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ChEMBL ligand: CHEMBL2179656 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]