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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL415521
  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
There should be some charts here, you may need to enable JavaScript!
  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
There should be some charts here, you may need to enable JavaScript!
  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
There should be some charts here, you may need to enable JavaScript!
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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]