eluxadoline [Ligand Id: 7691] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2159122 (Eluxadolina, Eluxadoline, JNJ-27018966, Truberzi, Viberzi) |
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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 delta opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assay | F | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 4869-4872 [PMID:22695132] |
| δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533] | ||||||||
| ChEMBL | Binding affinity to rat delta opioid receptor | B | 8.89 | pKi | 1.3 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 4869-4872 [PMID:22695132] |
| GtoPdb | - | - | 8.89 | pKi | 1.3 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 4869-72 [PMID:22695132] |
| Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144] | ||||||||
| ChEMBL | Binding affinity to guinea pig kappa opioid receptor | B | 7.26 | pKi | 55 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 4869-4872 [PMID:22695132] |
| ChEMBL | Agonist activity at kappa opioid receptor guinea pig colon tissue | F | 5.8 | pEC50 | 1600 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 4869-4872 [PMID:22695132] |
| μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| GtoPdb | - | - | 8.77 | pKi | 1.7 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 4869-72 [PMID:22695132] |
| ChEMBL | Agonist activity at mu opioid receptor expressed in CHO-hg cells by [35S]-GTPgammaS binding assay | F | 9 | pEC50 | 1 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 4869-4872 [PMID:22695132] |
| μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535] | ||||||||
| ChEMBL | Binding affinity to rat mu opioid receptor | B | 9.05 | pKi | 0.9 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 4869-4872 [PMID:22695132] |
| GtoPdb | - | - | 9.05 | pKi | 0.9 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 4869-72 [PMID:22695132] |
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]
