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Alpha-1a adrenergic receptor Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
(2-(2',6'-Dimethoxy)phenoxyethylamino)methylbenzo-1,4-dioxaneIC501.0 [1]
TamsulosinIC502.2 [1]
Methyl 5-[3-(4,4-diphenylpiperidin-1-yl)propylcarbamoyl]-2,6-dimethyl-4-(4-nitrophenyl)-1,4-dihydropyridine-3-carboxylateKi1.3 [1]
RisperidoneIC5010.0 [1], 10.9 [2]
RisperidoneKi2.3 [1], 2.8 [2], 10.0 [3]
AripiprazoleIC50170.0 [1]
AripiprazoleKi26.0 [1], 100.0 [2]
DoxazosinKi0.54 [1], 0.78 [2], 2.6 [3], 3.16 [4]
NaftopidilIC50555.0 [1]
NaftopidilKi3.7 [1], 3.71 [2], 5.88 [3]
3-[1-[4-(5-Chloro-1,1,3-trioxo-1,2-benzothiazol-2-yl)butyl]piperidin-4-yl]-1,3-benzoxazol-2-oneKi0.08 [1], 0.17 [2], 0.24 [3], 74.0 [4], 90.0 [5]
SilodosinIC501.8 [1], 1.9 [2]
SilodosinKi0.04 [1]
CyclazosinKi5.5 [1], 12.3 [2], 25.12 [3]
3-[2-[4-(2-Methoxyphenyl)-1-piperazinyl]ethyl]-1,5-dihydropyrimido[5,4-b]indole-2,4-dioneKi0.27 [1], 0.29 [2], 3.72e+18 [3]
(4S,5S)-4-(3,4-Difluorophenyl)-N-[3-[4-(4-fluorophenyl)piperidin-1-yl]propyl]-5-methyl-2-oxo-1,3-oxazolidine-3-carboxamideKi0.17 [1], 0.23 [2]
8-[(2R)-1-[4-(2,4,5-Trifluorophenyl)piperazin-1-yl]propan-2-yl]-8-azaspiro[4.5]decane-7,9-dioneKi290.0 [1], 294.0 [2], 14000.0 [3], 14900.0 [4]
5-N-[3-(4,4-Diphenylpiperidin-1-yl)propyl]-3-N,2,6-trimethyl-4-(4-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxamideKi3.1 [1], 3.16 [2], 4.47 [3]
5-N-[3-(4,4-Diphenylpiperidin-1-yl)propyl]-2,6-dimethyl-4-(4-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxamideKi1.3 [1], 1.86 [2], 1.87 [3]
N-((1r,4r)-4-(4-(2-Cyclopropoxyphenyl)piperidin-1-yl)cyclohexyl)-3,4-dimethoxybenzenesulfonamideKi0.91 [1], 11.0 [2]
N-((1r,4r)-4-(4-(2-Isopropoxyphenyl)piperidin-1-yl)cyclohexyl)-3,4-dimethoxybenzenesulfonamideKi1.8 [1], 2.2 [2], 28.0 [3]
3,4-Dimethoxy-N-[4-[4-[2-(2,2,2-trifluoroethoxy)phenyl]piperidin-1-yl]cyclohexyl]benzenesulfonamideKi1.8 [1], 21.0 [2]
N-((1r,4r)-4-(4-(2-(2-Fluoroethoxy)phenyl)piperidin-1-yl)cyclohexyl)-3,4-dimethoxybenzenesulfonamideKi8.5 [1], 11.0 [2], 69.0 [3]
N-[4-[4-[2-(2,2-Difluoroethoxy)phenyl]piperidin-1-yl]cyclohexyl]-3,4-dimethoxybenzenesulfonamideKi12.0 [1], 31.0 [2]
3,4-Dimethoxy-N-[4-[4-(2-propan-2-yloxyphenyl)piperazin-1-yl]cyclohexyl]benzenesulfonamideKi1.6 [1], 2.0 [2], 23.0 [3]
ClozapineKi10.0 [1], 19.0 [2]
OlanzapineKi60.0 [1], 1000.0 [2]
PhentolamineKi0.6 [1], 4.12 [2], 12.0 [3]
AzelastineKi50.12 [1]
8-(2-(4-(2-Methoxyphenyl)piperazin-1-yl)ethyl)-8-azaspiro[4.5]decane-7,9-dione dihydrochlorideKi42.66 [1], 251.19 [2], 380.19 [3]
NiguldipineKi0.16 [1], 1.8 [2]
UpidosinKi0.34 [1], 1.0 [2]
7-Chloro-2-ethenyl-3,4,5,6-tetrahydro-4-methylthieno(4,3,2-ef)(3)benzazepineKi25.12 [1], 36.0 [2]
Benzyl (2S)-4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-2-(tert-butylcarbamoyl)piperazine-1-carboxylateIC50590.0 [1]
Benzyl (2S)-4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-2-(tert-butylcarbamoyl)piperazine-1-carboxylateKi420.0 [1]
CID 9872515Ki1.0 [1], 1.26 [2], 1.3 [3]
2-[[(2R)-1-[4-[4-[3-(Azepan-1-yl)propoxy]phenyl]butyl]pyrrolidin-2-yl]methyl]-4-[(4-chlorophenyl)methyl]phthalazin-1-oneKi39.81 [1]
N-[[(3S)-2,3-Dihydro-1,4-benzodioxin-3-yl]methyl]-2-(2,6-dimethoxyphenoxy)ethanamine;hydrochlorideKi0.41 [1]
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)methanamineIC50537.03 [1]
Methyl 4-(3,4-difluorophenyl)-3-[3-(4-methoxycarbonyl-4-phenylpiperidin-1-yl)propylcarbamoyl]-6-methyl-2-oxo-1,4-dihydropyrimidine-5-carboxylateKi0.1 [1], 1.0 [2]
5-N-[4-(4,4-Diphenylpiperidin-1-yl)butyl]-2,6-dimethyl-4-(4-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxamideKi1.86 [1], 1.87 [2], 1.9 [3]
Methyl 5-[4-(4,4-diphenylpiperidin-1-yl)butylcarbamoyl]-2,6-dimethyl-4-(4-nitrophenyl)-1,4-dihydropyridine-3-carboxylateKi5.89 [1], 14.79 [2]
Methyl 5-[3-(4-methoxycarbonyl-4-phenylpiperidin-1-yl)propylcarbamoyl]-2,6-dimethyl-4-(4-nitrophenyl)-1,4-dihydropyridine-3-carboxylateKi3.55 [1], 3.58 [2], 3.6 [3]
1-(1,4-Dioxaspiro[4.5]decan-3-ylmethyl)-4-(2-methoxyphenyl)piperazineKi91.2 [1]
N-[(2,2-Diphenyl-1,3-dioxolan-4-yl)methyl]-2-phenoxyethanamine;oxalic acidKi37.15 [1]
Methyl 1-[3-[[5-carbamoyl-6-ethyl-4-(4-nitrophenyl)-2-oxo-1,4-dihydropyrimidine-3-carbonyl]amino]propyl]-4-phenylpiperidine-4-carboxylateKi0.19 [1], 0.5 [2], 1.9 [3]
ClonidineKi512.86 [1], 977.24 [2]
QuetiapineKi20.0 [1], 100.0 [2]
CorynanthineKi29.0 [1], 142.0 [2]
MianserinIC50407.38 [1]
Cyclohexanecarboxamide, n-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-n-2-pyridinyl-Ki18.62 [1], 20.0 [2]
AlfuzosinKi8.2 [1], 10.0 [2]
RilmenidineKi6025.6 [1], 8912.51 [2]
1-(2-Methoxyphenyl)-4-(4-(2-phthalimido)butyl)piperazineKi0.26 [1], 2.0 [2]
IndoraminKi3.7 [1], 3.98 [2]
5-MethylurapidilKi0.63 [1], 2.3 [2]
DexniguldipineKi0.16 [1], 4.7 [2]
1-(5-Chloro-1H-indol-3-yl)-N-[2-[2-(cyclopropylmethoxy)phenoxy]ethyl]-2-methylpropan-2-amineKi0.6 [1], 0.63 [2]
5-Methyl-3-[3-[4-[2-(2,2,2-trifluoroethoxy)phenyl]piperazin-1-yl]propyl]-1H-pyrimidine-2,4-dioneKi0.25 [1]
N,N-Diallyl-5-methoxytryptamineKi10000.0 [1]
Methyl (4R)-5-[3-(4,4-diphenylpiperidin-1-yl)propylcarbamoyl]-2,6-dimethyl-4-(4-nitrophenyl)-1,4-dihydropyridine-3-carboxylateKi0.18 [1]
5-[2-[(3Ar,9bR)-6-methoxy-1,3,3a,4,5,9b-hexahydrobenzo[e]isoindol-2-yl]ethyl]-8-thia-3,5,13-triazatricyclo[7.4.0.02,7]trideca-1(9),2(7),10,12-tetraene-4,6-dioneKi0.22 [1]
2-(2-Biphenylyloxymethyl)-2-imidazolineIC5027.54 [1], 66.07 [2]
3-[2-[4-(2-Methoxyphenyl)piperazin-1-yl]ethyl]-5-phenyl-1H-thieno[2,3-d]pyrimidine-2,4-dioneKi2.6 [1], 2.63 [2]
N-[2-(2,6-Dimethoxyphenoxy)ethyl]-2-(2-phenylmethoxyphenoxy)ethanamineKi0.47 [1]
2-Bromo-7-chloro-11-methyl-3-oxa-11-azatricyclo[6.4.1.04,13]trideca-1,4(13),5,7-tetraeneKi3300.0 [1]
2-(2-Oxopiperidin-1-yl)-N-[3-[4-(2-propan-2-yloxyphenyl)piperazin-1-yl]propyl]acetamideKi0.65 [1], 0.66 [2]
3-[2-[4-(2-Methoxyphenyl)piperazin-1-yl]ethyl]-5-(3-methylphenyl)-1H-thieno[2,3-d]pyrimidine-2,4-dioneKi4.17 [1], 4.2 [2]
2,9-Dimethoxy-5,8,13,13a-tetrahydro-6H-isoquino[3,2-a]isoquinoline-3,10-diolKi616.0 [1], 630.0 [2]
2-(2,6-Dimethoxyphenoxy)-N-[[(2R)-6,6-diphenyl-1,4-dioxan-2-yl]methyl]ethanamineKi165.96 [1], 338.84 [2]
N-[[(2R)-6,6-Diphenyl-1,4-dioxan-2-yl]methyl]-2-(2-methoxyphenoxy)ethanamineKi16.6 [1], 27.54 [2]
N-[[(2R)-6,6-Diphenyl-1,4-dioxan-2-yl]methyl]-2-phenoxyethanamineKi128.82 [1], 169.82 [2]
(4S)-2-(2-Aminoethoxymethyl)-3-N-[3-(4,4-diphenylpiperidin-1-yl)propyl]-6-ethyl-4-(4-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxamideKi0.4 [1], 0.65 [2]
N-[[(3R)-2,3-Dihydro-1,4-benzodioxin-3-yl]methyl]-2-(2,6-dimethoxyphenoxy)ethanamine;hydrochlorideKi11.22 [1]
JTH-601 free baseKi0.4 [1]
Unii-M7ias8PR23Ki8.7 [1], 9.3 [2]
2-(2-Oxoazepan-1-yl)-N-[2-[4-(2-propan-2-yloxyphenyl)piperazin-1-yl]ethyl]acetamideKi18.0 [1], 22.0 [2]
3-[2-[4-(2-Methoxyphenyl)piperazin-1-yl]ethyl]-1H-[1]benzothiolo[3,2-d]pyrimidine-2,4-dioneKi3.31 [1]
Methyl 1-[3-[[2,6-dimethyl-5-(methylcarbamoyl)-4-(4-nitrophenyl)-1,4-dihydropyridine-3-carbonyl]amino]propyl]-4-phenylpiperidine-4-carboxylateKi3.98 [1], 607.0 [2]
(4R)-4-(3,4-Difluorophenyl)-N-[3-[4-(4-fluorophenyl)piperidin-1-yl]propyl]-6-(methoxymethyl)-2-oxo-3,4-dihydro-1H-pyrimidine-5-carboxamideKi0.24 [1]
Methyl 1-[3-[[5-carbamoyl-4-(2,4-difluorophenyl)-6-ethyl-2-oxo-1,4-dihydropyrimidine-3-carbonyl]amino]propyl]-4-phenylpiperidine-4-carboxylateKi0.2 [1]
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-dimethylmethanamineIC5014.45 [1]
(4R)-4-(3,4-Difluorophenyl)-6-(methoxymethyl)-2-oxo-N-[3-(4-pyridin-2-ylpiperidin-1-yl)propyl]-3,4-dihydro-1H-pyrimidine-5-carboxamideKi0.45 [1]
(4R)-N-[3-[4-(2-Cyanophenyl)piperidin-1-yl]propyl]-4-(3,4-difluorophenyl)-2-oxo-3,4-dihydro-1H-pyrimidine-5-carboxamideKi0.13 [1]
(4R)-4-(3,4-Difluorophenyl)-N-[3-[4-(4-fluorophenyl)piperidin-1-yl]propyl]-1,3,6-trimethyl-2-oxo-4H-pyrimidine-5-carboxamideKi0.14 [1], 0.18 [2]
(4R)-4-(3,4-Difluorophenyl)-N-[3-[4-(4-fluorophenyl)piperidin-1-yl]propyl]-2-oxo-3,4-dihydro-1H-pyrimidine-5-carboxamideKi0.17 [1]
Methyl (4R)-4-(3,4-difluorophenyl)-5-[3-[4-(4-fluorophenyl)piperidin-1-yl]propylcarbamoyl]-1,6-dimethyl-2-oxo-4H-pyrimidine-3-carboxylateKi0.75 [1]
Methyl 4-(3,4-difluorophenyl)-3-[5-(4-methoxycarbonyl-4-phenylpiperidin-1-yl)pentyl]-6-methyl-2-oxo-1,4-dihydropyrimidine-5-carboxylateKi0.1 [1]
(4R)-N-[3-[4-(2-Cyano-4-fluorophenyl)piperidin-1-yl]propyl]-4-(3,4-difluorophenyl)-2-oxo-3,4-dihydro-1H-pyrimidine-5-carboxamideKi0.07 [1]
(4R)-3-Acetyl-4-(3,4-difluorophenyl)-N-[3-[4-(4-fluorophenyl)piperidin-1-yl]propyl]-1,6-dimethyl-2-oxo-4H-pyrimidine-5-carboxamideKi2.2 [1]
Methyl 1-[3-[[5-carbamoyl-2,6-dimethyl-4-(4-nitrophenyl)-1,4-dihydropyridine-3-carbonyl]amino]propyl]-4-phenylpiperidine-4-carboxylateKi0.84 [1], 2.4 [2]
3-[2-[4-(2-Methoxyphenyl)piperazin-1-yl]ethyl]-2-methyl-5H-pyrimido[5,4-b]indol-4-oneKi3.02 [1], 3.31e+17 [2]
4-[(4-Chlorophenyl)methyl]-2-[[(2R)-1-methylpyrrolidin-2-yl]methyl]phthalazin-1-oneKi25.12 [1], 31.62 [2]
5-Chloro-2-methoxy-N-[4-[4-(2-propan-2-yloxyphenyl)piperazin-1-yl]cyclohexyl]benzenesulfonamideKi1.0 [1], 3.8 [2]



References

This online tool may be cited as follows

MLA

"Quest Database™ Alpha-1a adrenergic receptor Inhibitors (IC50, Ki)." AAT Bioquest, Inc.10 May2024https://www.aatbio.com/data-sets/alpha-1a-adrenergic-receptor-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024May 10). Quest Database™ Alpha-1a adrenergic receptor Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/alpha-1a-adrenergic-receptor-inhibitors-ic50-ki.
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