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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 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]