Reaction Details Report a problem with these data
Target
Nociceptin receptor
Ligand
BDBM29995
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
2.6±n/a nM
EC50
0.65±n/a nM
Citation
Kobayashi, K; Kato, T; Yamamoto, I; Shimizu, A; Mizutani, S; Asai, M; Kawamoto, H; Ito, S; Yoshizumi, T; Hirayama, M; Ozaki, S; Ohta, H; Okamoto, O Optimization of benzimidazole series as opioid receptor-like 1 (ORL1) antagonists: SAR study directed toward improvement of selectivity over hERG activity. Bioorg Med Chem Lett 19:3100-3 (2009) [PubMed] Article
More Info.:
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:
BDBM29995
Synonyms:
CHEMBL494350 | benzimidazole-based antagonist, 1
Type:
Small organic molecule
Emp. Form.:
C18H27ClN4OS
Mol. Mass.:
382.951
SMILES:
C[C@@H]1CN(CCO)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl |r|