compound 46 [PMID: 25268943] [Ligand Id: 11235] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3361425
  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
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  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
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  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
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  • NPFF1 receptor/Neuropeptide FF receptor 1 in Human [ChEMBL: CHEMBL5951] [GtoPdb: 300] [UniProtKB: Q9GZQ6]
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  • NPFF2 receptor/Neuropeptide FF receptor 2 in Human [ChEMBL: CHEMBL5952] [GtoPdb: 301] [UniProtKB: Q9Y5X5]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
ChEMBL Displacement of [3H]DPDPE from human DOR expressed in HEK293 cells after 60 mins by scintillation counting analysis B 5.6 pKi 2486 nM Ki J. Med. Chem. (2014) 57: 8903-8927 [PMID:25268943]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Displacement of [3H]U-69593 from human KOR expressed in HEK293 cells after 60 mins by scintillation counting analysis B 6.65 pKi 224 nM Ki J. Med. Chem. (2014) 57: 8903-8927 [PMID:25268943]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Displacement of [3H]DAMGO from human MOR expressed in HEK293 cells after 60 mins by scintillation counting analysis B 6.7 pKi 201 nM Ki J. Med. Chem. (2014) 57: 8903-8927 [PMID:25268943]
NPFF1 receptor/Neuropeptide FF receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5951] [GtoPdb: 300] [UniProtKB: Q9GZQ6]
GtoPdb Binding affinity. - 7.09 pKi 81 nM Ki J Med Chem (2014) 57: 8903-27 [PMID:25268943]
ChEMBL Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis B 7.09 pKi 81 nM Ki J. Med. Chem. (2014) 57: 8903-8927 [PMID:25268943]
ChEMBL Antagonist activity at human NPFF1 receptor expressed in CHO cells assessed as reversal of NPVF-induced inhibition of intracellular cAMP accumulation after 10 mins by liquid scintillation counting analysis relative to control F 5.45 pEC50 3520 nM EC50 J. Med. Chem. (2014) 57: 8903-8927 [PMID:25268943]
NPFF2 receptor/Neuropeptide FF receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5952] [GtoPdb: 301] [UniProtKB: Q9Y5X5]
ChEMBL Displacement of [3H]EYF from human NPFF2 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis B 5.85 pKi 1426 nM Ki J. Med. Chem. (2014) 57: 8903-8927 [PMID:25268943]
GtoPdb Binding affinity. - 5.85 pKi 1426 nM Ki J Med Chem (2014) 57: 8903-27 [PMID:25268943]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]