Target
Nociceptin receptor
Ligand
BDBM29992
Substrate
BDBM29961
Meas. Tech.
In Vitro Binding Assay (IC50) and In Vitro Agonism/Antagonism Measurements (EC50/IC50)
pH
7.4±n/a
Temperature
310.15±n/a K
IC50
1.4±n/a nM
EC50
1.3±n/a nM
Citation
 Kobayashi, KUchiyama, MTakahashi, HKawamoto, HIto, SYoshizumi, TNakashima, HKato, TShimizu, AYamamoto, IAsai, MMiyazoe, HOhno, AHirayama, MOzaki, STani, TIshii, YTanaka, TMochidome, TTadano, KFukuroda, TOhta, HOkamoto, O 2-Cyclohexylcarbonylbenzimidazoles as potent, orally available and brain-penetrable opioid receptor-like 1 (ORL1) antagonists. Bioorg Med Chem Lett 19:3096-9 (2009) [PubMed]  Article 
Target
Name:
Nociceptin receptor
Synonyms:
KOR-3 | Kappa-type 3 opioid receptor | Mu-type opioid receptor (Mu) | NOP | Nociceptin Receptor (ORL1 Receptor) | Nociceptin receptor (NOP) | Nociceptin receptor (ORL-1) | Nociceptin receptor (ORL1) | Nociceptin/Orphanin FQ, NOP receptor | OOR | OPIATE ORL-1 | OPRL1 | OPRL1 protein | OPRX_HUMAN | ORL1 | ORL1 receptor | Opioid receptor like-1 | Orphanin FQ receptor | Orphanin FQ receptor (ORL1) | P41146
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
40702.87
Organism:
Homo sapiens (Human)
Description:
P41146
Residue:
370
Sequence:
MEPLFPAPFWEVIYGSHLQGNLSLLSPNHSLLPPHLLLNASHGAFLPLGLKVTIVGLYLAVCVGGLLGNCLVMYVILRHTKMKTATNIYIFNLALADTLVLLTLPFQGTDILLGFWPFGNALCKTVIAIDYYNMFTSTFTLTAMSVDRYVAICHPIRALDVRTSSKAQAVNVAIWALASVVGVPVAIMGSAQVEDEEIECLVEIPTPQDYWGPVFAICIFLFSFIVPVLVISVCYSLMIRRLRGVRLLSGSREKDRNLRRITRLVLVVVAVFVGCWTPVQVFVLAQGLGVQPSSETAVAILRFCTALGYVNSCLNPILYAFLDENFKACFRKFCCASALRRDVQVSDRVRSIAKDVALACKTSETVPRPA
  
Inhibitor
Name:
BDBM29992
Synonyms:
2-Cyclohexylcarbonylbenzimidazole, 7c
Type:
Small organic molecule
Emp. Form.:
C22H31ClN4O2
Mol. Mass.:
418.96
SMILES:
CCN1CCN(CC1)c1cc2[nH]c(nc2cc1Cl)C(=O)[C@]1(C)CC[C@@](C)(O)CC1 |r,wU:20.23,24.28,wD:20.22,24.27,(-10.04,.77,;-8.71,,;-7.38,.77,;-7.38,2.31,;-6.04,3.08,;-4.71,2.31,;-4.71,.77,;-6.04,,;-3.38,3.08,;-2.04,2.31,;-.71,3.08,;.76,2.6,;1.66,3.85,;.76,5.1,;-.71,4.62,;-2.04,5.39,;-3.38,4.62,;-4.71,5.39,;3.2,3.85,;3.97,5.18,;4.29,2.76,;4.84,4.2,;5.83,2.84,;6.66,1.54,;5.96,.17,;5.96,-1.37,;7.45,-.23,;4.42,.1,;3.59,1.39,)|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM29961
Synonyms:
[125I]Tyr14-NC/OFQ | [125I]Tyr14-Nociceptin
Type:
radiolabeled substrate
Emp. Form.:
n/a
Mol. Mass.:
n/a
SMILES:
n/a
Structure: