UFP-505 [Ligand Id: 9838] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL458631 |
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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 | - | - | 9.82 | pKi | - | - | - |
Br J Anaesth (2012) 108: 262-70 [PMID:22194444]; Br J Pharmacol (2018) 175: 2881-2896 [PMID:29524334] |
| ChEMBL | Binding affinity to delta opioid receptor | B | 10.51 | pKi | 0.03 | nM | Ki | J Med Chem (2006) 49: 3990-3993 [PMID:16789756] |
| δ receptor/Delta opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300] | ||||||||
| ChEMBL | Negative logarithm of the molar concentration required to double the agonist concentration to achieve the original response in mu receptor from mouse vas deferens (MVD) | F | 9.25 | pKd | 0.56 | nM | Kd | J Med Chem (2002) 45: 713-720 [PMID:11806723] |
| ChEMBL | Antagonist activity at delta opioid receptor in mouse vas deferens assessed as effect on deltorphin 2-induced response | F | 9.25 | pKd | 0.56 | nM | Kd | J Med Chem (2008) 51: 5109-5117 [PMID:18680274] |
| ChEMBL | Antagonist activity at delta opioid receptor in mouse assessed as effect on electrically evoked vas-deferens contraction by MVD test | F | 9.3 | pKd | 0.5 | nM | Kd | Bioorg Med Chem Lett (2009) 19: 433-437 [PMID:19062273] |
| ChEMBL | Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction | F | 8.57 | pIC50 | 2.69 | nM | IC50 | J Med Chem (2008) 51: 5109-5117 [PMID:18680274] |
| δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533] | ||||||||
| ChEMBL | Binding affinity at Opioid receptor delta 1 using rat brain receptor (P2 synaptosome) assay | B | 10.51 | pKi | 0.03 | nM | Ki | J Med Chem (2002) 45: 713-720 [PMID:11806723] |
| ChEMBL | Displacement of [3H]deltorphin2 from delta opioid receptor in Sprague-Dawley rat brain P2 synaptosomal membrane | B | 10.51 | pKi | 0.03 | nM | Ki | J Med Chem (2008) 51: 5109-5117 [PMID:18680274] |
| ChEMBL | Displacement of [3H]DPDPE from delta opioid receptor in Sprague-Dawley rat brain synaptosomal membranes | B | 10.51 | pKi | 0.03 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 433-437 [PMID:19062273] |
| μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| GtoPdb | - | - | 7.79 | pKi | - | - | - |
Br J Anaesth (2012) 108: 262-70 [PMID:22194444]; Br J Pharmacol (2018) 175: 2881-2896 [PMID:29524334] |
| ChEMBL | Binding affinity to mu opioid receptor | B | 9.8 | pKi | 0.16 | nM | Ki | J Med Chem (2006) 49: 3990-3993 [PMID:16789756] |
| μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535] | ||||||||
| ChEMBL | Binding affinity for rat brain P2 synaptosome Opioid receptor mu 1 | B | 9.8 | pKi | 0.16 | nM | Ki | J Med Chem (2002) 45: 713-720 [PMID:11806723] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in Sprague-Dawley rat brain P2 synaptosomal membrane | B | 9.8 | pKi | 0.16 | nM | Ki | J Med Chem (2008) 51: 5109-5117 [PMID:18680274] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in Sprague-Dawley rat brain synaptosomal membranes | B | 9.8 | pKi | 0.16 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 433-437 [PMID:19062273] |
| Mu opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266] | ||||||||
| ChEMBL | Agonist activity at mu opioid receptor by guinea pig ileum assay | F | 8.57 | pIC50 | 2.69 | nM | IC50 | J Med Chem (2006) 49: 3990-3993 [PMID:16789756] |
| ChEMBL | Agonist activity at mu opioid receptor in Hartley guinea pig assessed as inhibition of electrically evoked ileum contraction by GPI test | F | 8.57 | pIC50 | 2.69 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 433-437 [PMID:19062273] |
| ChEMBL | Negative logarithm of the molar concentration of an agonist to produce 50% of the maximum effect in guinea pig ileum (mu receptor) determined by Salvadori et al. | F | 8.57 | pEC50 | 2.69 | nM | EC50 | J Med Chem (2002) 45: 713-720 [PMID:11806723] |
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]
