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Alpha-2a adrenergic receptor Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
YohimbineIC503.67 [1], 8.4 [2]
YohimbineKi3.1 [1], 7.5 [2]
TerazosinKi549.54 [1], 550.0 [2], 1500.0 [3], 3702.0 [4], 5187.0 [5]
ClozapineKi24.0 [1], 34.0 [2], 185.0 [3], 1000.0 [4]
PhentolamineKi1.7 [1], 2.25 [2], 2.6 [3], 55.9 [4]
IdazoxanIC508.32 [1]
IdazoxanKi7.08 [1], 8.0 [2]
2-[1-(2-Prop-2-enylphenoxy)ethyl]-4,5-dihydro-1H-imidazoleKi57.54 [1]
Methyl 5-[3-(4,4-diphenylpiperidin-1-yl)propylcarbamoyl]-2,6-dimethyl-4-(4-nitrophenyl)-1,4-dihydropyridine-3-carboxylateKi1200.0 [1], 1202.26 [2], 2417.0 [3], 3300.0 [4]
2-[1-(2-Biphenylyloxy)ethyl]-2-imidazolineKi47.86 [1]
(3R,3As)-7,8-dimethoxy-3-[[4-[(E)-2-methyl-3-phenylprop-2-enyl]piperazin-1-yl]methyl]-3a,4-dihydro-3H-chromeno[4,3-c][1,2]oxazoleKi0.3 [1], 0.8 [2]
(3R,3As)-7,8-dimethoxy-3-[[4-[(E)-3-phenylbut-2-enyl]piperazin-1-yl]methyl]-3a,4-dihydro-3H-chromeno[4,3-c][1,2]oxazoleKi0.3 [1], 1.4 [2]
RisperidoneKi3.63 [1], 10.0 [2], 1000.0 [3]
OlanzapineKi192.0 [1], 203.0 [2], 1000.0 [3]
PrazosinKi210.0 [1], 989.0 [2], 2133.0 [3]
MianserinIC5020.89 [1]
MianserinKi4.8 [1], 16.0 [2]
BrimonidineKi2.7 [1], 6.76 [2], 112.0 [3]
OxymetazolineKi0.29 [1], 8.64 [2], 16.22 [3]
RilmenidineKi36.31 [1], 181.97 [2], 300.0 [3]
AtipamezoleKi1.2 [1], 1.86 [2], 3.16 [3]
N,N-Dimethyl-1-(3-oxa-2-azatetracyclo[12.4.0.02,6.07,12]octadeca-1(18),7,9,11,14,16-hexaen-4-yl)methanamineIC50371.54 [1]
3-[2-[1-(4,5-Dihydro-1H-imidazol-2-yl)ethoxy]phenyl]phenolKi27.54 [1]
2-[1-[2-(3-Nitrophenyl)phenoxy]ethyl]-4,5-dihydro-1H-imidazoleKi60.26 [1]
(3R,3As)-7,8-dimethoxy-3-[[4-[(E)-3-phenylprop-2-enyl]piperazin-1-yl]methyl]-3a,4-dihydro-3H-chromeno[4,3-c][1,2]oxazoleKi2.6 [1], 8.8 [2], 25.0 [3]
2-[(1S)-1-(2-Prop-2-enylphenoxy)ethyl]-4,5-dihydro-1H-imidazoleKi52.48 [1]
2-[(1R)-1-(2-Prop-2-enylphenoxy)ethyl]-4,5-dihydro-1H-imidazoleKi100.0 [1]
2-[1-[2-(Cyclopropylmethyl)phenoxy]ethyl]-4,5-dihydro-1H-imidazoleKi36.31 [1]
Unii-G7fms28pydIC501100.0 [1]
Unii-G7fms28pydKi411.0 [1]
N-(4,5-Dihydro-1H-imidazol-2-yl)-5-methylquinoxalin-6-amineKi2.0 [1], 7.24 [2]
(3R,3As)-7,8-dimethoxy-3-[[4-(naphthalen-2-ylmethyl)piperazin-1-yl]methyl]-3a,4-dihydro-3H-chromeno[4,3-c][1,2]oxazoleKi1.3 [1], 5.0 [2]
EpinephrineKi160.0 [1], 276.0 [2]
QuetiapineKi934.3 [1], 1000.0 [2]
MirtazapineIC5085.11 [1]
MirtazapineKi20.0 [1]
TamsulosinKi13.4 [1], 63.0 [2]
ClemastineKi69.0 [1], 169.82 [2]
CirazolineKi58.88 [1]
NiguldipineKi530.0 [1], 645.0 [2]
Unii-22xbk6DY1EKi114.0 [1]
N,N-Diallyl-5-methoxytryptamineKi213.8 [1], 10000.0 [2]
ATC-0175 free baseIC50104.0 [1], 260.0 [2]
1H-Imidazole, 4,5-dihydro-2-(1-phenoxyethyl)-Ki26.92 [1]
Ethanesulfonamide, N-(3-(1H-imidazol-4-ylmethyl)phenyl)-Ki169.82 [1]
2-(1-Benzofuran-6-yl)-N-[[(1R)-5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl]methyl]-N-methylethanamineKi2.4 [1], 2.5 [2]
2-[(1S)-1-(2-Phenylphenoxy)ethyl]-4,5-dihydro-1H-imidazoleKi91.2 [1]
4-(5-Fluoro-2-indanylmethyl)-2-imidazolineKi5.9 [1]
5-N-[3-(4,4-Diphenylpiperidin-1-yl)propyl]-3-N,2,6-trimethyl-4-(4-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxamideKi398.0 [1], 398.11 [2]
2-[(1R)-1-(2-Phenylphenoxy)ethyl]-4,5-dihydro-1H-imidazoleKi186.21 [1]
5-N-[3-(4,4-Diphenylpiperidin-1-yl)propyl]-2,6-dimethyl-4-(4-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxamideKi148.0 [1], 371.54 [2]
1-(17-Chloro-3-oxa-2-azatetracyclo[12.4.0.02,6.07,12]octadeca-1(14),7,9,11,15,17-hexaen-4-yl)-N,N-dimethylmethanamineIC50478.63 [1]
1-Benzyl-4-chroman-2-ylmethyl-piperazineKi146.1 [1], 167.0 [2]
4-Bromo-N-[4-[[4-(dimethylamino)quinazolin-2-yl]amino]cyclohexyl]-2-(trifluoromethoxy)benzenesulfonamideIC5047.0 [1], 57.0 [2]
2-[1-[2-(3-Fluorophenyl)phenoxy]ethyl]-4,5-dihydro-1H-imidazoleKi14.79 [1]
3-[2-[1-(4,5-Dihydro-1H-imidazol-2-yl)ethoxy]phenyl]pyridineKi138.04 [1]
4-Bromo-N-[[4-[[4-(dimethylamino)quinazolin-2-yl]amino]cyclohexyl]methyl]-2-(trifluoromethoxy)benzenesulfonamideIC50110.0 [1], 130.0 [2]
2-N-[1-[4-Bromo-2-(trifluoromethoxy)phenyl]sulfonylpiperidin-4-yl]-4-N,4-N-dimethylquinazoline-2,4-diamineIC50170.0 [1]
2-[1-(2-Thiophen-3-ylphenoxy)ethyl]-4,5-dihydro-1H-imidazoleKi45.71 [1]
(3R,3As)-3-[[4-[(E)-3-(4-fluorophenyl)-2-methylprop-2-enyl]piperazin-1-yl]methyl]-7,8-dimethoxy-3a,4-dihydro-3H-chromeno[4,3-c][1,2]oxazoleKi3.4 [1]
(R)-3-NitrobiphenylineKi81.28 [1]
2-[(1S)-1-[2-(3-Nitrophenyl)phenoxy]ethyl]-4,5-dihydro-1H-imidazoleKi72.44 [1]
(3R,3As)-7,8-dimethoxy-3-[[4-[(Z)-3-phenylprop-2-enyl]piperazin-1-yl]methyl]-3a,4-dihydro-3H-chromeno[4,3-c][1,2]oxazoleKi23.0 [1]
2-[1-(2-Cyclopropylphenoxy)ethyl]-4,5-dihydro-1H-imidazoleKi22.91 [1]
2-[(1S)-1-(2-Cyclopropylphenoxy)ethyl]-4,5-dihydro-1H-imidazoleKi20.89 [1]
2-[(1R)-1-(2-Cyclopropylphenoxy)ethyl]-4,5-dihydro-1H-imidazoleKi44.67 [1]
(8S)-N-[2-(3-Fluorophenyl)ethyl]pentacyclo[5.4.0.02,6.03,10.05,9]undecan-8-amineKi7609.0 [1]
2-(1-(2-Bromophenoxy)ethyl)-4,5-dihydro-1H-imidazoleKi22.91 [1]
2-[1-(2-Cyclopropyloxyphenoxy)ethyl]-4,5-dihydro-1H-imidazoleKi83.18 [1]
2-[(1R)-1-[2-(Cyclopropylmethyl)phenoxy]ethyl]-4,5-dihydro-1H-imidazoleKi44.67 [1]
2-[(1S)-1-[2-(Cyclopropylmethyl)phenoxy]ethyl]-4,5-dihydro-1H-imidazoleKi41.69 [1]
5-Methyl-1,5-diazapentacyclo[10.8.1.02,7.08,21.013,18]henicosa-2(7),8(21),9,11,13,15,17-heptaeneKi407.0 [1], 407.38 [2]
5-O-[3-(4,4-Diphenylpiperidin-1-yl)propyl] 3-O-methyl 2,6-dimethyl-4-(4-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylateKi800.0 [1], 1023.0 [2]
N-[2-[4-[[(3S)-2,3-Dihydro-1,4-benzodioxin-3-yl]methyl]-1,4-diazepan-1-yl]ethyl]-2-phenoxypyridine-3-carboxamideKi94.4 [1], 442.0 [2]
1-((2,3-Dihydrobenzo[b][1,4]dioxin-2-yl)methyl)-4-(2-methoxyphenyl)piperazineKi167.0 [1], 506.0 [2]
N-[2-[4-(2,3-Dihydro-1,4-benzodioxin-3-ylmethyl)-1,4-diazepan-1-yl]ethyl]-2-phenoxypyridine-3-carboxamideKi220.0 [1], 474.0 [2]
2-(3-Cyanophenoxy)-N-[2-[4-(2,3-dihydro-1,4-benzodioxin-3-ylmethyl)-1,4-diazepan-1-yl]ethyl]pyridine-3-carboxamideKi208.0 [1], 501.0 [2]
2-(Tert-butylamino)-N-[2-[4-(2,3-dihydro-1,4-benzodioxin-3-ylmethyl)-1,4-diazepan-1-yl]ethyl]pyridine-3-carboxamideKi138.0 [1], 366.0 [2]
2-Butoxy-N-[2-[4-(2,3-dihydro-1,4-benzodioxin-3-ylmethyl)-1,4-diazepan-1-yl]ethyl]pyridine-3-carboxamideKi73.6 [1], 81.0 [2]
6-Butoxy-N-[2-[4-(2,3-dihydro-1,4-benzodioxin-3-ylmethyl)-1,4-diazepan-1-yl]ethyl]pyridine-2-carboxamideKi48.4 [1], 118.0 [2]
1-(2,3-Dihydro-1,4-benzodioxin-3-ylmethyl)-4-[2-[(2-phenoxypyridin-3-yl)methoxy]ethyl]-1,4-diazepaneKi66.1 [1], 275.0 [2]
5-[[4-(2,3-Dihydro-1,4-benzodioxin-3-ylmethyl)-1,4-diazepan-1-yl]methyl]-3-(2-phenoxypyridin-3-yl)-1,2,4-oxadiazoleKi15.4 [1], 44.8 [2]
4-Bromo-N-[[4-[[[4-(dimethylamino)quinazolin-2-yl]amino]methyl]cyclohexyl]methyl]-2-(trifluoromethoxy)benzenesulfonamideIC507.7 [1]
NorepinephrineKi66.0 [1]
PropranololIC505011.87 [1]
VancomycinKi50.12 [1]
VerapamilKi217.0 [1]
TamoxifenKi726.0 [1]
ChlorpromazineKi132.0 [1]
HaloperidolKi1865.0 [1]
FluoxetineKi6.31 [1]
ChloroquineKi4365.16 [1]
TiclopidineKi143.0 [1]
Clonidine hydrochlorideKi20.89 [1]
AmiodaroneKi117.0 [1]
AmitriptylineKi132.0 [1]
KetoconazoleKi7419.0 [1]
DiethylstilbestrolKi5297.0 [1]
BromocriptineKi5.53 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Alpha-2a adrenergic receptor Inhibitors (IC50, Ki)." AAT Bioquest, Inc.22 Dec2024https://www.aatbio.com/data-sets/alpha-2a-adrenergic-receptor-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024December 22). Quest Database™ Alpha-2a adrenergic receptor Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/alpha-2a-adrenergic-receptor-inhibitors-ic50-ki.
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