UFP-512 [Ligand Id: 9006] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL442577 (UFP-512) |
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| 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 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]
