UFP-512 [Ligand Id: 9006] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL442577 (UFP-512)
  • δ receptor in Human [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]
Created with Highcharts 10.3.3ValuesChart context menuδ receptorpKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd MousepKi MousepIC50 MousepEC50 MousepKd RatpKi RatpIC50 RatpEC50 Rat024681012Highcharts.com
  • μ receptor in Human [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]
Created with Highcharts 10.3.3ValuesChart context menuμ receptorpKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd RatpKi RatpIC50 RatpEC50 RatpKd Guinea pigpKi Guinea pigpIC50 GuineapigpEC50 Guineapig0246810Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuMu-opioid receptorpKd Guinea pigpKi Guinea pigpIC50 Guinea pigpEC50 Guinea pig024681012Highcharts.com
  • κ receptor in Human [GtoPdb: 318] [UniProtKB: P41145]
Created with Highcharts 10.3.3ValuesChart context menuκ receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human02468Highcharts.com
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
δ receptor in Human [GtoPdb: 317] [UniProtKB: P41143]
GtoPdb Measuring displacement of [3H]-diprenorphine in vitro - 10.2 pKi - - - Peptides (2008) 29: 93-103 [PMID:18069089]
δ receptor/Delta opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300]
ChEMBL Antagonist activity at delta opioid receptor in mouse vas deferens assessed as effect on deltorphin 2-induced response F 9.9 pKd 0.13 nM Kd J Med Chem (2008) 51: 5109-5117 [PMID:18680274]
ChEMBL Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction F 5.76 pIC50 1724 nM IC50 J Med Chem (2008) 51: 5109-5117 [PMID:18680274]
ChEMBL In vitro inhibitory activity against electrically evoked contractions of in mouse vas deferens (MVD) F 9.92 pIC50 0.12 nM IC50 J Med Chem (2002) 45: 5556-5563 [PMID:12459023]
ChEMBL Agonist activity at delta opioid receptor in mouse vas deference F 9.92 pIC50 0.12 nM IC50 Bioorg Med Chem (2010) 18: 6024-6030 [PMID:20637637]
δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
ChEMBL Inhibition of [3H]DPDPE binding to Opioid receptor delta 1 of rat brain P2 synaptosomes B 9.35 pKi 0.44 nM Ki J Med Chem (2002) 45: 5556-5563 [PMID:12459023]
ChEMBL Displacement of [3H]deltorphin2 from delta opioid receptor in Sprague-Dawley rat brain P2 synaptosomal membrane B 9.35 pKi 0.44 nM Ki J Med Chem (2008) 51: 5109-5117 [PMID:18680274]
ChEMBL Displacement of [3H]deltorphin 2 from delta opioid receptor in Sprague-Dawley rat brain P2 synaptosomal membrane B 9.36 pKi 0.44 nM Ki Bioorg Med Chem (2010) 18: 6024-6030 [PMID:20637637]
μ receptor in Human [GtoPdb: 319] [UniProtKB: P35372]
GtoPdb Measuring displacement of [3H]-diprenorphine in vitro - 8 pKi - - - Peptides (2008) 29: 93-103 [PMID:18069089]
μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
ChEMBL Inhibition of [3H]DAGO binding to Opioid receptor mu 1 of rat brain P2 synaptosomes B 7.27 pKi 53.9 nM Ki J Med Chem (2002) 45: 5556-5563 [PMID:12459023]
ChEMBL Displacement of [3H]DAMGO from mu opioid receptor in Sprague-Dawley rat brain P2 synaptosomal membrane B 7.27 pKi 53.9 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 P2 synaptosomal membrane B 7.27 pKi 53.9 nM Ki Bioorg Med Chem (2010) 18: 6024-6030 [PMID:20637637]
Mu opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266]
ChEMBL In vitro inhibitory activity against electrically evoked contractions of guinea pig ileum (GPI) F 5.76 pIC50 1724 nM IC50 J Med Chem (2002) 45: 5556-5563 [PMID:12459023]
ChEMBL Agonist activity at mu opioid receptor in Hartley guinea pig small intestine F 5.76 pIC50 1724 nM IC50 Bioorg Med Chem (2010) 18: 6024-6030 [PMID:20637637]
Mu-opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5430] [UniProtKB: Q8CGM4]
ChEMBL Agonist activity at mu opioid receptor in Hartley guinea pig ileum myenteric plexus longitudinal muscle assessed as inhibition of electrically-stimulated muscle contraction F 9.92 pIC50 0.12 nM IC50 J Med Chem (2008) 51: 5109-5117 [PMID:18680274]
κ receptor in Human [GtoPdb: 318] [UniProtKB: P41145]
GtoPdb Measuring displacement of [3H]-diprenorphine in vitro - 6.66 pKi - - - Peptides (2008) 29: 93-103 [PMID:18069089]

ChEMBL data shown on this page come from version 35:

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]