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 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]
