QA1 [Ligand Id: 5815] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1210313
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
NPS receptor/Neuropeptide S receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5162] [GtoPdb: 302] [UniProtKB: Q6W5P4]
ChEMBL Antagonist activity at human recombinant NPS receptor expressed in CHOK1 cells assessed as inhibition of NPS-induced calcium mobilization by FLIPR assay F 6.11 pIC50 785 nM IC50 Bioorg Med Chem Lett (2010) 20: 4700-4703 [PMID:20510609]
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 7.26 pIC50 55 nM IC50 J Med Chem (2013) 56: 9045-9056 [PMID:24171469]
ChEMBL Antagonist activity at human recombinant NPS receptor expressed in CHOK1 cells assessed as inhibition of NPS-induced calcium mobilization by FLIPR assay F 7.64 pIC50 23 nM IC50 Bioorg Med Chem Lett (2010) 20: 4700-4703 [PMID:20510609]
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 7.96 pIC50 11 nM IC50 J Med Chem (2013) 56: 9045-9056 [PMID:24171469]
GtoPdb - - 8 pIC50 - - - Bioorg Med Chem Lett (2010) 20: 4700-3 [PMID:20510609]
ChEMBL Antagonist activity at human recombinant NPS receptor expressed in CHOK1 cells assessed as inhibition of NPS-induced calcium mobilization by FLIPR assay F 8 pIC50 10 nM IC50 Bioorg Med Chem Lett (2010) 20: 4700-4703 [PMID:20510609]
ChEMBL Antagonist activity at neuropeptide S receptor (unknown origin) assessed as intracellular calcium level by cell based assay F 8 pIC50 10 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 8.17 pIC50 6.7 nM IC50 J Med Chem (2013) 56: 9045-9056 [PMID:24171469]
ChEMBL Displacement of [125I]Tyr10-NPS from neuropeptide S receptor (unknown origin) 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 cAMP level after 30 mins by phosphate-buffered saline assay F 8.92 pIC50 1.2 nM IC50 J Med Chem (2013) 56: 9045-9056 [PMID:24171469]
NPS receptor/Neuropeptide S receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3308949] [GtoPdb: 302] [UniProtKB: P0C0L6]
ChEMBL Displacement of [125I]NPS from NPS receptor in rat brain superior coliculus after 30 mins B 5.84 pIC50 1440 nM IC50 Bioorg Med Chem Lett (2010) 20: 4700-4703 [PMID:20510609]
ChEMBL Displacement of [125I]NPS from NPS receptor in rat brain superior coliculus after 30 mins B 5.85 pEC50 1400 nM EC50 Bioorg Med Chem Lett (2010) 20: 4700-4703 [PMID:20510609]
ChEMBL Displacement of [3H]quinolinone from rat NPS receptor B 8.89 pEC50 1.3 nM EC50 Bioorg Med Chem Lett (2010) 20: 4700-4703 [PMID:20510609]

ChEMBL data shown on this page come from version 32:

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]