Reaction Details |
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Target | Nociceptin receptor |
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Ligand | BDBM29995 |
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Substrate/Competitor | BDBM29961 |
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Meas. Tech. | In Vitro Binding Assay (IC50) and In Vitro Agonism/Antagonism Measurements (EC50/IC50) |
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pH | 7.4±n/a |
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Temperature | 310.15±n/a K |
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IC50 | 2.6±n/a nM |
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EC50 | 0.65±n/a nM |
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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 Lett19:3100-3 (2009) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Nociceptin receptor |
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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: | MEPLFPAPFWEVIYGSHLQGNLSLLSPNHSLLPPHLLLNASHGAFLPLGLKVTIVGLYLA
VCVGGLLGNCLVMYVILRHTKMKTATNIYIFNLALADTLVLLTLPFQGTDILLGFWPFGN
ALCKTVIAIDYYNMFTSTFTLTAMSVDRYVAICHPIRALDVRTSSKAQAVNVAIWALASV
VGVPVAIMGSAQVEDEEIECLVEIPTPQDYWGPVFAICIFLFSFIVPVLVISVCYSLMIR
RLRGVRLLSGSREKDRNLRRITRLVLVVVAVFVGCWTPVQVFVLAQGLGVQPSSETAVAI
LRFCTALGYVNSCLNPILYAFLDENFKACFRKFCCASALRRDVQVSDRVRSIAKDVALAC
KTSETVPRPA
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BDBM29995 |
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BDBM29961 |
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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| |
Structure |
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