General Information of the Protein
Protein ID
PT02060
Protein Name
Alpha-1A adrenergic receptor
Secondarily
Protein Name
Alpha-1A adrenoreceptor
Alpha-1C adrenergic receptor
Gene Name
ADRA1A
Secondarily
Gene Name
ADRA1C
Sequence
MVFLSGNASDSSNCTHPPPPVNISKAILLGVILGGLILFGVLGNILVILSVACHRHLHSVTHYYIVNLAVADLLLTSTVLPFSAIFEILGYWAFGRVFCNVWAAVDVLCCTASIMGLCIISIDRYIGVSYPLRYPTIVTQKRGLMALLCVWALSLVISIGPLFGWRQPAPEDETICQINEEPGYVLFSALGSFYVPLTIILVMYCRVYVVAKRESRGLKSGLKTDKSDSEQVTLRIHRKNAQVGGSGVTSAKNKTHFSVRLLKFSREKKAAKTLGIVVGCFVLCWLPFFLVMPIGSFFPDFRPSETVFKIAFWLGYLNSCINPIIYPCSSQEFKKAFQNVLRIQCLRRKQSSKHTLGYTLHAPSHVLEGQHKDLVRIPVGSAETFYKISKTDGVCEWKIFSSLPRGSARMAVARDPSACTTARVRSKSFLQVCCCLGPSTPSHGENHQIPTIKIHTISLSENGEEV
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Organism
Bos taurus, Bovine
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Small molecule receptor (family A GPCR)
>
Monoamine receptor
>
Adrenergic receptor
Function
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine (PE)-stimulated ERK signaling in cardiac myocytes (By similarity).
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Uniprot ID
P18130
Ensembl ID
ENSG00000120907
Subcellular Location
Nucleus membrane
Cell membrane
Cytoplasm
Membrane
Caveola
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000051 , BHK-21
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0126864
 Compound Info 
1-Methyl-4-(8-(1-methyl-1H-tetrazol-5-yl)-10,11-dihydrodibenzo[b,f]thiepin-10-yl)piperazine
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C21H24N6S
  1
1
Ki = 0.067 nM
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CP0233816
 Compound Info 
(11-(4-Methylpiperazin-1-yl)-10,11-dihydrodibenzo[b,f]thiepin-2-yl)methanamine
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C20H25N3S
  1
1
Ki = 0.082 nM
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CP0283889
 Compound Info 
1-Methyl-4-(8-(1-methyl-1H-1,2,4-triazol-3-yl)-10,11-dihydrodibenzo[b,f]thiepin-10-yl)piperazine
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C22H25N5S
  1
1
Ki = 0.086 nM
 Bioactivity Info 
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CP0126978
 Compound Info 
N-[[5-(4-methylpiperazin-1-yl)-5,6-dihydrobenzo[b][1]benzothiepin-3-yl]methyl]acetamide
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C22H27N3OS
  1
1
Ki = 0.088 nM
 Bioactivity Info 
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CP0298666
 Compound Info 
11-(4-Methylpiperazin-1-yl)-10,11-dihydrodibenzo[b,f]thiepine-2-carbonitrile
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C20H21N3S
  1
1
Ki = 0.096 nM
 Bioactivity Info 
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CP0298668
 Compound Info 
2-methyl-N-[[5-(4-methylpiperazin-1-yl)-5,6-dihydrobenzo[b][1]benzothiepin-3-yl]methyl]propanamide
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C24H31N3OS
  1
1
Ki = 0.12 nM
 Bioactivity Info 
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CP0260914
 Compound Info 
(S)-N-((11-(4-methylpiperazin-1-yl)-10,11-dihydrodibenzo[b,f]thiepin-2-yl)methyl)isobutyramide
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C24H31N3OS
  1
1
Ki = 0.16 nM
 Bioactivity Info 
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CP0156782
 Compound Info 
1-(4-fluorophenyl)-3-(1-methylpiperidin-4-yl)-5-(1-methyl-1,2,4-triazol-3-yl)indole
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C23H24FN5
  1
1
Ki = 0.16 nM
 Bioactivity Info 
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CP0205851
 Compound Info 
1-Methyl-4-(8-(2-methyl-2H-tetrazol-5-yl)-10,11-dihydrodibenzo[b,f]thiepin-10-yl)piperazine
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C21H24N6S
  1
1
Ki = 0.17 nM
 Bioactivity Info 
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CP0195465
 Compound Info 
1-(2-(4-(5-(aminomethyl)-1-(4-fluorophenyl)-1H-indol-3-yl)piperidin-1-yl)ethyl)imidazolidin-2-one
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C25H30FN5O
  1
1
Ki = 0.18 nM
 Bioactivity Info 
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CP0240468
 Compound Info 
1-Methyl-4-(8-(pyridin-3-yl)-10,11-dihydrodibenzo[b,f]thiepin-10-yl)piperazine
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C24H25N3S
  1
1
Ki = 0.19 nM
 Bioactivity Info 
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CP0126975
 Compound Info 
5-(11-(4-Methylpiperazin-1-yl)-10,11-dihydrodibenzo[b,f]thiepin-2-yl)pyrimidine
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C23H24N4S
  1
1
Ki = 0.2 nM
 Bioactivity Info 
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CP0228798
 Compound Info 
1-(2-{4-[1-(4-Fluoro-phenyl)-5-(2-methyl-2H-tetrazol-5-yl)-1H-indol-3-yl]-piperidin-1-yl}-ethyl)-imidazolidin-2-one
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C26H29FN8O
  1
1
Ki = 0.23 nM
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CP0126865
 Compound Info 
1-Methyl-4-(8-(1-methyl-1H-pyrazol-4-yl)-10,11-dihydrodibenzo[b,f]thiepin-10-yl)piperazine
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C23H26N4S
  1
1
Ki = 0.24 nM
 Bioactivity Info 
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CP0167142
 Compound Info 
1-Methyl-4-(8-(pyridin-2-yl)-10,11-dihydrodibenzo[b,f]thiepin-10-yl)piperazine
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C24H25N3S
  1
1
Ki = 0.24 nM
 Bioactivity Info 
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CP0071691
 Compound Info 
1-Methyl-4-(8-(1-methyl-1H-pyrazol-3-yl)-10,11-dihydrodibenzo[b,f]thiepin-10-yl)piperazine
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C23H26N4S
  1
1
Ki = 0.26 nM
 Bioactivity Info 
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CP0112004
 Compound Info 
1-((S)-8-Chloro-10,11-dihydro-dibenzo[b,f]thiepin-10-yl)-4-methyl-piperazine
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C19H21ClN2S
  2
1
Ki = 0.28 nM
 Bioactivity Info 
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2
Ki = 0.56 nM
 Bioactivity Info 
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CP0078373
 Compound Info 
1-(4-fluorophenyl)-3-(1-methylpiperidin-4-yl)-5-(2-methyltetrazol-5-yl)indole
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C22H23FN6
  1
1
Ki = 0.28 nM
 Bioactivity Info 
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CP0186855
 Compound Info 
1-(4-fluorophenyl)-3-(1-methylpiperidin-4-yl)-5-(2-methylpyrazol-3-yl)indole
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C24H25FN4
  1
1
Ki = 0.32 nM
 Bioactivity Info 
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CP0240469
 Compound Info 
(S)-N-((11-(4-methylpiperazin-1-yl)-10,11-dihydrodibenzo[b,f]thiepin-2-yl)methyl)acetamide
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C22H27N3OS
  1
1
Ki = 0.34 nM
 Bioactivity Info 
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CP0267173
 Compound Info 
3-(2-{4-[1-(4-Fluoro-phenyl)-5-(2-methyl-2H-tetrazol-5-yl)-1H-indol-3-yl]-piperidin-1-yl}-ethyl)-oxazolidin-2-one
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C26H28FN7O2
  1
1
Ki = 0.35 nM
 Bioactivity Info 
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CP0046703
 Compound Info 
1-(2-{4-[5-chloro-1-(4-fluorophenyl)-1H-indol-3-yl]piperidin-1-yl}ethyl)imidazolidin-2-one
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C24H26ClFN4O
  1
1
Ki = 0.37 nM
 Bioactivity Info 
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CP0040110
 Compound Info 
1-Methyl-4-(8-(1-methyl-1H-pyrazol-5-yl)-10,11-dihydrodibenzo[b,f]thiepin-10-yl)piperazine
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C23H26N4S
  1
1
Ki = 0.41 nM
 Bioactivity Info 
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CP0205856
 Compound Info 
(R)-N-((11-(4-methylpiperazin-1-yl)-10,11-dihydrodibenzo[b,f]thiepin-2-yl)methyl)acetamide
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C22H27N3OS
  1
1
Ki = 0.42 nM
 Bioactivity Info 
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CP0167141
 Compound Info 
(R)-N-((11-(4-methylpiperazin-1-yl)-10,11-dihydrodibenzo[b,f]thiepin-2-yl)methyl)isobutyramide
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C24H31N3OS
  1
1
Ki = 0.43 nM
 Bioactivity Info 
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CP0277576
 Compound Info 
1-(2-{4-[1-(4-Fluoro-phenyl)-5-(1-methyl-1H-pyrazol-3-yl)-1H-indol-3-yl]-piperidin-1-yl}-ethyl)-imidazolidin-2-one
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C28H31FN6O
  1
1
Ki = 0.49 nM
 Bioactivity Info 
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CP0267544
 Compound Info 
1-Methyl-4-(8-phenyl-10,11-dihydrodibenzo[b,f]thiepin-10-yl)-piperazine
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C25H26N2S
  1
1
Ki = 0.5 nM
 Bioactivity Info 
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CP0126862
 Compound Info 
1-(8-chloro-10,11-dihydrodibenzo[b,f]thiepin-10-yl)-4-methylpiperazine
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C24H23FN4
  1
1
Ki = 0.52 nM
 Bioactivity Info 
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CP0126866
 Compound Info 
1-Methyl-4-(8-(5-methylthiophen-2-yl)-10,11-dihydrodibenzo-[b,f]thiepin-10-yl)piperazine
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C24H26N2S2
  1
1
Ki = 0.52 nM
 Bioactivity Info 
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CP0477104
 Compound Info 
1-(4-fluorophenyl)-3-(1-methylpiperidin-4-yl)-5-(1-methylpyrazol-3-yl)indole
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C24H25FN4
  1
1
Ki = 0.54 nM
 Bioactivity Info 
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CP0134581
 Compound Info 
3-(2-{4-[1-(4-Fluoro-phenyl)-5-pyrimidin-2-yl-1H-indol-3-yl]-piperidin-1-yl}-ethyl)-oxazolidin-2-one
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C28H28FN5O2
  1
1
Ki = 0.56 nM
 Bioactivity Info 
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CP0343878
 Compound Info 
3-(2-{4-[1-(4-Fluoro-phenyl)-5-(1-methyl-1H-[1,2,4]triazol-3-yl)-1H-indol-3-yl]-piperidin-1-yl}-ethyl)-oxazolidin-2-one
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C27H29FN6O2
  1
1
Ki = 0.62 nM
 Bioactivity Info 
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CP0080536
 Compound Info 
1-(3-chloro-5,6-dihydrobenzo[b][1]benzothiepin-5-yl)-4-methyl-piperazine;maleate
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C19H21ClN2S
  1
1
Ki = 0.66 nM
 Bioactivity Info 
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CP0195466
 Compound Info 
1-(2-(4-(1-(4-fluorophenyl)-5-((2-methyl-2H-tetrazol-5-yl)methyl)-1H-indol-3-yl)piperidin-1-yl)ethyl)imidazolidin-2-one
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C27H31FN8O
  1
1
Ki = 0.66 nM
 Bioactivity Info 
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CP0126974
 Compound Info 
N-[[1-(4-fluorophenyl)-3-[1-[2-(2-oxoimidazolidin-1-yl)ethyl]piperidin-4-yl]indol-5-yl]methyl]acetamide
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C27H32FN5O2
  1
1
Ki = 0.68 nM
 Bioactivity Info 
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CP0147752
 Compound Info 
1-(8-Chloro-10,11-dihydro-dibenzo[b,f]thiepin-10-yl)-4-methyl-piperazine
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C19H21ClN2S
  2
1
Ki = 0.7 nM
 Bioactivity Info 
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2
Ki = 1.4 nM
 Bioactivity Info 
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CP0151333
 Compound Info 
1-(2-{4-[1-(4-Fluoro-phenyl)-5-(1-methyl-1H-[1,2,4]triazol-3-yl)-1H-indol-3-yl]-piperidin-1-yl}-ethyl)-imidazolidin-2-one
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C27H30FN7O
  1
1
Ki = 0.8 nM
 Bioactivity Info 
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CP0071690
 Compound Info 
1-Methyl-4-(8-o-tolyl-10,11-dihydrodibenzo[b,f]thiepin-10-yl)-piperazine
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C26H28N2S
  1
1
Ki = 0.87 nM
 Bioactivity Info 
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CP0040814
 Compound Info 
[4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-(furan-2-yl)methanone
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C19H21N5O4
  1
1
Ki = 0.93 nM
 Bioactivity Info 
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CP0195469
 Compound Info 
1-Methyl-4-(8-m-tolyl-10,11-dihydrodibenzo[b,f]thiepin-10-yl)-piperazine
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C26H28N2S
  1
1
Ki = 0.95 nM
 Bioactivity Info 
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CP0163622
 Compound Info 
3-{4-[1-(4-Fluoro-phenyl)-5-(1-methyl-1H-[1,2,4]triazol-3-yl)-1H-indol-3-yl]-piperidin-1-yl}-propionitrile
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C25H25FN6
  1
1
Ki = 0.99 nM
 Bioactivity Info 
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CP0126977
 Compound Info 
1-(8-(2,5-Dimethylphenyl)-10,11-dihydrodibenzo[b,f]thiepin-10-yl)-4-methylpiperazine
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C27H30N2S
  1
1
Ki = 1 nM
 Bioactivity Info 
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CP0260913
 Compound Info 
1-Methyl-4-(8-p-tolyl-10,11-dihydrodibenzo[b,f]thiepin-10-yl)-piperazine
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C26H28N2S
  1
1
Ki = 1.1 nM
 Bioactivity Info 
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CP0333143
 Compound Info 
3-(2-{4-[1-(4-Fluoro-phenyl)-5-(1-methyl-1H-[1,2,4]triazol-3-yl)-1H-indol-3-yl]-piperidin-1-yl}-ethyl)-1H-quinazoline-2,4-dione
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C32H30FN7O2
  1
1
Ki = 1.3 nM
 Bioactivity Info 
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CP0195470
 Compound Info 
2,2-dimethyl-N-[[5-(4-methylpiperazin-1-yl)-5,6-dihydrobenzo[b][1]benzothiepin-3-yl]methyl]propanamide
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C25H33N3OS
  1
1
Ki = 1.3 nM
 Bioactivity Info 
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CP0195467
 Compound Info 
1-Methyl-4-(8-(pyridin-4-yl)-10,11-dihydrodibenzo[b,f]thiepin-10-yl)piperazine
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C24H25N3S
  1
1
Ki = 1.5 nM
 Bioactivity Info 
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CP0195472
 Compound Info 
1-(8-(2,3-Dimethylphenyl)-10,11-dihydrodibenzo[b,f]thiepin-10-yl)-4-methylpiperazine
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C27H30N2S
  1
1
Ki = 1.5 nM
 Bioactivity Info 
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CP0240470
 Compound Info 
1-(8-Mesityl-10,11-dihydrodibenzo[b,f]thiepin-10-yl)-4-methylpiperazine
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C28H32N2S
  1
1
Ki = 2 nM
 Bioactivity Info 
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CP0320413
 Compound Info 
3-(2-{4-[1-(4-Fluoro-phenyl)-5-(1-methyl-1H-[1,2,4]triazol-3-yl)-1H-indol-3-yl]-piperidin-1-yl}-ethyl)-1-methyl-pyrrolidin-2-one
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C29H33FN6O
  1
1
Ki = 2.2 nM
 Bioactivity Info 
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CP0208485
 Compound Info 
1-(4-fluorophenyl)-3-(1-methylpiperidin-4-yl)-5-pyridin-3-ylindole
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C25H24FN3
  1
1
Ki = 2.3 nM
 Bioactivity Info 
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CP0337896
 Compound Info 
1-(4-fluorophenyl)-3-(1-methylpiperidin-4-yl)-5-(1-methylpyrazol-4-yl)indole
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C24H25FN4
  1
1
Ki = 2.7 nM
 Bioactivity Info 
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CP0126860
 Compound Info 
1-(2-{4-[1-(4-Fluoro-phenyl)-5-(1-methyl-1H-[1,2,3]triazol-4-yl)-1H-indol-3-yl]-piperidin-1-yl}-ethyl)-imidazolidin-2-one
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C27H30FN7O
  1
1
Ki = 3 nM
 Bioactivity Info 
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CP0105167
 Compound Info 
3-{4-[1-(4-Fluoro-phenyl)-5-pyrimidin-2-yl-1H-indol-3-yl]-piperidin-1-yl}-propionitrile
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C26H24FN5
  1
1
Ki = 3.9 nM
 Bioactivity Info 
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CP0235398
 Compound Info 
(Cyclazosin)[4-(4-Amino-6,7-dimethoxy-quinazolin-2-yl)-octahydro-quinoxalin-1-yl]-furan-2-yl-methanone
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C23H27N5O4
  1
1
Ki = 5.1 nM
 Bioactivity Info 
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CP0072943
 Compound Info 
3-[4,5-dihydro-1H-imidazol-2-ylmethyl-(4-methylphenyl)amino]phenol;methanesulfonic acid
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C17H19N3O
  1
1
Ki = 6.8 nM
 Bioactivity Info 
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CP0078375
 Compound Info 
1-(4-fluorophenyl)-3-(1-methylpiperidin-4-yl)-5-pyridin-4-ylindole
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C25H24FN3
  1
1
Ki = 10 nM
 Bioactivity Info 
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CP0410809
 Compound Info 
3-(1-methylpiperidin-4-yl)-5-(2-methylpyrazol-3-yl)-1-pyridin-4-ylindole
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C23H25N5
  1
1
Ki = 19 nM
 Bioactivity Info 
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CP0489907
 Compound Info 
3-(1-methylpiperidin-4-yl)-1-pyridin-4-yl-5-pyrimidin-5-ylindole
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C23H23N5
  1
1
Ki = 19 nM
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CP0428117
 Compound Info 
3-(1-methylpiperidin-4-yl)-5-pyridin-3-yl-1-pyridin-4-ylindole
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C24H24N4
  1
1
Ki = 22 nM
 Bioactivity Info 
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CP0427043
 Compound Info 
3-(1-methylpiperidin-4-yl)-1,5-dipyridin-4-ylindole
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C24H24N4
  1
1
Ki = 24 nM
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CP0385760
 Compound Info 
3-(1-methylpiperidin-4-yl)-5-(1-methylpyrazol-4-yl)-1-pyridin-4-ylindole
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C23H25N5
  1
1
Ki = 38 nM
 Bioactivity Info 
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CP0072419
 Compound Info 
(SNAP-8719)[4-(4-Amino-6,7-dimethoxy-quinazolin-2-yl)-octahydro-quinoxalin-1-yl]-furan-2-yl-methanone
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C22H28F3N3O2
  1
1
Ki = 5900 nM
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Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0040814
 Compound Info 
[4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-(furan-2-yl)methanone
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C19H21N5O4
  2
1 Ki = 0.1259 nM
2 Ki = 0.17 nM
CP0072943
 Compound Info 
3-[4,5-dihydro-1H-imidazol-2-ylmethyl-(4-methylphenyl)amino]phenol;methanesulfonic acid
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C17H19N3O
  1
1 Ki = 0.7943 nM
CP0147996
 Compound Info 
CHEBI:8093
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C9H13NO2
  1
1 Ki = 933.25 nM
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT01089 Alpha-1A adrenergic receptor Homo sapiens, Human
 Protein Info 
PT01339 Alpha-1A adrenergic receptor Rattus norvegicus, Rat
 Protein Info