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 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]