NCGC 84 [Ligand Id: 9168] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1474387
  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
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  • NPS receptor/Neuropeptide S receptor in Human [ChEMBL: CHEMBL5162] [GtoPdb: 302] [UniProtKB: Q6W5P4]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Displacement of radiolabeled DAMGO from human recombinant mu opioid receptor expressed in OPRM1 cells B 6.24 pIC50 580 nM IC50 J Med Chem (2013) 56: 9045-9056 [PMID:24171469]
NPS receptor/Neuropeptide S receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5162] [GtoPdb: 302] [UniProtKB: Q6W5P4]
ChEMBL Antagonist activity at neuropeptide S receptor (unknown origin) expressed in CHO cells assessed as cAMP level after 30 mins by phosphate-buffered saline assay F 7.35 pIC50 45 nM IC50 J Med Chem (2013) 56: 9045-9056 [PMID:24171469]
ChEMBL Displacement of [125I]Tyr10-NPS from human neuropeptide S receptor expressed in CHO cells after 1.5 hrs by liquid scintillation counting B 8.46 pIC50 3.5 nM IC50 J Med Chem (2013) 56: 9045-9056 [PMID:24171469]
ChEMBL Antagonist activity at neuropeptide S receptor (unknown origin) expressed in CHO cells assessed as inhibition of NPS-induced ERK activation after 20 mins by HTRF assay B 8.89 pIC50 1.3 nM IC50 J Med Chem (2013) 56: 9045-9056 [PMID:24171469]
ChEMBL Antagonist activity at neuropeptide S receptor (unknown origin) expressed in CHO cells assessed as inhibition of NPS-induced calcium mobilization after 10 mins by fluorescence assay F 9.02 pIC50 0.96 nM IC50 J Med Chem (2013) 56: 9045-9056 [PMID:24171469]
GtoPdb Result from a cAMP accumulation assay. - 8.98 pA2 - - - J Neurosci (2013) 33: 10132-42 [PMID:23761908]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]