SRI22141 [Ligand Id: 11694] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2179656
  • 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 Binding affinity - 8.29 pKi 5.1 nM Ki J Pain (2020) 21: 146-160 [PMID:31201990]
ChEMBL Displacement of [3H]DADLE from human delta opioid receptor expressed in CHO cells by scintillation counting analysis B 8.98 pKi 1.04 nM Ki J Med Chem (2012) 55: 8350-8363 [PMID:23016952]
GtoPdb Potency in a 35S-GTPγS assay - 8.89 pEC50 1.3 nM EC50 J Pain (2020) 21: 146-160 [PMID:31201990]
ChEMBL Agonist activity at delta opioid receptor expressed in rat/mouse NG108-15 cells assessed as [35S]GTPgammaS binding by scintillation counting analysis F 9.57 pEC50 0.27 nM EC50 J Med Chem (2012) 55: 8350-8363 [PMID:23016952]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Displacement of [3H]U69,593 from human kappa opioid receptor expressed in CHO cells by scintillation counting analysis B 8.82 pKi 1.53 nM Ki J Med Chem (2012) 55: 8350-8363 [PMID:23016952]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
GtoPdb Binding affinity - 7.71 pKi 19.7 nM Ki J Pain (2020) 21: 146-160 [PMID:31201990]
ChEMBL Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cells by scintillation counting analysis B 9.27 pKi 0.54 nM Ki J Med Chem (2012) 55: 8350-8363 [PMID:23016952]
ChEMBL Agonist activity at human mu opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting analysis F 8.67 pEC50 2.15 nM EC50 J Med Chem (2012) 55: 8350-8363 [PMID:23016952]
GtoPdb Potency in a 35S-GTPγS assay - 9.7 pEC50 0.2 nM EC50 J Pain (2020) 21: 146-160 [PMID:31201990]

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]