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TargetKappa-type opioid receptor
LigandBDBM50293856
Substrate/Competitorn/a
Meas. Tech.ChEMBL_572571 (CHEMBL1025187)
IC50 6800±n/a nM
Citation Satoh, ASagara, TSakoh, HHashimoto, MNakashima, HKato, TGoto, YMizutani, SAzuma-Kanoh, TTani, TOkuda, SOkamoto, OOzaki, SIwasawa, YOhta, HKawamoto, H Identification of an orally active opioid receptor-like 1 (ORL1) receptor antagonist 4-{3-[(2R)-2,3-dihydroxypropyl]-2-oxo-2,3-dihydro-1H-benzimidazol-1-yl}-1-[(1S,3S,4R)-spiro[bicyclo[2.2.1]heptane-2,1'-cyclopropan]-3-ylmethyl]piperidine as clinical candidate. J Med Chem52:4091-4 (2009) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Kappa-type opioid receptor
Name:Kappa-type opioid receptor
Synonyms:K-OR-1 | KOR-1 | Kappa-opioid receptor (KOR) | Kappa-type opioid receptor (KOPR) | Kappa-type opioid receptor (KOR) | Kappa-type opioid receptor (Kappa) | OPIATE Kappa | OPRK | OPRK1 | OPRK_HUMAN | kappa opioid receptor (KOR)
Type:G Protein-Coupled Receptor (GPCR)
Mol. Mass.:42648.76
Organism:Homo sapiens (Human)
Description:P41145
Residue:380
Sequence:
MDSPIQIFRGEPGPTCAPSACLPPNSSAWFPGWAEPDSNGSAGSEDAQLEPAHISPAIPV
IITAVYSVVFVVGLVGNSLVMFVIIRYTKMKTATNIYIFNLALADALVTTTMPFQSTVYL
MNSWPFGDVLCKIVISIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPLKAKIINI
CIWLLSSSVGISAIVLGGTKVREDVDVIECSLQFPDDDYSWWDLFMKICVFIFAFVIPVL
IIIVCYTLMILRLKSVRLLSGSREKDRNLRRITRLVLVVVAVFVVCWTPIHIFILVEALG
STSHSTAALSSYYFCIALGYTNSSLNPILYAFLDENFKRCFRDFCFPLKMRMERQSTSRV
RNTVQDPAYLRDIDGMNKPV
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50293856
n/a
NameBDBM50293856
Synonyms:1-(2,2-dimethyl-1,3-dioxan-5-yl)-3-{[1S,3R,6S)-2,1'-spirocyclopropane(bicyclo[2.2.1]heptane)-1'-norbornylmethyl]piperidin-4-yl}-1,3-dihydro-2H-benzimidazol-2-one hydrochloride | CHEMBL563980
TypeSmall organic molecule
Emp. Form.C25H35N3O3
Mol. Mass.425.5637
SMILESOC[C@@H](O)Cn1c2ccccc2n(C2CCN(C[C@H]3[C@H]4CC[C@H](C4)C33CC3)CC2)c1=O |r|
Structure
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