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

Structure ▲ ▼	Compound Name ▲ ▼	Standard Type ▲ ▼	Standard Values (in nM) ▲ ▼
	Yohimbine	IC50	3.67 [1], 8.4 [2]
	Yohimbine	Ki	3.1 [1], 7.5 [2]
	Terazosin	Ki	549.54 [1], 550.0 [2], 1500.0 [3], 3702.0 [4], 5187.0 [5]
	Clozapine	Ki	24.0 [1], 34.0 [2], 185.0 [3], 1000.0 [4]
	Phentolamine	Ki	1.7 [1], 2.25 [2], 2.6 [3], 55.9 [4]
	Idazoxan	IC50	8.32 [1]
	Idazoxan	Ki	7.08 [1], 8.0 [2]
	2-[1-(2-Prop-2-enylphenoxy)ethyl]-4,5-dihydro-1H-imidazole	Ki	57.54 [1]
	Methyl 5-[3-(4,4-diphenylpiperidin-1-yl)propylcarbamoyl]-2,6-dimethyl-4-(4-nitrophenyl)-1,4-dihydropyridine-3-carboxylate	Ki	1200.0 [1], 1202.26 [2], 2417.0 [3], 3300.0 [4]
	2-[1-(2-Biphenylyloxy)ethyl]-2-imidazoline	Ki	47.86 [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]oxazole	Ki	0.3 [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]oxazole	Ki	0.3 [1], 1.4 [2]
	Risperidone	Ki	3.63 [1], 10.0 [2], 1000.0 [3]
	Olanzapine	Ki	192.0 [1], 203.0 [2], 1000.0 [3]
	Prazosin	Ki	210.0 [1], 989.0 [2], 2133.0 [3]
	Mianserin	IC50	20.89 [1]
	Mianserin	Ki	4.8 [1], 16.0 [2]
	Brimonidine	Ki	2.7 [1], 6.76 [2], 112.0 [3]
	Oxymetazoline	Ki	0.29 [1], 8.64 [2], 16.22 [3]
	Rilmenidine	Ki	36.31 [1], 181.97 [2], 300.0 [3]
	Atipamezole	Ki	1.2 [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)methanamine	IC50	371.54 [1]
	3-[2-[1-(4,5-Dihydro-1H-imidazol-2-yl)ethoxy]phenyl]phenol	Ki	27.54 [1]
	2-[1-[2-(3-Nitrophenyl)phenoxy]ethyl]-4,5-dihydro-1H-imidazole	Ki	60.26 [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]oxazole	Ki	2.6 [1], 8.8 [2], 25.0 [3]
	2-[(1S)-1-(2-Prop-2-enylphenoxy)ethyl]-4,5-dihydro-1H-imidazole	Ki	52.48 [1]
	2-[(1R)-1-(2-Prop-2-enylphenoxy)ethyl]-4,5-dihydro-1H-imidazole	Ki	100.0 [1]
	2-[1-[2-(Cyclopropylmethyl)phenoxy]ethyl]-4,5-dihydro-1H-imidazole	Ki	36.31 [1]
	Unii-G7fms28pyd	IC50	1100.0 [1]
	Unii-G7fms28pyd	Ki	411.0 [1]
	N-(4,5-Dihydro-1H-imidazol-2-yl)-5-methylquinoxalin-6-amine	Ki	2.0 [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]oxazole	Ki	1.3 [1], 5.0 [2]
	Epinephrine	Ki	160.0 [1], 276.0 [2]
	Quetiapine	Ki	934.3 [1], 1000.0 [2]
	Mirtazapine	IC50	85.11 [1]
	Mirtazapine	Ki	20.0 [1]
	Tamsulosin	Ki	13.4 [1], 63.0 [2]
	Clemastine	Ki	69.0 [1], 169.82 [2]
	Cirazoline	Ki	58.88 [1]
	Niguldipine	Ki	530.0 [1], 645.0 [2]
	Unii-22xbk6DY1E	Ki	114.0 [1]
	N,N-Diallyl-5-methoxytryptamine	Ki	213.8 [1], 10000.0 [2]
	ATC-0175 free base	IC50	104.0 [1], 260.0 [2]
	1H-Imidazole, 4,5-dihydro-2-(1-phenoxyethyl)-	Ki	26.92 [1]
	Ethanesulfonamide, N-(3-(1H-imidazol-4-ylmethyl)phenyl)-	Ki	169.82 [1]
	2-(1-Benzofuran-6-yl)-N-[[(1R)-5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl]methyl]-N-methylethanamine	Ki	2.4 [1], 2.5 [2]
	2-[(1S)-1-(2-Phenylphenoxy)ethyl]-4,5-dihydro-1H-imidazole	Ki	91.2 [1]
	4-(5-Fluoro-2-indanylmethyl)-2-imidazoline	Ki	5.9 [1]
	5-N-[3-(4,4-Diphenylpiperidin-1-yl)propyl]-3-N,2,6-trimethyl-4-(4-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxamide	Ki	398.0 [1], 398.11 [2]
	2-[(1R)-1-(2-Phenylphenoxy)ethyl]-4,5-dihydro-1H-imidazole	Ki	186.21 [1]
	5-N-[3-(4,4-Diphenylpiperidin-1-yl)propyl]-2,6-dimethyl-4-(4-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxamide	Ki	148.0 [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-dimethylmethanamine	IC50	478.63 [1]
	1-Benzyl-4-chroman-2-ylmethyl-piperazine	Ki	146.1 [1], 167.0 [2]
	4-Bromo-N-[4-[[4-(dimethylamino)quinazolin-2-yl]amino]cyclohexyl]-2-(trifluoromethoxy)benzenesulfonamide	IC50	47.0 [1], 57.0 [2]
	2-[1-[2-(3-Fluorophenyl)phenoxy]ethyl]-4,5-dihydro-1H-imidazole	Ki	14.79 [1]
	3-[2-[1-(4,5-Dihydro-1H-imidazol-2-yl)ethoxy]phenyl]pyridine	Ki	138.04 [1]
	4-Bromo-N-[[4-[[4-(dimethylamino)quinazolin-2-yl]amino]cyclohexyl]methyl]-2-(trifluoromethoxy)benzenesulfonamide	IC50	110.0 [1], 130.0 [2]
	2-N-[1-[4-Bromo-2-(trifluoromethoxy)phenyl]sulfonylpiperidin-4-yl]-4-N,4-N-dimethylquinazoline-2,4-diamine	IC50	170.0 [1]
	2-[1-(2-Thiophen-3-ylphenoxy)ethyl]-4,5-dihydro-1H-imidazole	Ki	45.71 [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]oxazole	Ki	3.4 [1]
	(R)-3-Nitrobiphenyline	Ki	81.28 [1]
	2-[(1S)-1-[2-(3-Nitrophenyl)phenoxy]ethyl]-4,5-dihydro-1H-imidazole	Ki	72.44 [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]oxazole	Ki	23.0 [1]
	2-[1-(2-Cyclopropylphenoxy)ethyl]-4,5-dihydro-1H-imidazole	Ki	22.91 [1]
	2-[(1S)-1-(2-Cyclopropylphenoxy)ethyl]-4,5-dihydro-1H-imidazole	Ki	20.89 [1]
	2-[(1R)-1-(2-Cyclopropylphenoxy)ethyl]-4,5-dihydro-1H-imidazole	Ki	44.67 [1]
	(8S)-N-[2-(3-Fluorophenyl)ethyl]pentacyclo[5.4.0.02,6.03,10.05,9]undecan-8-amine	Ki	7609.0 [1]
	2-(1-(2-Bromophenoxy)ethyl)-4,5-dihydro-1H-imidazole	Ki	22.91 [1]
	2-[1-(2-Cyclopropyloxyphenoxy)ethyl]-4,5-dihydro-1H-imidazole	Ki	83.18 [1]
	2-[(1R)-1-[2-(Cyclopropylmethyl)phenoxy]ethyl]-4,5-dihydro-1H-imidazole	Ki	44.67 [1]
	2-[(1S)-1-[2-(Cyclopropylmethyl)phenoxy]ethyl]-4,5-dihydro-1H-imidazole	Ki	41.69 [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-heptaene	Ki	407.0 [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-dicarboxylate	Ki	800.0 [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-carboxamide	Ki	94.4 [1], 442.0 [2]
	1-((2,3-Dihydrobenzo[b][1,4]dioxin-2-yl)methyl)-4-(2-methoxyphenyl)piperazine	Ki	167.0 [1], 506.0 [2]
	N-[2-[4-(2,3-Dihydro-1,4-benzodioxin-3-ylmethyl)-1,4-diazepan-1-yl]ethyl]-2-phenoxypyridine-3-carboxamide	Ki	220.0 [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-carboxamide	Ki	208.0 [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-carboxamide	Ki	138.0 [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-carboxamide	Ki	73.6 [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-carboxamide	Ki	48.4 [1], 118.0 [2]
	1-(2,3-Dihydro-1,4-benzodioxin-3-ylmethyl)-4-[2-[(2-phenoxypyridin-3-yl)methoxy]ethyl]-1,4-diazepane	Ki	66.1 [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-oxadiazole	Ki	15.4 [1], 44.8 [2]
	4-Bromo-N-[[4-[[[4-(dimethylamino)quinazolin-2-yl]amino]methyl]cyclohexyl]methyl]-2-(trifluoromethoxy)benzenesulfonamide	IC50	7.7 [1]
	Norepinephrine	Ki	66.0 [1]
	Propranolol	IC50	5011.87 [1]
	Vancomycin	Ki	50.12 [1]
	Verapamil	Ki	217.0 [1]
	Tamoxifen	Ki	726.0 [1]
	Chlorpromazine	Ki	132.0 [1]
	Haloperidol	Ki	1865.0 [1]
	Fluoxetine	Ki	6.31 [1]
	Chloroquine	Ki	4365.16 [1]
	Ticlopidine	Ki	143.0 [1]
	Clonidine hydrochloride	Ki	20.89 [1]
	Amiodarone	Ki	117.0 [1]
	Amitriptyline	Ki	132.0 [1]
	Ketoconazole	Ki	7419.0 [1]
	Diethylstilbestrol	Ki	5297.0 [1]
	Bromocriptine	Ki	5.53 [1]

Entire TableStructureCompound NameStandard TypeStandard Values (in nM)

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References

This online tool may be cited as follows

MLA	"Quest Database™ Alpha-2a adrenergic receptor Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 21 Feb. 2025, https://www.aatbio.com/data-sets/alpha-2a-adrenergic-receptor-inhibitors-ic50-ki.
APA	AAT Bioquest, Inc. (2025, February 21). 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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