Page last updated: 2024-08-07 15:48:34
Alpha-2A adrenergic receptor
An alpha-2A adrenergic receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:P08913]
Synonyms
Alpha-2 adrenergic receptor subtype C10;
Alpha-2A adrenoreceptor;
Alpha-2A adrenoceptor;
Alpha-2AAR
Research
Bioassay Publications (117)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 11 (9.40) | 18.7374 |
1990's | 21 (17.95) | 18.2507 |
2000's | 47 (40.17) | 29.6817 |
2010's | 30 (25.64) | 24.3611 |
2020's | 8 (6.84) | 2.80 |
Compounds (219)
Drugs with Inhibition Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
quinacrine | Homo sapiens (human) | IC50 | 2.2800 | 1 | 0 |
quinacrine | Homo sapiens (human) | Ki | 0.8550 | 1 | 0 |
4-nonylphenol | Homo sapiens (human) | IC50 | 6.7800 | 1 | 0 |
4-nonylphenol | Homo sapiens (human) | Ki | 2.5430 | 1 | 0 |
6-fluoronorepinephrine | Homo sapiens (human) | Ki | 0.0120 | 1 | 1 |
amiodarone | Homo sapiens (human) | IC50 | 0.3120 | 1 | 0 |
amiodarone | Homo sapiens (human) | Ki | 0.1170 | 1 | 0 |
amitriptyline | Homo sapiens (human) | IC50 | 0.1755 | 2 | 1 |
amitriptyline | Homo sapiens (human) | Ki | 0.1320 | 1 | 0 |
amlodipine | Homo sapiens (human) | IC50 | 0.6020 | 1 | 0 |
amlodipine | Homo sapiens (human) | Ki | 0.2260 | 1 | 0 |
amoxapine | Homo sapiens (human) | IC50 | 1.3140 | 1 | 0 |
amoxapine | Homo sapiens (human) | Ki | 0.4930 | 1 | 0 |
apraclonidine | Homo sapiens (human) | IC50 | 0.0040 | 1 | 1 |
apraclonidine | Homo sapiens (human) | Ki | 0.0029 | 1 | 1 |
astemizole | Homo sapiens (human) | IC50 | 4.8460 | 1 | 0 |
astemizole | Homo sapiens (human) | Ki | 1.8170 | 1 | 0 |
bithionol | Homo sapiens (human) | IC50 | 3.8240 | 1 | 0 |
bithionol | Homo sapiens (human) | Ki | 1.4340 | 1 | 0 |
bmy 7378 | Homo sapiens (human) | Ki | 0.1820 | 1 | 1 |
brimonidine | Homo sapiens (human) | IC50 | 0.1505 | 2 | 1 |
brimonidine | Homo sapiens (human) | Ki | 0.0294 | 3 | 3 |
butenafine | Homo sapiens (human) | IC50 | 3.6443 | 1 | 0 |
butenafine | Homo sapiens (human) | Ki | 1.3666 | 1 | 0 |
verapamil | Homo sapiens (human) | IC50 | 0.5790 | 1 | 0 |
verapamil | Homo sapiens (human) | Ki | 0.2170 | 1 | 0 |
carvedilol | Homo sapiens (human) | IC50 | 0.1060 | 1 | 0 |
carvedilol | Homo sapiens (human) | Ki | 0.0400 | 1 | 0 |
chloroquine | Homo sapiens (human) | Ki | 4.3652 | 1 | 1 |
chlorpromazine | Homo sapiens (human) | IC50 | 0.3520 | 1 | 0 |
chlorpromazine | Homo sapiens (human) | Ki | 0.1320 | 1 | 0 |
ciglitazone | Homo sapiens (human) | IC50 | 16.5510 | 1 | 0 |
ciglitazone | Homo sapiens (human) | Ki | 6.2070 | 1 | 0 |
cirazoline | Homo sapiens (human) | Ki | 0.0589 | 2 | 2 |
cisapride | Homo sapiens (human) | IC50 | 3.5923 | 3 | 2 |
cisapride | Homo sapiens (human) | Ki | 0.6660 | 1 | 0 |
clomipramine | Homo sapiens (human) | IC50 | 0.7070 | 2 | 1 |
clomipramine | Homo sapiens (human) | Ki | 0.5300 | 1 | 0 |
clonidine | Homo sapiens (human) | IC50 | 0.1010 | 3 | 2 |
clonidine | Homo sapiens (human) | Ki | 0.1437 | 7 | 6 |
clotrimazole | Homo sapiens (human) | IC50 | 11.8860 | 1 | 0 |
clotrimazole | Homo sapiens (human) | Ki | 4.4570 | 1 | 0 |
cyproheptadine | Homo sapiens (human) | IC50 | 0.2830 | 1 | 0 |
cyproheptadine | Homo sapiens (human) | Ki | 0.1060 | 1 | 0 |
desipramine | Homo sapiens (human) | IC50 | 0.0002 | 1 | 1 |
disulfiram | Homo sapiens (human) | IC50 | 4.9040 | 1 | 0 |
disulfiram | Homo sapiens (human) | Ki | 1.8390 | 1 | 0 |
domperidone | Homo sapiens (human) | IC50 | 2.7400 | 1 | 0 |
domperidone | Homo sapiens (human) | Ki | 1.0270 | 1 | 0 |
doxazosin | Homo sapiens (human) | Ki | 0.7290 | 1 | 1 |
doxepin | Homo sapiens (human) | IC50 | 0.6675 | 2 | 1 |
doxepin | Homo sapiens (human) | Ki | 0.5010 | 1 | 0 |
droperidol | Homo sapiens (human) | IC50 | 2.9650 | 1 | 0 |
droperidol | Homo sapiens (human) | Ki | 1.1120 | 1 | 0 |
ebastine | Homo sapiens (human) | IC50 | 0.8316 | 1 | 0 |
ebastine | Homo sapiens (human) | Ki | 0.3119 | 1 | 0 |
econazole | Homo sapiens (human) | IC50 | 4.3250 | 1 | 0 |
econazole | Homo sapiens (human) | Ki | 1.6220 | 1 | 0 |
fluphenazine | Homo sapiens (human) | IC50 | 0.2150 | 1 | 0 |
fluphenazine | Homo sapiens (human) | Ki | 0.0800 | 1 | 0 |
fluoxetine | Homo sapiens (human) | Ki | 0.0063 | 1 | 1 |
guanfacine | Homo sapiens (human) | IC50 | 0.1340 | 1 | 0 |
guanfacine | Homo sapiens (human) | Ki | 0.0500 | 1 | 0 |
haloperidol | Homo sapiens (human) | IC50 | 4.9730 | 1 | 0 |
haloperidol | Homo sapiens (human) | Ki | 3.4325 | 2 | 1 |
haloprogin | Homo sapiens (human) | IC50 | 1.2220 | 1 | 0 |
haloprogin | Homo sapiens (human) | Ki | 0.4580 | 1 | 0 |
hexachlorophene | Homo sapiens (human) | IC50 | 5.4965 | 1 | 0 |
hexachlorophene | Homo sapiens (human) | Ki | 2.0612 | 1 | 0 |
hydroxychloroquine | Homo sapiens (human) | Ki | 6.4565 | 1 | 1 |
ici 118551 | Homo sapiens (human) | IC50 | 0.0005 | 1 | 1 |
ketoconazole | Homo sapiens (human) | IC50 | 19.7830 | 1 | 0 |
ketoconazole | Homo sapiens (human) | Ki | 7.4190 | 1 | 0 |
ketotifen | Homo sapiens (human) | IC50 | 2.1870 | 1 | 0 |
ketotifen | Homo sapiens (human) | Ki | 0.8200 | 1 | 0 |
maprotiline | Homo sapiens (human) | IC50 | 1.8240 | 1 | 0 |
maprotiline | Homo sapiens (human) | Ki | 0.6840 | 1 | 0 |
methapyrilene | Homo sapiens (human) | IC50 | 1.1650 | 1 | 0 |
methapyrilene | Homo sapiens (human) | Ki | 0.4370 | 1 | 0 |
metoclopramide | Homo sapiens (human) | IC50 | 2.7210 | 1 | 0 |
metoclopramide | Homo sapiens (human) | Ki | 1.0200 | 1 | 0 |
mianserin | Homo sapiens (human) | IC50 | 0.0213 | 3 | 2 |
mianserin | Homo sapiens (human) | Ki | 0.0104 | 2 | 1 |
miconazole | Homo sapiens (human) | IC50 | 3.9660 | 1 | 0 |
miconazole | Homo sapiens (human) | Ki | 1.4870 | 1 | 0 |
mirtazapine | Homo sapiens (human) | IC50 | 0.0851 | 1 | 1 |
mirtazapine | Homo sapiens (human) | Ki | 0.0200 | 1 | 1 |
mitotane | Homo sapiens (human) | IC50 | 7.3470 | 1 | 0 |
mitotane | Homo sapiens (human) | Ki | 2.7550 | 1 | 0 |
nan 190 | Homo sapiens (human) | Ki | 0.0008 | 1 | 1 |
nortriptyline | Homo sapiens (human) | IC50 | 0.3660 | 2 | 1 |
nortriptyline | Homo sapiens (human) | Ki | 0.2750 | 1 | 0 |
orphenadrine | Homo sapiens (human) | IC50 | 2.1560 | 1 | 0 |
orphenadrine | Homo sapiens (human) | Ki | 0.8090 | 1 | 0 |
oxymetazoline | Homo sapiens (human) | IC50 | 0.0230 | 1 | 0 |
oxymetazoline | Homo sapiens (human) | Ki | 0.0890 | 17 | 20 |
4-iodoclonidine | Homo sapiens (human) | IC50 | 0.0015 | 1 | 1 |
pentamidine | Homo sapiens (human) | IC50 | 1.3750 | 1 | 0 |
pentamidine | Homo sapiens (human) | Ki | 0.5160 | 1 | 0 |
phenylpropanolamine | Homo sapiens (human) | Ki | 0.2754 | 1 | 1 |
moxonidine | Homo sapiens (human) | Ki | 0.1125 | 2 | 2 |
prazosin | Homo sapiens (human) | IC50 | 2.6380 | 1 | 0 |
prazosin | Homo sapiens (human) | Ki | 1.0695 | 14 | 13 |
prochlorperazine | Homo sapiens (human) | IC50 | 0.1690 | 1 | 0 |
prochlorperazine | Homo sapiens (human) | Ki | 0.0630 | 1 | 0 |
promazine | Homo sapiens (human) | IC50 | 0.3370 | 1 | 0 |
promazine | Homo sapiens (human) | Ki | 0.1260 | 1 | 0 |
promethazine | Homo sapiens (human) | IC50 | 0.6810 | 1 | 0 |
promethazine | Homo sapiens (human) | Ki | 0.2560 | 1 | 0 |
propranolol | Homo sapiens (human) | IC50 | 5.0119 | 1 | 1 |
pyrilamine | Homo sapiens (human) | IC50 | 2.9760 | 1 | 0 |
pyrilamine | Homo sapiens (human) | Ki | 1.1160 | 1 | 0 |
quetiapine | Homo sapiens (human) | IC50 | 2.4914 | 1 | 0 |
quetiapine | Homo sapiens (human) | Ki | 0.7071 | 3 | 2 |
raloxifene | Homo sapiens (human) | IC50 | 1.6640 | 1 | 0 |
raloxifene | Homo sapiens (human) | Ki | 0.6240 | 1 | 0 |
risperidone | Homo sapiens (human) | IC50 | 0.0097 | 1 | 0 |
risperidone | Homo sapiens (human) | Ki | 0.0102 | 5 | 4 |
semustine | Homo sapiens (human) | IC50 | 4.8090 | 1 | 0 |
semustine | Homo sapiens (human) | Ki | 1.8030 | 1 | 0 |
sk&f 29661 | Homo sapiens (human) | Ki | 75.8500 | 3 | 4 |
sulconazole | Homo sapiens (human) | IC50 | 4.0430 | 1 | 0 |
sulconazole | Homo sapiens (human) | Ki | 1.5160 | 1 | 0 |
sulpiride | Homo sapiens (human) | IC50 | 2.0190 | 1 | 0 |
sulpiride | Homo sapiens (human) | Ki | 0.7570 | 1 | 0 |
terazosin | Homo sapiens (human) | IC50 | 13.8320 | 1 | 0 |
terazosin | Homo sapiens (human) | Ki | 2.2977 | 5 | 4 |
thioridazine | Homo sapiens (human) | IC50 | 0.1330 | 1 | 0 |
thioridazine | Homo sapiens (human) | Ki | 0.0500 | 1 | 0 |
tiapride | Homo sapiens (human) | IC50 | 2.0780 | 1 | 0 |
tiapride | Homo sapiens (human) | Ki | 0.7790 | 1 | 0 |
ticlopidine | Homo sapiens (human) | IC50 | 0.3820 | 1 | 0 |
ticlopidine | Homo sapiens (human) | Ki | 0.1430 | 1 | 0 |
trazodone | Homo sapiens (human) | IC50 | 0.9090 | 1 | 0 |
trazodone | Homo sapiens (human) | Ki | 0.3410 | 1 | 0 |
5-methylurapidil | Homo sapiens (human) | Ki | 0.6120 | 1 | 1 |
wb 4101 | Homo sapiens (human) | Ki | 0.0035 | 1 | 1 |
xylometazoline | Homo sapiens (human) | Ki | 0.2955 | 2 | 2 |
zotepine | Homo sapiens (human) | Ki | 0.5700 | 2 | 2 |
phentolamine | Homo sapiens (human) | IC50 | 0.0060 | 1 | 0 |
phentolamine | Homo sapiens (human) | Ki | 0.0135 | 5 | 4 |
2-acetylaminofluorene | Homo sapiens (human) | IC50 | 21.0610 | 1 | 0 |
2-acetylaminofluorene | Homo sapiens (human) | Ki | 7.8980 | 1 | 0 |
phenylephrine | Homo sapiens (human) | Ki | 0.3900 | 1 | 1 |
mepazine | Homo sapiens (human) | IC50 | 1.4560 | 1 | 0 |
mepazine | Homo sapiens (human) | Ki | 0.5460 | 1 | 0 |
yohimbine hydrochloride | Homo sapiens (human) | IC50 | 0.0037 | 1 | 1 |
yohimbine hydrochloride | Homo sapiens (human) | Ki | 0.0018 | 1 | 1 |
cyclizine | Homo sapiens (human) | IC50 | 1.5510 | 1 | 0 |
cyclizine | Homo sapiens (human) | Ki | 0.5820 | 1 | 0 |
ergotamine | Homo sapiens (human) | IC50 | 0.0021 | 1 | 0 |
ergotamine | Homo sapiens (human) | Ki | 0.0008 | 1 | 0 |
methylergonovine | Homo sapiens (human) | IC50 | 1.5900 | 1 | 0 |
methylergonovine | Homo sapiens (human) | Ki | 0.5960 | 1 | 0 |
dibenzothiazyl disulfide | Homo sapiens (human) | IC50 | 0.8990 | 1 | 0 |
dibenzothiazyl disulfide | Homo sapiens (human) | Ki | 0.3370 | 1 | 0 |
benzethonium chloride | Homo sapiens (human) | IC50 | 3.1020 | 1 | 0 |
benzethonium chloride | Homo sapiens (human) | Ki | 1.1630 | 1 | 0 |
sterogenol | Homo sapiens (human) | IC50 | 0.2420 | 1 | 0 |
sterogenol | Homo sapiens (human) | Ki | 0.0910 | 1 | 0 |
yohimbine | Homo sapiens (human) | IC50 | 0.0353 | 6 | 5 |
yohimbine | Homo sapiens (human) | Ki | 0.0129 | 19 | 20 |
indopan | Homo sapiens (human) | Ki | 0.6330 | 1 | 2 |
methysergide | Homo sapiens (human) | IC50 | 1.6310 | 1 | 0 |
methysergide | Homo sapiens (human) | Ki | 0.6110 | 1 | 0 |
emetine | Homo sapiens (human) | IC50 | 0.0380 | 1 | 0 |
emetine | Homo sapiens (human) | Ki | 0.0140 | 1 | 0 |
dihydroergotamine | Homo sapiens (human) | IC50 | 0.0010 | 1 | 0 |
dihydroergotamine | Homo sapiens (human) | Ki | 0.0004 | 1 | 0 |
dimenhydrinate | Homo sapiens (human) | IC50 | 4.3130 | 1 | 0 |
dimenhydrinate | Homo sapiens (human) | Ki | 1.6170 | 1 | 0 |
gentian violet | Homo sapiens (human) | IC50 | 0.5360 | 1 | 0 |
gentian violet | Homo sapiens (human) | Ki | 0.2010 | 1 | 0 |
naphazoline hydrochloride | Homo sapiens (human) | IC50 | 0.0000 | 1 | 1 |
1-naphthylisothiocyanate | Homo sapiens (human) | IC50 | 6.2720 | 1 | 0 |
1-naphthylisothiocyanate | Homo sapiens (human) | Ki | 2.3520 | 1 | 0 |
vancomycin | Homo sapiens (human) | Ki | 0.0501 | 1 | 1 |
4-octylphenol | Homo sapiens (human) | IC50 | 14.2880 | 1 | 0 |
4-octylphenol | Homo sapiens (human) | Ki | 5.3580 | 1 | 0 |
selegiline | Homo sapiens (human) | IC50 | 1.7980 | 1 | 0 |
selegiline | Homo sapiens (human) | Ki | 0.6740 | 1 | 0 |
clemastine | Homo sapiens (human) | IC50 | 0.1830 | 1 | 0 |
clemastine | Homo sapiens (human) | Ki | 0.1194 | 2 | 1 |
danazol | Homo sapiens (human) | IC50 | 18.3280 | 1 | 0 |
danazol | Homo sapiens (human) | Ki | 6.8730 | 1 | 0 |
metergoline | Homo sapiens (human) | IC50 | 0.0580 | 1 | 0 |
metergoline | Homo sapiens (human) | Ki | 0.0220 | 1 | 0 |
lisuride | Homo sapiens (human) | IC50 | 0.0003 | 1 | 0 |
lisuride | Homo sapiens (human) | Ki | 0.0001 | 1 | 0 |
lofexidine | Homo sapiens (human) | Ki | 0.0044 | 1 | 1 |
bromocriptine | Homo sapiens (human) | IC50 | 0.0150 | 1 | 0 |
bromocriptine | Homo sapiens (human) | Ki | 0.0055 | 1 | 0 |
dexchlorpheniramine | Homo sapiens (human) | IC50 | 20.3330 | 1 | 0 |
dexchlorpheniramine | Homo sapiens (human) | Ki | 7.6250 | 1 | 0 |
indoramin | Homo sapiens (human) | Ki | 2.2400 | 1 | 1 |
amitraz | Homo sapiens (human) | IC50 | 0.9269 | 1 | 0 |
amitraz | Homo sapiens (human) | Ki | 0.3476 | 1 | 0 |
st 1059 | Homo sapiens (human) | Ki | 1.4454 | 1 | 1 |
pergolide | Homo sapiens (human) | IC50 | 0.2640 | 1 | 0 |
pergolide | Homo sapiens (human) | Ki | 0.0990 | 1 | 0 |
idazoxan | Homo sapiens (human) | IC50 | 0.0083 | 1 | 1 |
idazoxan | Homo sapiens (human) | Ki | 0.0067 | 4 | 4 |
ipsapirone | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
sertindole | Homo sapiens (human) | Ki | 1.6800 | 1 | 1 |
niguldipine | Homo sapiens (human) | Ki | 0.5875 | 2 | 2 |
ziprasidone | Homo sapiens (human) | Ki | 0.3900 | 2 | 2 |
medetomidine hydrochloride | Homo sapiens (human) | IC50 | 3.3000 | 1 | 1 |
medetomidine | Homo sapiens (human) | IC50 | 3.4000 | 1 | 1 |
sertraline | Homo sapiens (human) | IC50 | 0.2888 | 1 | 0 |
sertraline | Homo sapiens (human) | Ki | 0.1083 | 1 | 0 |
rilmenidine | Homo sapiens (human) | Ki | 0.1721 | 3 | 3 |
atipamezole | Homo sapiens (human) | Ki | 0.0021 | 3 | 3 |
efaroxan | Homo sapiens (human) | Ki | 0.0278 | 2 | 2 |
ergocornine | Homo sapiens (human) | IC50 | 0.0063 | 1 | 0 |
ergocornine | Homo sapiens (human) | Ki | 0.0024 | 1 | 0 |
corynanthine | Homo sapiens (human) | Ki | 1.2180 | 1 | 1 |
gr 127935 | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
rx 821002 | Homo sapiens (human) | Ki | 0.0009 | 2 | 2 |
st 587 | Homo sapiens (human) | Ki | 1.5600 | 1 | 1 |
pramipexole | Homo sapiens (human) | Ki | 0.0757 | 1 | 1 |
mosapride | Homo sapiens (human) | IC50 | 3.6794 | 1 | 0 |
mosapride | Homo sapiens (human) | Ki | 1.3798 | 1 | 0 |
sb 204070a | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
dx 9065 | Homo sapiens (human) | IC50 | 0.0700 | 1 | 1 |
sk&f 104078 | Homo sapiens (human) | Ki | 0.1140 | 2 | 2 |
7,8-dichloro-1,2,3,4-tetrahydroisoquinoline | Homo sapiens (human) | Ki | 3.2705 | 2 | 2 |
sk&f 86466 | Homo sapiens (human) | Ki | 0.0130 | 2 | 2 |
sk&f 104856 | Homo sapiens (human) | Ki | 0.0240 | 1 | 1 |
tamsulosin | Homo sapiens (human) | Ki | 0.0382 | 2 | 2 |
sc 53116 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
sc 53116 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
4-(benzodioxan-5-yl)-1-(indan-2-yl)piperazine | Homo sapiens (human) | Ki | 0.1445 | 1 | 1 |
sonepiprazole | Homo sapiens (human) | Ki | 1.6000 | 1 | 1 |
alpha-ergocryptine | Homo sapiens (human) | IC50 | 0.0079 | 1 | 0 |
alpha-ergocryptine | Homo sapiens (human) | Ki | 0.0030 | 1 | 0 |
n-demethyllysergic acid diethylamide | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
3-fluoronorepinephrine | Homo sapiens (human) | Ki | 0.7000 | 1 | 1 |
nantenine, (+-)-isomer | Homo sapiens (human) | Ki | 1.2880 | 1 | 1 |
maduramicin | Homo sapiens (human) | IC50 | 0.1800 | 1 | 0 |
maduramicin | Homo sapiens (human) | Ki | 0.0670 | 1 | 0 |
latrepirdine | Homo sapiens (human) | Ki | 0.1096 | 1 | 1 |
fipamezole | Homo sapiens (human) | Ki | 0.0072 | 1 | 1 |
conessine | Homo sapiens (human) | Ki | 0.6607 | 1 | 1 |
terconazole | Homo sapiens (human) | IC50 | 0.9830 | 1 | 0 |
terconazole | Homo sapiens (human) | Ki | 0.3690 | 1 | 0 |
raubasine | Homo sapiens (human) | Ki | 0.0082 | 1 | 1 |
ergonovine | Homo sapiens (human) | IC50 | 1.6800 | 1 | 0 |
ergonovine | Homo sapiens (human) | Ki | 0.6300 | 1 | 0 |
dihydroergocristine monomesylate | Homo sapiens (human) | IC50 | 0.0020 | 1 | 0 |
dihydroergocristine monomesylate | Homo sapiens (human) | Ki | 0.0007 | 1 | 0 |
diethylstilbestrol | Homo sapiens (human) | IC50 | 14.1270 | 1 | 0 |
diethylstilbestrol | Homo sapiens (human) | Ki | 5.2970 | 1 | 0 |
jp-1302 | Homo sapiens (human) | Ki | 3.2000 | 1 | 1 |
rauwolscine | Homo sapiens (human) | Ki | 0.0022 | 9 | 10 |
(1S,2R)-2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanol | Homo sapiens (human) | IC50 | 2.0232 | 1 | 0 |
(1S,2R)-2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanol | Homo sapiens (human) | Ki | 0.7587 | 1 | 0 |
flunarizine | Homo sapiens (human) | IC50 | 0.5810 | 1 | 0 |
flunarizine | Homo sapiens (human) | Ki | 0.2180 | 1 | 0 |
benztropine | Homo sapiens (human) | IC50 | 0.5440 | 1 | 0 |
benztropine | Homo sapiens (human) | Ki | 0.2040 | 1 | 0 |
cinnarizine | Homo sapiens (human) | IC50 | 0.4440 | 1 | 0 |
cinnarizine | Homo sapiens (human) | Ki | 0.1670 | 1 | 0 |
enclomiphene | Homo sapiens (human) | IC50 | 0.9360 | 1 | 0 |
enclomiphene | Homo sapiens (human) | Ki | 0.3510 | 1 | 0 |
terbinafine | Homo sapiens (human) | IC50 | 5.7029 | 1 | 0 |
terbinafine | Homo sapiens (human) | Ki | 2.1386 | 1 | 0 |
tamoxifen | Homo sapiens (human) | IC50 | 1.9350 | 1 | 0 |
tamoxifen | Homo sapiens (human) | Ki | 0.7260 | 1 | 0 |
mitragynine | Homo sapiens (human) | Ki | 4.7200 | 1 | 1 |
thioperamide | Homo sapiens (human) | Ki | 0.1259 | 1 | 1 |
bp 897 | Homo sapiens (human) | Ki | 0.0028 | 1 | 1 |
vx-745 | Homo sapiens (human) | IC50 | 34.1670 | 1 | 0 |
vx-745 | Homo sapiens (human) | Ki | 12.8130 | 1 | 0 |
2-(2-benzofuranyl)-2-imidazoline | Homo sapiens (human) | Ki | 26.6091 | 2 | 2 |
n-(1-methyl-5-indolyl)-n'-(3-methyl-5-isothiazolyl)urea | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
sb-224289 | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
3-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-1,5-dihydropyrimido[5,4-b]indole-2,4-dione | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
a 61603 | Homo sapiens (human) | Ki | 0.0331 | 1 | 1 |
rutin | Homo sapiens (human) | Ki | 9.3400 | 1 | 1 |
harmine | Homo sapiens (human) | Ki | 6.2700 | 2 | 2 |
montelukast | Homo sapiens (human) | IC50 | 3.9190 | 1 | 0 |
montelukast | Homo sapiens (human) | Ki | 1.4700 | 1 | 0 |
dexmedetomidine | Homo sapiens (human) | Ki | 0.0025 | 1 | 1 |
l 745870 | Homo sapiens (human) | Ki | 0.1700 | 1 | 1 |
cgp 71683 a | Homo sapiens (human) | IC50 | 0.0970 | 1 | 1 |
oxiconazole | Homo sapiens (human) | IC50 | 4.0827 | 1 | 0 |
oxiconazole | Homo sapiens (human) | Ki | 1.5310 | 1 | 0 |
guanabenz | Homo sapiens (human) | IC50 | 0.0410 | 1 | 0 |
guanabenz | Homo sapiens (human) | Ki | 0.0150 | 1 | 0 |
ciproxifan | Homo sapiens (human) | Ki | 0.0427 | 1 | 1 |
jl 13 compound | Homo sapiens (human) | Ki | 0.1800 | 1 | 1 |
dexniguldipine | Homo sapiens (human) | Ki | 0.9000 | 1 | 1 |
vilazodone | Homo sapiens (human) | IC50 | 6.0000 | 1 | 1 |
n-demethylloperamide | Homo sapiens (human) | Ki | 0.0010 | 1 | 1 |
rwj 52353 | Homo sapiens (human) | Ki | 0.2540 | 1 | 1 |
pd 144418 | Homo sapiens (human) | Ki | 8.3176 | 1 | 1 |
abt 866 | Homo sapiens (human) | Ki | 0.1698 | 1 | 1 |
4-(3-(4-chlorophenyl)-3-hydroxypyrrolidin-1-yl)-1-(4-fluorophenyl)butan-1-one | Homo sapiens (human) | Ki | 4.0280 | 1 | 2 |
pnu 96415e | Homo sapiens (human) | Ki | 0.1810 | 1 | 1 |
st 1936 | Homo sapiens (human) | Ki | 0.3000 | 1 | 1 |
n-(4-((4-(dimethylamino)quinazolin-2-yl)amino)cyclohexyl)-3,4-difluorobenzamide hydrochloride | Homo sapiens (human) | IC50 | 0.1820 | 2 | 2 |
4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride | Homo sapiens (human) | Ki | 0.5300 | 1 | 1 |
2-(2-fluoro-5-methylphenyl)-4,5-dihydro-1h-imidazole | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
3-trifluoromethyl-7-bromo-1,2,3,4-tetrahydroisoquinoline | Homo sapiens (human) | Ki | 502.1750 | 2 | 2 |
PB28 | Homo sapiens (human) | Ki | 1.5136 | 1 | 1 |
amd 070 | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
a 803467 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
sp 203 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
srt1720 | Homo sapiens (human) | IC50 | 2.8300 | 1 | 1 |
2-(1-(2-allylphenoxy)ethyl)-4,5-dihydro-1h-imidazole | Homo sapiens (human) | Ki | 0.0575 | 4 | 4 |
nitd 609 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
2-((r-5-chloro-4-methoxymethylindan-1-yl)-1h-imidazole) | Homo sapiens (human) | Ki | 1.7000 | 1 | 1 |
n,n-diallyl-5-methoxytryptamine | Homo sapiens (human) | Ki | 6.7379 | 2 | 3 |
clozapine | Homo sapiens (human) | IC50 | 0.0900 | 1 | 0 |
clozapine | Homo sapiens (human) | Ki | 0.0908 | 5 | 4 |
olanzapine | Homo sapiens (human) | IC50 | 0.5410 | 1 | 0 |
olanzapine | Homo sapiens (human) | Ki | 0.1913 | 4 | 3 |
Drugs with Activation Measurements
Drugs with Other Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
alprenolol | Homo sapiens (human) | Kapp | 0.0200 | 1 | 1 |
bunolol | Homo sapiens (human) | Kapp | 0.0170 | 1 | 1 |
pindolol | Homo sapiens (human) | Kapp | 0.0930 | 1 | 1 |
practolol | Homo sapiens (human) | Kapp | 313.0000 | 1 | 1 |
prazosin | Homo sapiens (human) | EC40 | 1.3000 | 2 | 3 |
propranolol | Homo sapiens (human) | Kapp | 0.0180 | 1 | 1 |
phentolamine | Homo sapiens (human) | Kb | 0.0070 | 1 | 1 |
metergoline | Homo sapiens (human) | Activity | 0.0310 | 1 | 1 |
cannabigerol | Homo sapiens (human) | EC5 | 0.0020 | 1 | 1 |
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[no title available],
Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity.ACS medicinal chemistry letters, , Sep-12, Volume: 4, Issue:9, 2013
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Pyrrolizidine esters and amides as 5-HT4 receptor agonists and antagonists.Journal of medicinal chemistry, , Feb-09, Volume: 49, Issue:3, 2006
Azaadamantane benzamide 5-HT4 agonists: gastrointestinal prokinetic SC-54750.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 14, Issue:22, 2004
[no title available],
A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin.Bioorganic & medicinal chemistry, , 07-15, Volume: 24, Issue:14, 2016
Transfer of SAR information from hypotensive indazole to indole derivatives acting at α-adrenergic receptors: In vitro and in vivo studies.European journal of medicinal chemistry, , Jun-10, Volume: 115, 2016
Synthesis and biological evaluation of 2-aryliminopyrrolidines as selective ligands for I1 imidazoline receptors: discovery of new sympatho-inhibitory hypotensive agents with potential beneficial effects in metabolic syndrome.Journal of medicinal chemistry, , Jan-22, Volume: 58, Issue:2, 2015
Synthesis and biological activities of 2-[(heteroaryl)methyl]imidazolines.Bioorganic & medicinal chemistry, , Jan-01, Volume: 20, Issue:1, 2012
Methylation of imidazoline related compounds leads to loss of α₂-adrenoceptor affinity. Synthesis and biological evaluation of selective I₁ imidazoline receptor ligands.Bioorganic & medicinal chemistry, , Aug-01, Volume: 20, Issue:15, 2012
3-[(Imidazolidin-2-yl)imino]indazole ligands with selectivity for the α(2)-adrenoceptor compared to the imidazoline I(1) receptor.Bioorganic & medicinal chemistry, , Jan-01, Volume: 19, Issue:1, 2011
Fruitful adrenergic α(2C)-agonism/α(2A)-antagonism combination to prevent and contrast morphine tolerance and dependence.Journal of medicinal chemistry, , Nov-11, Volume: 53, Issue:21, 2010
alpha(2) Adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-Imidazo)-1,3-dimethyl-6,7-dihydrothianaphthene [corrected] as a high-affinity ligand for the alpha(2D) adrenergic receptor.Journal of medicinal chemistry, , Mar-09, Volume: 43, Issue:5, 2000
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Synthesis and evaluation of 2-[(5-methylbenz-1-ox-4-azin-6-yl)imino]imidazoline, a potent, peripherally acting alpha 2 adrenoceptor agonist.Journal of medicinal chemistry, , Aug-30, Volume: 39, Issue:18, 1996
2H-[1]benzopyrano[3,4-b]pyridines: synthesis and activity at central monoamine receptors.Journal of medicinal chemistry, , Volume: 32, Issue:3, 1989
Radioiodinated p-iodoclonidine: a high-affinity probe for the alpha 2-adrenergic receptor.Journal of medicinal chemistry, , Volume: 30, Issue:7, 1987
[no title available],
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Synthesis and structure-activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: a novel series of 5-HT(2A/2C) receptor antagonists. Part 1.Bioorganic & medicinal chemistry letters, , Jan-21, Volume: 12, Issue:2, 2002
Development of predictive retention-activity relationship models of tricyclic antidepressants by micellar liquid chromatography.Journal of medicinal chemistry, , Aug-12, Volume: 42, Issue:16, 1999
[no title available],
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
New 2-substituted 1,2,3,4-tetrahydrobenzofuro[3,2-c]pyridine having highly active and potent central alpha 2-antagonistic activity as potential antidepressants.Bioorganic & medicinal chemistry letters, , Jan-03, Volume: 10, Issue:1, 2000
The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 24, Issue:2, 2014
2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: the discovery of alpha1a subtype selective 2'-alkylsulfonyl-substituted analogues.Journal of medicinal chemistry, , May-23, Volume: 45, Issue:11, 2002
Benzylimidazolines as h5-HT1B/1D serotonin receptor ligands: a structure-affinity investigation.Journal of medicinal chemistry, , Jun-18, Volume: 41, Issue:13, 1998
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.Journal of medicinal chemistry, , Sep-01, Volume: 38, Issue:18, 1995
[no title available],
Synthesis and biological evaluation of 2-aryliminopyrrolidines as selective ligands for I1 imidazoline receptors: discovery of new sympatho-inhibitory hypotensive agents with potential beneficial effects in metabolic syndrome.Journal of medicinal chemistry, , Jan-22, Volume: 58, Issue:2, 2015
Synthesis and pharmacologic evaluation of 2-endo-amino-3-exo-isopropylbicyclo[2.2.1]heptane: a potent imidazoline1 receptor specific agent.Journal of medicinal chemistry, , Mar-15, Volume: 39, Issue:6, 1996
Discovery of alpha 1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine.Journal of medicinal chemistry, , May-12, Volume: 38, Issue:10, 1995
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.Journal of medicinal chemistry, , Sep-01, Volume: 38, Issue:18, 1995
2,4-diamino-6,7-dimethoxyquinazolines. 1. 2-[4-(1,4-benzodioxan-2-ylcarbonyl)piperazin-1-yl] derivatives as alpha 1-adrenoceptor antagonists and antihypertensive agents.Journal of medicinal chemistry, , Volume: 30, Issue:1, 1987
2,4-Diamino-6,7-dimethoxyquinazolines. 2. 2-(4-Carbamoylpiperidino) derivatives as alpha 1-adrenoceptor antagonists and antihypertensive agents.Journal of medicinal chemistry, , Volume: 30, Issue:6, 1987
[no title available],
Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example.Journal of medicinal chemistry, , Dec-10, Volume: 58, Issue:23, 2015
Arylethanolamines derived from salicylamide with alpha- and beta-adrenoceptor blocking activities. Preparation of labetalol, its enantiomers, and related salicylamides.Journal of medicinal chemistry, , Volume: 25, Issue:6, 1982
Cardioselectivity of beta-adrenoceptor blocking agents 1. 1-[(4-Hydroxyphenethyl)amino]-3-(aryloxy)propan-2-ols.Journal of medicinal chemistry, , Volume: 22, Issue:6, 1979
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
[no title available],
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.Bioorganic & medicinal chemistry letters, , 10-15, Volume: 30, Issue:20, 2020
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
[no title available],
Exploring the active site of phenylethanolamine N-methyltransferase with 3-hydroxyethyl- and 3-hydroxypropyl-7-substituted-1,2,3,4-tetrahydroisoquinolines.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 15, Issue:4, 2005
Inhibitors of phenylethanolamine N-methyltransferase devoid of alpha2-adrenoceptor affinity.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 15, Issue:23, 2005
Molecular recognition of sub-micromolar inhibitors by the epinephrine-synthesizing enzyme phenylethanolamine N-methyltransferase.Journal of medicinal chemistry, , Jan-01, Volume: 47, Issue:1, 2004
Identification of a dihydropyridine as a potent alpha1a adrenoceptor-selective antagonist that inhibits phenylephrine-induced contraction of the human prostate.Journal of medicinal chemistry, , Jul-02, Volume: 41, Issue:14, 1998
Synthesis and pharmacological characterization of 3-[2-((3aR,9bR)-cis-6-methoxy-2,3,3a,4,5,9b-hexahydro-1H-benz[e] isoindol-2-yl)ethyl]pyrido-[3',4':4,5]thieno[3,2-d]pyrimidine-2,4 (1H,3H)-dione (A-131701): a uroselective alpha 1A adrenoceptor antagonist Journal of medicinal chemistry, , Sep-26, Volume: 40, Issue:20, 1997
Discovery of alpha 1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine.Journal of medicinal chemistry, , May-12, Volume: 38, Issue:10, 1995
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.Journal of medicinal chemistry, , Sep-01, Volume: 38, Issue:18, 1995
[no title available],
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.Journal of medicinal chemistry, , Sep-01, Volume: 38, Issue:18, 1995
Absolute configuration of glycerol derivatives. 7. Enantiomers of 2-[[[2-(2,6-dimethoxyphenoxy)ethyl]amino]methyl]-1,4-benzodioxane (WB-4101), a potent competitive alpha-adrenergic antagonist.Journal of medicinal chemistry, , Volume: 22, Issue:9, 1979
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
Bioisosteric phentolamine analogs as potent alpha-adrenergic antagonists.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 15, Issue:21, 2005
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.Journal of medicinal chemistry, , Sep-01, Volume: 38, Issue:18, 1995
The role of receptor binding in drug discovery.Journal of natural products, , Volume: 56, Issue:4, 1993
Development of an affinity ligand for purification of alpha 2-adrenoceptors from human platelet membranes.Journal of medicinal chemistry, , Volume: 27, Issue:7, 1984
6-Chloro-2,3,4,5-tetrahydro-3-methyl-1H-3-benzazepine: a potent and selective antagonist of alpha 2-adrenoceptors.Journal of medicinal chemistry, , Volume: 26, Issue:9, 1983
Arylethanolamines derived from salicylamide with alpha- and beta-adrenoceptor blocking activities. Preparation of labetalol, its enantiomers, and related salicylamides.Journal of medicinal chemistry, , Volume: 25, Issue:6, 1982
[no title available],
Further studies on arylpiperazinyl alkyl pyridazinones: discovery of an exceptionally potent, orally active, antinociceptive agent in thermally induced pain.Journal of medicinal chemistry, , Dec-10, Volume: 52, Issue:23, 2009
Novel 4-(6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolin-2-yl)methylbenzofuran derivatives as selective alpha(2C)-adrenergic receptor antagonists.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 17, Issue:6, 2007
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.Journal of medicinal chemistry, , 01-09, Volume: 63, Issue:1, 2020
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 23, Issue:6, 2013
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.Bioorganic & medicinal chemistry, , May-15, Volume: 21, Issue:10, 2013
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.European journal of medicinal chemistry, , Volume: 63, 2013
Alkaloids from Eschscholzia californica and their capacity to inhibit binding of [3H]8-Hydroxy-2-(di-N-propylamino)tetralin to 5-HT1A receptors in Vitro.Journal of natural products, , Volume: 69, Issue:3, 2006
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
Synthesis and biological studies of yohimbine derivatives on human alpha2C-adrenergic receptors.Bioorganic & medicinal chemistry letters, , Jun-02, Volume: 15, Issue:11, 2005
Yohimbine dimers exhibiting binding selectivities for human alpha2a- versus alpha2b-adrenergic receptors.Bioorganic & medicinal chemistry letters, , Apr-03, Volume: 10, Issue:7, 2000
A series of 6- and 7-piperazinyl- and -piperidinylmethylbenzoxazinones with dopamine D4 antagonist activity: discovery of a potential atypical antipsychotic agent.Journal of medicinal chemistry, , Dec-16, Volume: 42, Issue:25, 1999
Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.Journal of medicinal chemistry, , Sep-15, Volume: 38, Issue:19, 1995
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.Journal of medicinal chemistry, , Sep-01, Volume: 38, Issue:18, 1995
Radioiodinated p-iodoclonidine: a high-affinity probe for the alpha 2-adrenergic receptor.Journal of medicinal chemistry, , Volume: 30, Issue:7, 1987
[no title available],
Benzofuranyl-2-imidazoles as imidazoline IEuropean journal of medicinal chemistry, , Oct-15, Volume: 222, 2021
Favourable involvement of α2A-adrenoreceptor antagonism in the I₂-imidazoline binding sites-mediated morphine analgesia enhancement.Bioorganic & medicinal chemistry, , Apr-01, Volume: 20, Issue:7, 2012
Alpha2-adrenoreceptors profile modulation. 4. From antagonist to agonist behavior.Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 2008
Novel 4-(6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolin-2-yl)methylbenzofuran derivatives as selective alpha(2C)-adrenergic receptor antagonists.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 17, Issue:6, 2007
New 2-substituted 1,2,3,4-tetrahydrobenzofuro[3,2-c]pyridine having highly active and potent central alpha 2-antagonistic activity as potential antidepressants.Bioorganic & medicinal chemistry letters, , Jan-03, Volume: 10, Issue:1, 2000
Discovery of alpha 1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine.Journal of medicinal chemistry, , May-12, Volume: 38, Issue:10, 1995
Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.Journal of medicinal chemistry, , Sep-15, Volume: 38, Issue:19, 1995
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin.Bioorganic & medicinal chemistry, , 07-15, Volume: 24, Issue:14, 2016
Synthesis and biological evaluation of 2-aryliminopyrrolidines as selective ligands for I1 imidazoline receptors: discovery of new sympatho-inhibitory hypotensive agents with potential beneficial effects in metabolic syndrome.Journal of medicinal chemistry, , Jan-22, Volume: 58, Issue:2, 2015
Methylation of imidazoline related compounds leads to loss of α₂-adrenoceptor affinity. Synthesis and biological evaluation of selective I₁ imidazoline receptor ligands.Bioorganic & medicinal chemistry, , Aug-01, Volume: 20, Issue:15, 2012
A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin.Bioorganic & medicinal chemistry, , 07-15, Volume: 24, Issue:14, 2016
Rigid analogues of the α2-adrenergic blocker atipamezole: small changes, big consequences.Journal of medicinal chemistry, , Oct-14, Volume: 53, Issue:19, 2010
Potential antidepressants displayed combined alpha(2)-adrenoceptor antagonist and monoamine uptake inhibitor properties.Journal of medicinal chemistry, , Mar-01, Volume: 44, Issue:5, 2001
A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin.Bioorganic & medicinal chemistry, , 07-15, Volume: 24, Issue:14, 2016
Imidazoline binding sites (IBS) profile modulation: key role of the bridge in determining I1-IBS or I2-IBS selectivity within a series of 2-phenoxymethylimidazoline analogues.Journal of medicinal chemistry, , May-22, Volume: 46, Issue:11, 2003
[no title available]European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
Substituted conformationally restricted guanidine derivatives: Probing the α2-adrenoceptors' binding pocket.European journal of medicinal chemistry, , Nov-10, Volume: 123, 2016
Alpha2-adrenoreceptors profile modulation. 4. From antagonist to agonist behavior.Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 2008
Design, synthesis, and structure-activity relationships of a new series of alpha-adrenergic agonists: spiro[(1,3-diazacyclopent-1-ene)-5,2'-(1',2',3',4'- tetrahydronaphthalene)].Journal of medicinal chemistry, , Sep-29, Volume: 38, Issue:20, 1995
Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: a novel, potent and orally active direct inhibitor of factor Xa.Bioorganic & medicinal chemistry, , Feb-01, Volume: 17, Issue:3, 2009
Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.Journal of medicinal chemistry, , Sep-15, Volume: 38, Issue:19, 1995
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.Journal of medicinal chemistry, , Sep-01, Volume: 38, Issue:18, 1995
Exploring the active site of phenylethanolamine N-methyltransferase with 3-hydroxyethyl- and 3-hydroxypropyl-7-substituted-1,2,3,4-tetrahydroisoquinolines.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 15, Issue:4, 2005
Inhibitors of phenylethanolamine N-methyltransferase devoid of alpha2-adrenoceptor affinity.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 15, Issue:23, 2005
Design, synthesis, and structure-activity relationships of phthalimide-phenylpiperazines: a novel series of potent and selective alpha(1)(a)-adrenergic receptor antagonists.Journal of medicinal chemistry, , Jun-01, Volume: 43, Issue:11, 2000
Synthesis and pharmacological characterization of 3-[2-((3aR,9bR)-cis-6-methoxy-2,3,3a,4,5,9b-hexahydro-1H-benz[e] isoindol-2-yl)ethyl]pyrido-[3',4':4,5]thieno[3,2-d]pyrimidine-2,4 (1H,3H)-dione (A-131701): a uroselective alpha 1A adrenoceptor antagonist Journal of medicinal chemistry, , Sep-26, Volume: 40, Issue:20, 1997
Pyrrolizidine esters and amides as 5-HT4 receptor agonists and antagonists.Journal of medicinal chemistry, , Feb-09, Volume: 49, Issue:3, 2006
Bridgehead-methyl analog of SC-53116 as a 5-HT4 agonist.Bioorganic & medicinal chemistry letters, , Jun-21, Volume: 14, Issue:12, 2004
Return of DJournal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.Journal of medicinal chemistry, , Sep-15, Volume: 38, Issue:19, 1995
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.Journal of medicinal chemistry, , Sep-01, Volume: 38, Issue:18, 1995
The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function bJournal of medicinal chemistry, , Apr-09, Volume: 41, Issue:8, 1998
A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin.Bioorganic & medicinal chemistry, , 07-15, Volume: 24, Issue:14, 2016
3-[(Imidazolidin-2-yl)imino]indazole ligands with selectivity for the α(2)-adrenoceptor compared to the imidazoline I(1) receptor.Bioorganic & medicinal chemistry, , Jan-01, Volume: 19, Issue:1, 2011
[no title available],
Return of DJournal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Novel 2-imidazoles as potent and selective alpha1A adrenoceptor partial agonists.Bioorganic & medicinal chemistry letters, , May-01, Volume: 18, Issue:9, 2008
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.Journal of medicinal chemistry, , Jun-03, Volume: 47, Issue:12, 2004
Return of DJournal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: in vitro profiling and in vivo evaluation.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 19, Issue:21, 2009
Lead optimization of 4-(dimethylamino)quinazolines, potent and selective antagonists for the melanin-concentrating hormone receptor 1.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 15, Issue:17, 2005
Exploring the active site of phenylethanolamine N-methyltransferase with 3-hydroxyethyl- and 3-hydroxypropyl-7-substituted-1,2,3,4-tetrahydroisoquinolines.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 15, Issue:4, 2005
Inhibitors of phenylethanolamine N-methyltransferase devoid of alpha2-adrenoceptor affinity.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 15, Issue:23, 2005
Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity.ACS medicinal chemistry letters, , Sep-12, Volume: 4, Issue:9, 2013
Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect.ACS medicinal chemistry letters, , Jul-12, Volume: 3, Issue:7, 2012
Fruitful adrenergic α(2C)-agonism/α(2A)-antagonism combination to prevent and contrast morphine tolerance and dependence.Journal of medicinal chemistry, , Nov-11, Volume: 53, Issue:21, 2010
Alpha2-adrenoreceptors profile modulation. 4. From antagonist to agonist behavior.Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 2008
Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 26, Issue:3, 2016
An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: emerging 'Novel Psychoactive Drugs'.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
New pyridobenzoxazepine derivatives derived from 5-(4-methylpiperazin-1-yl)-8-chloro-pyrido[2,3-b][1,5]benzoxazepine (JL13): chemical synthesis and pharmacological evaluation.Journal of medicinal chemistry, , Feb-23, Volume: 55, Issue:4, 2012
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
[no title available],
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
[no title available],
Enables
This protein enables 11 target(s):
Target | Category | Definition |
alpha2-adrenergic receptor activity | molecular function | Combining with epinephrine or norepinephrine to initiate a change in cell activity via activation of a G protein, with pharmacological characteristics of alpha2-adrenergic receptors; the activity involves transmitting the signal to the Gi alpha subunit of a heterotrimeric G protein. [GOC:cb, GOC:mah, IUPHAR_GPCR:1274] |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
protein kinase binding | molecular function | Binding to a protein kinase, any enzyme that catalyzes the transfer of a phosphate group, usually from ATP, to a protein substrate. [GOC:jl] |
alpha-1B adrenergic receptor binding | molecular function | Binding to an alpha-1B adrenergic receptor. [GOC:mah, GOC:nln] |
alpha-2C adrenergic receptor binding | molecular function | Binding to an alpha-2C adrenergic receptor. [GOC:mah, GOC:nln] |
thioesterase binding | molecular function | Binding to a thioesterase. [GOC:dl] |
heterotrimeric G-protein binding | molecular function | Binding to a heterotrimeric G-protein. [GOC:nln] |
protein homodimerization activity | molecular function | Binding to an identical protein to form a homodimer. [GOC:jl] |
protein heterodimerization activity | molecular function | Binding to a nonidentical protein to form a heterodimer. [GOC:ai] |
epinephrine binding | molecular function | Binding to epinephrine, a hormone produced by the medulla of the adrenal glands that increases heart activity, improves the power and prolongs the action of muscles, and increases the rate and depth of breathing. It is synthesized by the methylation of norepinephrine. [GOC:ai] |
norepinephrine binding | molecular function | Binding to norepinephrine, (3,4-dihydroxyphenyl-2-aminoethanol), a hormone secreted by the adrenal medulla and a neurotransmitter in the sympathetic peripheral nervous system and in some tracts of the CNS. It is also the biosynthetic precursor of epinephrine. [GOC:ai] |
Located In
This protein is located in 10 target(s):
Target | Category | Definition |
cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
basolateral plasma membrane | cellular component | The region of the plasma membrane that includes the basal end and sides of the cell. Often used in reference to animal polarized epithelial membranes, where the basal membrane is the part attached to the extracellular matrix, or in plant cells, where the basal membrane is defined with respect to the zygotic axis. [GOC:go_curators] |
neuronal cell body | cellular component | The portion of a neuron that includes the nucleus, but excludes cell projections such as axons and dendrites. [GOC:go_curators] |
axon terminus | cellular component | Terminal inflated portion of the axon, containing the specialized apparatus necessary to release neurotransmitters. The axon terminus is considered to be the whole region of thickening and the terminal button is a specialized region of it. [GOC:dph, GOC:jl] |
presynaptic active zone membrane | cellular component | The membrane portion of the presynaptic active zone; it is the site where docking and fusion of synaptic vesicles occurs for the release of neurotransmitters. [PMID:12812759, PMID:12923177, PMID:3152289] |
dopaminergic synapse | cellular component | A synapse that uses dopamine as a neurotransmitter. [GOC:dos] |
postsynaptic density membrane | cellular component | The membrane component of the postsynaptic density. This is the region of the postsynaptic membrane in which the population of neurotransmitter receptors involved in synaptic transmission are concentrated. [GOC:dos] |
glutamatergic synapse | cellular component | A synapse that uses glutamate as a neurotransmitter. [GOC:dos] |
GABA-ergic synapse | cellular component | A synapse that uses GABA as a neurotransmitter. These synapses are typically inhibitory. [GOC:dos] |
Active In
This protein is active in 1 target(s):
Target | Category | Definition |
plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Part Of
This protein is part of 1 target(s):
Target | Category | Definition |
receptor complex | cellular component | Any protein complex that undergoes combination with a hormone, neurotransmitter, drug or intracellular messenger to initiate a change in cell function. [GOC:go_curators] |
Involved In
This protein is involved in 42 target(s):
Target | Category | Definition |
positive regulation of cytokine production | biological process | Any process that activates or increases the frequency, rate or extent of production of a cytokine. [GOC:add, ISBN:0781735149] |
DNA replication | biological process | The cellular metabolic process in which a cell duplicates one or more molecules of DNA. DNA replication begins when specific sequences, known as origins of replication, are recognized and bound by the origin recognition complex, and ends when the original DNA molecule has been completely duplicated and the copies topologically separated. The unit of replication usually corresponds to the genome of the cell, an organelle, or a virus. The template for replication can either be an existing DNA molecule or RNA. [GOC:mah] |
G protein-coupled receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor] |
adenylate cyclase-activating G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation of adenylyl cyclase activity which results in an increase in the intracellular concentration of cyclic AMP (cAMP). This pathway is negatively regulated by phosphodiesterase, which cleaves cAMP and terminates the signaling. [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194] |
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the inhibition of adenylyl cyclase activity and a subsequent decrease in the intracellular concentration of cyclic AMP (cAMP). [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194] |
Ras protein signal transduction | biological process | An intracellular signaling cassette in which a small monomeric GTPase of the Ras subfamily relays a signal. [GOC:bf] |
Rho protein signal transduction | biological process | An intracellular signaling cassette in which a small monomeric GTPase of the Rho subfamily relays a signal. [GOC:bf] |
female pregnancy | biological process | The set of physiological processes that allow an embryo or foetus to develop within the body of a female animal. It covers the time from fertilization of a female ovum by a male spermatozoon until birth. [ISBN:0192800825] |
positive regulation of cell population proliferation | biological process | Any process that activates or increases the rate or extent of cell proliferation. [GOC:go_curators] |
negative regulation of norepinephrine secretion | biological process | Any process that decreases the frequency, rate or extent of the regulated release of norepinephrine. [GOC:dph, GOC:tb] |
regulation of vasoconstriction | biological process | Any process that modulates the frequency, rate or extent of reductions in the diameter of blood vessels. [GOC:jl] |
actin cytoskeleton organization | biological process | A process that is carried out at the cellular level which results in the assembly, arrangement of constituent parts, or disassembly of cytoskeletal structures comprising actin filaments and their associated proteins. [GOC:dph, GOC:jl, GOC:mah] |
platelet activation | biological process | A series of progressive, overlapping events triggered by exposure of the platelets to subendothelial tissue. These events include shape change, adhesiveness, aggregation, and release reactions. When carried through to completion, these events lead to the formation of a stable hemostatic plug. [http://www.graylab.ac.uk/omd/] |
positive regulation of cell migration | biological process | Any process that activates or increases the frequency, rate or extent of cell migration. [GOC:go_curators] |
activation of protein kinase activity | biological process | Any process that initiates the activity of an inactive protein kinase. [GOC:mah] |
activation of protein kinase B activity | biological process | Any process that initiates the activity of the inactive enzyme protein kinase B. [GOC:pg] |
negative regulation of epinephrine secretion | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the regulated release of epinephrine. [GOC:vk] |
cellular response to hormone stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a hormone stimulus. [GOC:mah] |
receptor transactivation | biological process | The process in which a receptor is activated by another receptor. Receptor transactivation can occur through different mechanisms and includes cross-talk between signaling pathways where one receptor activates a receptor for a different ligand, and also activation of subunits within a receptor oligomer. [GOC:al, GOC:bf, GOC:BHF, PMID:16870826, PMID:21063387] |
vasodilation | biological process | An increase in the internal diameter of blood vessels, especially arterioles or capillaries, due to relaxation of smooth muscle cells that line the vessels, and usually resulting in a decrease in blood pressure. [GOC:pr, ISBN:0192800981] |
glucose homeostasis | biological process | Any process involved in the maintenance of an internal steady state of glucose within an organism or cell. [GOC:go_curators] |
fear response | biological process | The response of an organism to a perceived external threat. [GOC:go_curators] |
positive regulation of potassium ion transport | biological process | Any process that activates or increases the frequency, rate or extent of the directed movement of potassium ions (K+) into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:jl] |
positive regulation of MAP kinase activity | biological process | Any process that activates or increases the frequency, rate or extent of MAP kinase activity. [GOC:dph, GOC:go_curators] |
positive regulation of MAPK cascade | biological process | Any process that activates or increases the frequency, rate or extent of signal transduction mediated by the MAPK cascade. [GOC:go_curators] |
positive regulation of epidermal growth factor receptor signaling pathway | biological process | Any process that activates or increases the frequency, rate or extent of epidermal growth factor receptor signaling pathway activity. [GOC:go_curators] |
negative regulation of calcium ion-dependent exocytosis | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of calcium ion-dependent exocytosis. [GOC:go_curators] |
negative regulation of insulin secretion | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the regulated release of insulin. [GOC:ai] |
intestinal absorption | biological process | A process in which nutrients are taken up from the contents of the intestine. [GOC:ai, GOC:dph] |
thermoception | biological process | The series of events required for an organism to receive a temperature stimulus, convert it to a molecular signal, and recognize and characterize the signal. Thermoception in larger animals is mainly done in the skin; mammals have at least two types of sensor, for detecting heat (temperatures above body temperature) and cold (temperatures below body temperature). [GOC:ai, Wikipedia:Thermoception] |
negative regulation of lipid catabolic process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the chemical reactions and pathways resulting in the breakdown of lipids. [GOC:ai] |
positive regulation of membrane protein ectodomain proteolysis | biological process | Any process that activates or increases the frequency, rate or extent of membrane protein ectodomain peptidolysis. [GOC:ai] |
negative regulation of calcium ion transport | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the directed movement of calcium ions into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:ai] |
negative regulation of insulin secretion involved in cellular response to glucose stimulus | biological process | Any process that decreases the frequency, rate or extent of the regulated release of insulin that contributes to the response of a cell to glucose. [GOC:BHF, GOC:dph] |
negative regulation of uterine smooth muscle contraction | biological process | Any process that decreases the frequency, rate or extent of uterine smooth muscle contraction. [GOC:go_curators] |
adrenergic receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by a ligand binding to an adrenergic receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process. [GOC:BHF] |
adenylate cyclase-activating adrenergic receptor signaling pathway | biological process | An adenylate cyclase-activating G protein-coupled receptor signaling pathway initiated by a ligand binding to an adrenergic receptor on the surface of the target cell, and ending with the regulation of a downstream cellular process. [GOC:BHF, GOC:mah, GOC:signaling] |
adenylate cyclase-inhibiting adrenergic receptor signaling pathway | biological process | An adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway initiated by a ligand binding to an adrenergic receptor, and ending with the regulation of a downstream cellular process. [GOC:BHF, GOC:mah, GOC:signaling] |
phospholipase C-activating adrenergic receptor signaling pathway | biological process | A phospholipase C-activating receptor G protein-coupled receptor signaling pathway initiated by ligand binding to an adrenergic receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:BHF, GOC:mah, GOC:signaling] |
positive regulation of wound healing | biological process | Any process that increases the rate, frequency, or extent of the series of events that restore integrity to a damaged tissue, following an injury. [GOC:BHF] |
presynaptic modulation of chemical synaptic transmission | biological process | Any process, acting in the presynapse that results in modulation of chemical synaptic transmission. [GOC:dos] |
negative regulation of calcium ion transmembrane transporter activity | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of calcium ion transmembrane transporter activity. [GOC:BHF, GOC:TermGenie] |