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 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]