AR-M1000390 [Ligand Id: 9005] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL415521
  • 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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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]
GtoPdb - - 6.97 pKi 106 nM Ki Life Sci (2003) 73: 1691-704 [PMID:12875901]
GtoPdb - - 9.05 pIC50 0.89 nM IC50 WO2006124687 A1. Opioid receptor subtype-selective agents. (2006)
ChEMBL Binding affinity on cloned opioid receptor delta 1 in human HEK293S cells using [125I]-[D-Ala2]-deltorphin II as radioligand. B 9.06 pIC50 0.87 nM IC50 J Med Chem (2000) 43: 3895-3905 [PMID:11052794]
ChEMBL Effective concentration as delta agonist potency using [35S]GTP-gamma-S binding assay. F 8.14 pEC50 7.2 nM EC50 J Med Chem (2000) 43: 3895-3905 [PMID:11052794]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Binding affinity on cloned opioid receptor kappa 1 in human HEK293S cells using [125I]-D-Pro10-dynorphin A[1-11] as radioligand. B 5.13 pIC50 7470 nM IC50 J Med Chem (2000) 43: 3895-3905 [PMID:11052794]
GtoPdb - - 5.13 pIC50 7470 nM IC50 WO2006124687 A1. Opioid receptor subtype-selective agents. (2006)
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
GtoPdb - - 5.42 pIC50 3800 nM IC50 WO2006124687 A1. Opioid receptor subtype-selective agents. (2006)
ChEMBL Binding affinity on cloned opioid receptor mu 1 in human HEK293S cells using [125I]FK33824 as radioligand. B 5.42 pIC50 3800 nM IC50 J Med Chem (2000) 43: 3895-3905 [PMID:11052794]

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]