquid scintillation counter
|
Homo sapiens
|
8.73
nM
|
|
|
Displacement of [3H]7-OH-DPAT from human D3 receptor transfected in HEK293 cells measured after 60 mins by liquid scintillation counter
|
Homo sapiens
|
7.58
nM
|
|
|
Agonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assay
|
Homo sapiens
|
5.0
nM
|
|
|
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
|
Homo sapiens
|
1.8
nM
|
|
|
Agonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
|
Homo sapiens
|
7.7
nM
|
|
|
Agonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
|
Homo sapiens
|
2.7
nM
|
|
|
Displacement of [3H]SCH23390 from D1-like dopaminergic receptor (unknown origin) in striatal membrane measured after 1 hr by liquid scintillation counting method
|
Homo sapiens
|
549.54
nM
|
|
Displacement of [3H]SCH23390 from D1-like dopaminergic receptor (unknown origin) in striatal membrane measured after 1 hr by liquid scintillation counting method
|
Homo sapiens
|
550.0
nM
|
|
|
Displacement of [3H]raclopride from D2-like dopaminergic receptor (unknown origin) in striatal membrane measured after 1 hr by liquid scintillation counting method
|
Homo sapiens
|
145.55
nM
|
|
Displacement of [3H]raclopride from D2-like dopaminergic receptor (unknown origin) in striatal membrane measured after 1 hr by liquid scintillation counting method
|
Homo sapiens
|
560.0
nM
|
|
|
Agonist activity at D2 receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 by fluo-4 dye based FLIPR assay
|
Homo sapiens
|
0.69
nM
|
|
|
Agonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay
|
Homo sapiens
|
3.981
nM
|
|
|
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai2 after 10 mins by BRET assay
|
Homo sapiens
|
3.9
nM
|
|
|
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai1 after 10 mins by BRET assay
|
Homo sapiens
|
2.8
nM
|
|
|
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai3 after 10 mins by BRET assay
|
Homo sapiens
|
4.5
nM
|
|
|
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assay
|
Homo sapiens
|
0.67
nM
|
|
|
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assay
|
Homo sapiens
|
0.78
nM
|
|
|
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells assessed as induction of renilla luciferase 2-tagged beta-arrestin-1 recruitment after 15 mins by BRET assay
|
Homo sapiens
|
226.0
nM
|
|
|
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells assessed as induction of renilla luciferase 2-tagged beta-arrestin-2 recruitment after 15 mins by BRET assay
|
Homo sapiens
|
163.0
nM
|
|
|
Agonist activity at ARMS2-PK2 tagged D2S receptor (unknown origin) expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin-2 recruitment incubated for 5 hrs measured after 60 mins by PathHunter assay
|
Homo sapiens
|
156.0
nM
|
|
|
Displacement of [3H]-(R)-(+)-7-OH-DPAT from human dopamine D2 receptor expressed in HEK293 cell membranes after 90 mins by micro beta scintillation counting analysis
|
Homo sapiens
|
16.0
nM
|
|
|
Displacement of [3H]-(R)-(+)-7-OH-DPAT from human dopamine D3 receptor expressed in HEK293 cell membranes after 90 mins by micro beta scintillation counting analysis
|
Homo sapiens
|
2.97
nM
|
|
|
Partial agonist activity at human D2SR expressed in HEK293T cells co-expressing (EA)beta-arrestin2 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assay
|
Homo sapiens
|
390.0
nM
|
|
|
Agonist activity at human D2S receptor expressed in HEK293T cell membranes coexpressing Galphao1 assessed as induction of nucleotide exchange preincubated for 30 mins followed by addition of [35S]GTPgammaS measured after 30 mins by [35S]GTPgammaS binding assay
|
Homo sapiens
|
200.0
nM
|
|
|
Partial agonist activity at human D2SR expressed in HEK293T cells co-expressing (EA)beta-arrestin2 and GRK2 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assay
|
Homo sapiens
|
160.0
nM
|
|
|
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assay
|
Homo sapiens
|
12.3
nM
|
|
|
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assay
|
Homo sapiens
|
91.2
nM
|
|
|
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
|
Homo sapiens
|
232.0
nM
|
|
|
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
|
Homo sapiens
|
243.0
nM
|
|
|
Agonist activity at dopamine D2 receptor long isoform (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 min by calcium 4-dye based FLIPR assay
|
Homo sapiens
|
19.0
nM
|
|
|
Agonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay
|
Homo sapiens
|
2.1
nM
|
|
|
Agonist activity at D2 receptor (unknown origin) expressed in CHOK1 cells assessed as increase in calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation under room temperature measured after 20 secs for 100 secs by calcium-4 dye based FLIPR assay
|
Homo sapiens
|
0.99
nM
|
|
|
Agonist activity at human D2S receptor expressed in CHOK1 cells assessed as inhibition of forskolin induced cAMP production incubated for 10 mins followed by forskolin addition and measured after 5 mins by HTRF assay
|
Homo sapiens
|
40.0
nM
|
|
|
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
|
Homo sapiens
|
0.11
nM
|
|
|
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
|
Homo sapiens
|
6.4
nM
|
|
|
Agonist activity at human D2R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
|
Homo sapiens
|
140.0
nM
|
|
|
Agonist activity at RLuc8-fused human D3R expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
|
Homo sapiens
|
2.3
nM
|
|
|
Agonist activity at RLuc8-fused Go-coupled human D3R expressed in HEK293 cells untagged beta1 and mVenus-tagged gamma2 measured after 5 mins in presence of coelenterazine H by BRET assay
|
Homo sapiens
|
1.1
nM
|
|
|
Agonist activity at human D3R expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 5 mins in presence of beta-adrenergic blocker propranolol and coelenterazine H by CAMYEL BRET assay
|
Homo sapiens
|
3.5
nM
|
|
|
Agonist activity at human D3R stably expressed in CHOK1 cells assessed as increase in ERK1/2 phosphorylation measured after 15 mins by AlphaScreen surefire assay
|
Homo sapiens
|
2.9
nM
|
|
|
Agonist activity at RLuc8-fused human D3R Y198A mutant expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
|
Homo sapiens
|
55.0
nM
|
|
|
Agonist activity at RLuc8-fused human D3R Y365A mutant expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
|
Homo sapiens
|
33.0
nM
|
|
|
Agonist activity at RLuc8-fused human D3R Y198A/Y365A double mutant expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
|
Homo sapiens
|
820.0
nM
|
|
|
Displacement of [3H]spiperone from rat D2L dopamine receptor expressed in HEK293 cell membranes after 1 hr
|
Rattus norvegicus
|
990.0
nM
|
|
|
Displacement of [3H]spiperone from rat D3 dopamine receptor expressed in HEK293 cell membranes after 1 hr
|
Rattus norvegicus
|
101.0
nM
|
|
|
Agonist activity at human D2 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assay
|
Homo sapiens
|
376.0
nM
|
|
|
Agonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assay
|
Homo sapiens
|
7.26
nM
|
|
|
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
|
Homo sapiens
|
44.0
nM
|
|
|
Agonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
|
Homo sapiens
|
0.8
nM
|
|
|
Agonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
|
Homo sapiens
|
1.8
nM
|
|
|
Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
|
Homo sapiens
|
2.0
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
|
-7.49
%
|
|
|
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
|
-0.21
%
|
|
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
|
-0.21
%
|
|
|
Inhibition of alpha-synuclein fibril formation (unknown origin) incubated for 6 days by thioflavin S based fluorescence assay
|
Homo sapiens
|
530.0
nM
|
|
|
Agonist activity at human D2 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay
|
Homo sapiens
|
18.2
nM
|
|
|
Agonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay
|
Homo sapiens
|
0.8913
nM
|
|
