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 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]