compound 24 [PMID: 16451050] [Ligand Id: 7361] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL201945
  • 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]
  • NOP receptor/Nociceptin receptor in Mouse [ChEMBL: CHEMBL3621] [GtoPdb: 320] [UniProtKB: P35377]
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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]naltrindole from cloned human delta opioid receptor expressed in CHO cells B 5 pIC50 >10000 nM IC50 J Med Chem (2006) 49: 847-849 [PMID:16451050]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Displacement of [3H]U-69593 from cloned human kappa opioid receptor expressed in CHO cells B 5.6 pIC50 2500 nM IC50 J Med Chem (2006) 49: 847-849 [PMID:16451050]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Displacement of [3H]diprenorphin from cloned human mu opioid receptor expressed in CHO cells B 5.17 pIC50 6700 nM IC50 J Med Chem (2006) 49: 847-849 [PMID:16451050]
NOP receptor/Nociceptin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2014] [GtoPdb: 320] [UniProtKB: P41146]
ChEMBL Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells B 9.62 pKi 0.24 nM Ki Bioorg Med Chem (2009) 17: 5080-5095 [PMID:19527931]
GtoPdb - - 9.62 pKi 0.24 nM Ki Eur J Pharmacol (2009) 614: 50-7 [PMID:19445927]
ChEMBL Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells B 9.57 pIC50 0.27 nM IC50 J Med Chem (2006) 49: 847-849 [PMID:16451050]
ChEMBL Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells F 9.82 pIC50 0.15 nM IC50 J Med Chem (2006) 49: 847-849 [PMID:16451050]
GtoPdb - - 10 pIC50 0.1 nM IC50 Eur J Pharmacol (2009) 614: 50-7 [PMID:19445927];
J Med Chem (2006) 49: 847-9 [PMID:16451050]
ChEMBL Agonist activity on nociceptin-induced maximal [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells F 6 pEC50 >1000 nM EC50 J Med Chem (2006) 49: 847-849 [PMID:16451050]
NOP receptor/Nociceptin receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3621] [GtoPdb: 320] [UniProtKB: P35377]
ChEMBL Antagonist activity at nociceptin receptor in Swiss mouse vas deferens assessed as inhibition of electrically evoked twitches F 8.24 pKd 5.75 nM Kd Bioorg Med Chem (2009) 17: 5080-5095 [PMID:19527931]

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]