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ChEMBL ligand: CHEMBL1474387 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]