Reaction Details |
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Target | Nociceptin receptor |
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Ligand | BDBM29984 |
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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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IC50 | 9.3±n/a nM |
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EC50 | 4.5±n/a nM |
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Citation | Kobayashi, K; Uchiyama, M; Ito, H; Takahashi, H; Yoshizumi, T; Sakoh, H; Nagatomi, Y; Asai, M; Miyazoe, H; Tsujita, T; Hirayama, M; Ozaki, S; Tani, T; Ishii, Y; Ohta, H; Okamoto, O Discovery of novel arylpyrazole series as potent and selective opioid receptor-like 1 (ORL1) antagonists. Bioorg Med Chem Lett19:3627-31 (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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BDBM29984 |
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BDBM29961 |
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Name | BDBM29984 |
Synonyms: | arylpyrazole, 29 |
Type | Small organic molecule |
Emp. Form. | C21H22ClF2N5 |
Mol. Mass. | 417.883 |
SMILES | Cc1c(CNC2CCC(F)(F)C2)nn(c1-c1ccc(C)nc1)-c1ncccc1Cl |
Structure |
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