General Information of the Protein
Protein ID
PT02100
Protein Name
Nischarin
Secondarily
Protein Name
Imidazoline receptor 1
Imidazoline-1 receptor
Gene Name
NISCH
Sequence
MAAATLSFGPEREAEPAKEARVVGSELVDTYTVYVIQVTDGNHEWTIKHRYSDFHDLHEKLVAERKIDKTLLPPKKIIGKNSRSLVEKREKDLEVYLQTLLKTFPDVAPRVLAHFLHFHLYEINGVTAALAEELFEKGEQLLGAGEVFAIRPLQLYAITEQLQQGKPTCASGDAKTDLGHILDFTCRLKYLKVSGTEGPFGTSNIREQLLPFDLSIFKSLHQVEMSHCDAKHVRGLVTSKPTLATMSVRFSAASMKEVLVPEASEFDEWEPEGTTLGGPVTAVIPTWQALTTLDLSHNSISEIDESVKLIPKIEYLDLSHNGVLVVDNLQHLYNLVHLDLSYNKLSSLEGVHTKLGNVKTLNLAGNFLERLSGLHKLYSLVNLDLRDNRIEQLDEVKSIGNLPCLEHVALLNNPLSIIPDYRTKVLSQFGERASEICLDDVATTEKELDTVEVLKAIQKAKDVKSKLSSTEKKVGEDFRLPTAPCIRPSSSPPTAVPTSASLPQPILSNQGIMFVQEEALASSLSSTDSLPPDDRPIAQACSNSMGSLPTGQVAAEDLRDLPGAVGGVSPDHAEPEVQVVPGSGQIIFLPFTCIGYTATNQDFIQRLSTLIRQAIERQLPAWIEAANQREEAHGEQGEEEEEEEEEDVAESRYFEMGPPDAEEEEGSGQGEEDEEDEDEEAEEERLALEWALGADEDFLLEHIRILKVLWCFLIHVQGSIRQFAACLVLTDFGIAVFEIPHQESRGSSQHILSSLRFVFCFPHGDLTEFGFLMPELCLVLKVRHSENTLFIISDAANLHEFHADLRSCFAPQHMAMLCSPILYGSHTSLQEFLRQLLTFYKVAGGSQERSQGCFPVYLVYSDKRMVQTAAGDYSGNIEWASCTLCSAVRRSCCAPSEAVKSAAIPYWLLLTSQHLNVIKADFNPMPSRGTHNCRNRNSFKLSRVPLSTVLLDPTRSCTQPRGAFADGHVLELLVGYRFVTAIFVLPHEKFHFLRVYNQLRASLKDLKTVVIAKNPSARPRTQGPLAGGQPAKSRVSAEQRLQETPAEAPAPAPAAAESAAEAPAAAEASAPAGAPAPAGAPAPAGAPAGAQAPAPAQAEVPAQYPSERLIQSTSEENQIPSHLPVCPSLQHIARLRGRAIIDLFHSSIAEVENEELRHLLWSSVVFYQTPGLEVTACVLLSTKAVYFILHDGLRRYFSEPLQDFWHQKNTDYNNSPFHISQCFVLKLSDLQSVNVGLFDQYFRLTGSSPTQVVTCLTRDSYLTHCFLQHLMLVLSSLERTPSPEPIDKDFYSEFGDKNTGKMENYELIHSSRVKFTYPSEEEVGDLTYVVAQKMADPAKNPALSILLYIQAFQVITPQLGRGRGPLRPKTLLLTSAEIFLLDEDYIHYPLPEFAKEPPQRDRYRLDDGRRVRDLDRVLMGYNPYPQALTLVFDDTQGHDLMGSVTLDHFGEMPGGPGRAGQGREVQWQVFVPSAESREKLISLLARQWEALCGRELPVELTG
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Organism
Rattus norvegicus, Rat
Protein Classification
Other cytosolic protein
Function
Acts either as the functional imidazoline-1 receptor (I1R) candidate or as a membrane-associated mediator of the I1R signaling. Binds numerous imidazoline ligands that induces initiation of cell-signaling cascades triggering to cell survival, growth and migration. Its activation by the agonist rilmenidine induces an increase in phosphorylation of mitogen-activated protein kinases MAPK1 and MAPK3 in rostral ventrolateral medulla (RVLM) neurons that exhibited rilmenidine-evoked hypotension. Blocking its activation with efaroxan abolished rilmenidine-induced mitogen-activated protein kinase phosphorylation in RVLM neurons. Acts as a modulator of Rac-regulated signal transduction pathways (By similarity). Suppresses Rac1-stimulated cell migration by interacting with PAK1 and inhibiting its kinase activity (By similarity). Also blocks Pak-independent Rac signaling by interacting with RAC1 and inhibiting Rac1-stimulated NF-kB response element and cyclin D1 promoter activation (By similarity). Inhibits also LIMK1 kinase activity by reducing LIMK1 'Tyr-508' phosphorylation (By similarity). Inhibits Rac-induced cell migration and invasion in breast and colon epithelial cells (By similarity). Inhibits lamellipodia formation, when overexpressed (By similarity). Plays a role in protection against apoptosis (By similarity). Involved in association with IRS4 in the enhancement of insulin activation of MAPK1 and MAPK3 (By similarity). When overexpressed, induces a redistribution of cell surface ITGA5 integrin to intracellular endosomal structures (By similarity).
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Uniprot ID
Q4G017
Ensembl ID
ENSG00000010322
Subcellular Location
Cell membrane
Cytoplasm
Early endosome
Recycling endosome
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: CL000868 , PC12
Compound ID Compound Name Compound Formula
CP0250723
(2,6-Dichloro-4-iodo-phenyl)-(4,5-dihydro-1H-imidazol-2-yl)-amine
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C9H8Cl2IN3
 2
1
Ki = 0.03388 nM
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2
Ki = 0.7943 nM
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CP0497542
N-(2-chloro-4-iodophenyl)-2-methyl-3,4-dihydro-2H-pyrrol-5-amine
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C11H12ClIN2
 3
1
Ki = 0.1778 nM
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2
Ki = 0.2 nM
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3
Ki = 0.2188 nM
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CP0928349
N-(7-Chloro-2,3-dihydro-1H-inden-4-yl)-4-methylpyrrolidin-2-imine Hydrochloride
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C14H18Cl2N2
 1
1
Ki = 0.22 nM
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CP0441537
Phenamazoline
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C10H13N3
 1
1
Ki = 0.5012 nM
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CP0387054
N-(2,6-dichlorophenyl)-5-methyl-4,5-dihydro-1H-imidazol-2-amine
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C10H11Cl2N3
 2
1
Ki = 0.93 nM
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2
Ki = 0.9333 nM
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CP0385262
N-(4,5-dihydro-1H-imidazol-2-ylmethyl)-2-phenylaniline
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C16H17N3
 1
1
Ki = 0.9333 nM
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CP0295376
2-[(2S)-1-phenylpropan-2-yl]-4,5-dihydro-1H-imidazole
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C12H16N2
 1
1
Ki = 1.072 nM
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CP0491333
2-(naphthalen-2-yl)-4,5-dihydro-1H-imidazole
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C13H12N2
 1
1
Ki = 1.288 nM
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CP0497968
2-[(2-phenylphenoxy)methyl]-4,5-dihydro-1H-imidazole
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C16H16N2O
 1
1
Ki = 2.344 nM
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CP0919726
N-(7-Methyl-2,3-dihydro-1H-inden-4-yl)-4-methylpyrrolidin-2-imine Hydrochloride
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C15H21ClN2
 1
1
Ki = 2.8 nM
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CP0945094
N-(7-Chloro-2,3-dihydro-1H-inden-4-yl)-5-methylpyrrolidin-2-imine Hydrochloride
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C14H18Cl2N2
 1
1
Ki = 2.8 nM
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CP0919713
N-(3-Chloro-2-methylphenyl)-4-methylpyrrolidin-2-imine Hydrochloride
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C12H16Cl2N2
 1
1
Ki = 3.2 nM
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CP0378484
2-[(1R)-1-(2-phenylphenoxy)ethyl]-4,5-dihydro-1H-imidazole
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C17H18N2O
 1
1
Ki = 3.981 nM
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CP0447798
2-(1-phenylpropan-2-yl)-4,5-dihydro-1H-imidazole
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C12H16N2
 2
1
Ki = 5.012 nM
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2
Ki = 6309.57 nM
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CP0411604
2-(2-fluoro-5-methylphenyl)-4,5-dihydro-1H-imidazole
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C10H11FN2
 1
1
Ki = 5.3 nM
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CP0418063
CAS_81447-78-1
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C11H12Cl2N2O
 1
1
Ki = 5.623 nM
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CP0426323
N-(5-azido-2-chloro-4-iodophenyl)-2-methyl-3,4-dihydro-2H-pyrrol-5-amine
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C11H11ClIN5
 1
1
Ki = 6.03 nM
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CP0426322
5-[(2-bromophenoxy)methyl]-4,5-dihydro-1,3-oxazol-2-amine
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C10H11BrN2O2
 1
1
Ki = 6.4 nM
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CP0388283
4-chloro-2-(2-imidazolin-2-ylamino)isoindoline
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C11H13ClN4
 2
1
Ki = 6.918 nM
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2
Ki = 28.18 nM
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CP0056760
CHEBI:8862
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C10H16N2O
 3
1
Ki = 11.22 nM
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2
Ki = 12.59 nM
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3
Ki = 83.1 nM
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CP0296173
2-[(1S,2S)-2-phenylcyclopropyl]-4,5-dihydro-1H-imidazole
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C12H14N2
 2
1
Ki = 11.75 nM
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2
Ki = 346.74 nM
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CP0385365
2-[(2S)-1-(2-methylphenyl)propan-2-yl]-4,5-dihydro-1H-imidazole
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C13H18N2
 1
1
Ki = 13.18 nM
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CP0041905
2-(2,6-dichloroanilino)-1,3-diazacyclopentene-(2)
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C9H9Cl2N3
 4
1
Ki = 14.1 nM
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2
Ki = 112.2 nM
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3
Ki = 125.89 nM
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4
Ki = 281.84 nM
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CP0385264
2-((E)-Styryl)-4,5-dihydro-1H-imidazole
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C11H12N2
 2
1
Ki = 18.62 nM
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2
Ki = 19.05 nM
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CP0945093
N-(2,3-Dihydro-1H-inden-4-yl)-5-methylpyrrolidin-2-imine Hydrochloride
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C14H19ClN2
 1
1
Ki = 19 nM
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CP0963676
N-(2,3-Dihydro-1H-inden-4-yl)-4-methylpyrrolidin-2-imine Hydrochloride
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C14H19ClN2
 1
1
Ki = 19 nM
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CP0381525
2-[1-(2-methylphenyl)propan-2-yl]-4,5-dihydro-1H-imidazole
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C13H18N2
 1
1
Ki = 23.44 nM
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CP0967475
N-(3-Chloro-2-methylphenyl)-5-methylpyrrolidin-2-imine Hydrochloride
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C12H16Cl2N2
 1
1
Ki = 27 nM
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CP0570418
2-chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-6-methoxy-2-methyl-3H-pyridin-5-amine
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C10H15ClN4O
 1
1
Ki = 33.88 nM
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CP0504735
N-(2,3-dimethylphenyl)-3-methyl-3,4-dihydro-2H-pyrrol-5-amine;hydrochloride
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C13H19ClN2
 1
1
Ki = 42 nM
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CP0448995
2-[1-(2-thiophen-3-ylphenyl)propan-2-yl]-4,5-dihydro-1H-imidazole
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C16H18N2S
 1
1
Ki = 63.1 nM
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CP0850314
N-(2,3-Dimethylphenyl)-5-methylpyrrolidin-2-imine Hydrochloride
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C13H19ClN2
 1
1
Ki = 70 nM
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CP0868785
N-(5,6,7,8-Tetrahydronaphthalen-1-yl)-5-methylpyrrolidin-2-imine Hydrochloride
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C15H21ClN2
 1
1
Ki = 73 nM
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CP0421105
N-(2-chlorophenyl)-3,4-dihydro-2H-pyrrol-5-amine
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C10H11ClN2
 1
1
Ki = 77.62 nM
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CP0084070
(4-Chloro-6-methoxy-2-methyl-pyrimidin-5-yl)-imidazolidin-2-ylidene-amine
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C9H12ClN5O
 1
1
Ki = 77.8 nM
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CP0499262
2-[(2S)-1-(2-phenylphenyl)propan-2-yl]-4,5-dihydro-1H-imidazole
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C18H20N2
 1
1
Ki = 97.72 nM
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CP0333694
2-[1-(2-phenylphenoxy)ethyl]-4,5-dihydro-1H-imidazole
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C17H18N2O
 1
1
Ki = 125.89 nM
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CP0413599
2-[(1S)-1-(2-phenylphenoxy)ethyl]-4,5-dihydro-1H-imidazole
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C17H18N2O
 1
1
Ki = 128.82 nM
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CP0421104
US9303019, 13
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C11H13ClN2
 1
1
Ki = 131.83 nM
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CP0566129
2-[1-(2-phenylphenyl)propan-2-yl]-4,5-dihydro-1H-imidazole
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C18H20N2
 1
1
Ki = 154.88 nM
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CP0456129
2-[1-(2-chlorophenyl)propan-2-yl]-4,5-dihydro-1H-imidazole
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C12H15ClN2
 1
1
Ki = 194.98 nM
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CP0283392
2-Naphthalen-1-ylmethyl-4,5-dihydro-1H-imidazole; hydrochloride
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C14H14N2
 1
1
Ki = 245.47 nM
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CP0387572
2-(1-phenoxyethyl)-4,5-dihydro-1H-imidazole
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C11H14N2O
 1
1
Ki = 309.03 nM
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CP0343543
2-[(1R,2R)-2-phenylcyclopropyl]-4,5-dihydro-1H-imidazole
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C12H14N2
 1
1
Ki = 346.74 nM
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CP0410228
N-(dicyclopropylmethyl)-4-methyl-4,5-dihydro-1,3-oxazol-2-amine
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C11H18N2O
 1
1
Ki = 363.08 nM
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CP0441538
N-(dicyclopropylmethyl)-3,4-dihydro-2H-pyrrol-5-amine
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C11H18N2
 1
1
Ki = 512.86 nM
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CP0494836
N-(dicyclopropylmethyl)-2,3-dimethyl-3,4-dihydro-2H-pyrrol-5-amine
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C13H22N2
 1
1
Ki = 537 nM
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CP0289773
2-[(2R)-2-phenylpropyl]-4,5-dihydro-1H-imidazole
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C12H16N2
 1
1
Ki = 588.84 nM
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CP0409418
2-(phenoxymethyl)-4,5-dihydro-1H-imidazole
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C10H12N2O
 2
1
Ki = 691.83 nM
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2
Ki = 707.95 nM
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CP0562243
2-[(2R)-1-(2-methylphenyl)propan-2-yl]-4,5-dihydro-1H-imidazole
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C13H18N2
 1
1
Ki = 1047.13 nM
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CP0037622
2-(2,3-dihydro-1,4-benzodioxin-2-yl)-4,5-dihydro-1H-imidazole
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C11H12N2O2
 1
1
Ki = 1258.93 nM
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CP0044542
2-(2-Cyclopropyl-phenoxymethyl)-4,5-dihydro-1H-imidazole
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C13H16N2O
 1
1
Ki = 1737.8 nM
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CP0433771
2-[(2R)-1-(2-phenylphenyl)propan-2-yl]-4,5-dihydro-1H-imidazole
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C18H20N2
 1
1
Ki = 2238.72 nM
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CP0405873
2-(2,2-diphenylethyl)-4,5-dihydro-1H-imidazole
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C17H18N2
 1
1
Ki = 3090.3 nM
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CP0497969
2-(2-Biphenyl-2-yl-ethyl)-4,5-dihydro-1H-imidazole
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C17H18N2
 1
1
Ki = 3235.94 nM
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CP0427292
2-Phenethyl-4,5-dihydro-1H-imidazole
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C11H14N2
 1
1
Ki = 3715.35 nM
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CP0391248
2-[(2R)-1-phenylpropan-2-yl]-4,5-dihydro-1H-imidazole
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C12H16N2
 1
1
Ki = 6309.57 nM
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CP0415978
2-[(2S)-2-phenylpropyl]-4,5-dihydro-1H-imidazole
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C12H16N2
 1
1
Ki = 7244.36 nM
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CP0464865
2-(2-phenylpropyl)-4,5-dihydro-1H-imidazole
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C12H16N2
 1
1
Ki = 7244.36 nM
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CP0448994
3-[2-[2-(4,5-dihydro-1H-imidazol-2-yl)propyl]phenyl]pyridine
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C17H19N3
 1
1
Ki > 1000 nM
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CP0562244
3-[2-[2-(4,5-dihydro-1H-imidazol-2-yl)propyl]phenyl]phenol
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C18H20N2O
 1
1
Ki > 1000 nM
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Biochemical Assays
Compound ID Compound Name Compound Formula
CP0041905
2-(2,6-dichloroanilino)-1,3-diazacyclopentene-(2)
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C9H9Cl2N3
 1
1 IC50 = 366.2 nM