asimadoline [Ligand Id: 9279] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1190199 (Asimadoline, EMD-61753)
  • 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]
  • κ receptor in Guinea pig [GtoPdb: 318]
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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]
ChEMBL Agonist activity at human delta opioid receptor expressed in COS7 cells after 60 mins IP1 assay B 5.1 pEC50 8000 nM EC50 Bioorg. Med. Chem. Lett. (2015) 25: 887-892 [PMID:25599839]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Agonist activity at human kappa opioid receptor expressed in COS7 cells after 60 mins IP1 assay B 9.3 pEC50 0.5 nM EC50 Bioorg. Med. Chem. Lett. (2015) 25: 887-892 [PMID:25599839]
κ receptor in Guinea pig [GtoPdb: 318]
GtoPdb Displacement of [3H]- 69593 from K opioid receptors from guinea pig cerebellum. - 9 pKi 1 nM Ki Bioorg. Med. Chem. Lett. (1994) 4: 677–682
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Agonist activity at human mu opioid receptor expressed in COS7 cells after 60 mins IP1 assay B 4.22 pEC50 60000 nM EC50 Bioorg. Med. Chem. Lett. (2015) 25: 887-892 [PMID:25599839]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]