J-113397 [Ligand Id: 1691] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL357076 (J-113397)
  • 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]diprenorphine from human cloned delta type opioid receptor expressed in CHO cell membranes by scintillation counter B 6.4 pKi >400 nM Ki J Med Chem (2012) 55: 4955-4967 [PMID:22541041]
ChEMBL Binding affinity in CHO cells stably expressing cloned human Opioid receptor delta 1 by displacing radioligand [3H][D-Ala2,D-Leu5]enkephalin B 5 pIC50 >10000 nM IC50 J Med Chem (1999) 42: 5061-5063 [PMID:10602690]
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]diprenorphine from human cloned kappa type opioid receptor expressed in CHO cell membranes by scintillation counter B 6.4 pKi >400 nM Ki J Med Chem (2012) 55: 4955-4967 [PMID:22541041]
ChEMBL Displacement of [3H]U-69593 from cloned human kappa opioid receptor expressed in CHO cells B 5.8 pIC50 1600 nM IC50 J Med Chem (2006) 49: 847-849 [PMID:16451050]
ChEMBL Binding affinity in CHO cells stably expressing cloned human Opioid receptor kappa 1 by displacing radioligand [3H]U-69593 B 5.85 pIC50 1400 nM IC50 J Med Chem (1999) 42: 5061-5063 [PMID:10602690]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Displacement of [3H]diprenorphine from human cloned mu type opioid receptor expressed in CHO cell membranes by scintillation counter B 6.4 pKi >400 nM Ki J Med Chem (2012) 55: 4955-4967 [PMID:22541041]
ChEMBL Displacement of [3H]diprenorphin from cloned human mu opioid receptor expressed in CHO cells B 5.47 pIC50 3400 nM IC50 J Med Chem (2006) 49: 847-849 [PMID:16451050]
ChEMBL Binding affinity in CHO cells stably expressing cloned human Opioid receptor mu 1 by displacing diprenorphine B 5.66 pIC50 2200 nM IC50 J Med Chem (1999) 42: 5061-5063 [PMID:10602690]
NOP receptor/Nociceptin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2014] [GtoPdb: 320] [UniProtKB: P41146]
ChEMBL Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay B 8.64 pKi 2.3 nM Ki Bioorg Med Chem Lett (2004) 14: 1347-1351 [PMID:14980696]
GtoPdb - - 8.7 pKi - - - Eur J Pharmacol (2000) 402: 45-53 [PMID:10940356]
ChEMBL Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter B 9.39 pKi 0.4 nM Ki J Med Chem (2012) 55: 4955-4967 [PMID:22541041]
ChEMBL Antagonistic activity against nociceptin produced [35S]GTP-gamma-S, binding to Opioid receptor like 1 expressed in CHO cells F 8.25 pIC50 5.6 nM IC50 J Med Chem (1999) 42: 5061-5063 [PMID:10602690]
GtoPdb - - 8.3 pIC50 - - IC50 J Med Chem (1999) 42: 5061-3 [PMID:10602690]
ChEMBL Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells B 8.62 pIC50 2.4 nM IC50 J Med Chem (2006) 49: 847-849 [PMID:16451050]
ChEMBL Binding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptin B 8.64 pIC50 2.3 nM IC50 J Med Chem (1999) 42: 5061-5063 [PMID:10602690]
ChEMBL Displacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cells B 8.64 pIC50 2.3 nM IC50 J Med Chem (2009) 52: 4091-4094 [PMID:19537798]
ChEMBL Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells F 8.82 pIC50 1.5 nM IC50 J Med Chem (2006) 49: 847-849 [PMID:16451050]
ChEMBL Agonistic activity against nociceptin produced GTPgammaS binding to Opioid receptor like 1 expressed in CHO cells B 5 pEC50 >10000 nM EC50 J Med Chem (1999) 42: 5061-5063 [PMID:10602690]
ChEMBL Agonist activity on nociceptin-induced maximal [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells F 5 pEC50 >10000 nM EC50 J Med Chem (2006) 49: 847-849 [PMID:16451050]

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]