UFP-505 [Ligand Id: 9838] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL458631
  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
  • δ receptor/Delta opioid receptor in Mouse [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300]
  • δ receptor/Delta opioid receptor in Rat [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
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  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
  • μ receptor/Mu opioid receptor in Rat [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
  • Mu opioid receptor in Guinea pig [ChEMBL: CHEMBL4354] [UniProtKB: P97266]
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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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]