MCOPPB [Ligand Id: 12419] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL481512
  • 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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  • NOP receptor/Nociceptin receptor in Human [ChEMBL: CHEMBL2014] [GtoPdb: 320] [UniProtKB: P41146]
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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 delta opioid receptor expressed in CHOK1 cells B 6.18 pKi >667 nM Ki J Med Chem (2009) 52: 610-625 [PMID:19125610]
ChEMBL Agonist activity at human delta opioid receptor expressed in CHOK1 cells by [35S]GTPgammaS binding F 5.33 pEC50 4696 nM EC50 J Med Chem (2009) 52: 610-625 [PMID:19125610]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Displacement of [3H]enadoline from human kappa opioid receptor expressed in HEK293 cells B 7.64 pKi 23.1 nM Ki J Med Chem (2009) 52: 610-625 [PMID:19125610]
ChEMBL Agonist activity at human kappa opioid receptor expressed in HEK293 cells by [35S]GTPgammaS binding F 7.1 pEC50 80 nM EC50 J Med Chem (2009) 52: 610-625 [PMID:19125610]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHOK1 cells B 8.98 pKi 1.05 nM Ki J Med Chem (2009) 52: 610-625 [PMID:19125610]
ChEMBL Agonist activity at human mu opioid receptor expressed in CHOK1 cells by [35S]GTPgammaS binding F 7.47 pEC50 34 nM EC50 J Med Chem (2009) 52: 610-625 [PMID:19125610]
NOP receptor/Nociceptin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2014] [GtoPdb: 320] [UniProtKB: P41146]
ChEMBL Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells B 10.07 pKi 0.09 nM Ki J Med Chem (2009) 52: 610-625 [PMID:19125610]
GtoPdb Binding affinity for hNOP - 10.07 pKi 0.09 nM Ki J Med Chem (2009) 52: 610-25 [PMID:19125610]
ChEMBL Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding F 9.41 pEC50 0.39 nM EC50 J Med Chem (2009) 52: 610-625 [PMID:19125610]
GtoPdb Potency determined in a functional assay; [35S]GTPγS recruitment - 9.41 pEC50 0.39 nM EC50 J Med Chem (2009) 52: 610-25 [PMID:19125610]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]