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ChEMBL ligand: CHEMBL1921847 (Aticaprant, Cerc-501, CERC-501, Jnj-67953964, JNJ-67953964-AAA, JSPA-0658, JSPA0658, Ly2456302, LY-2456302, LY2456302) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] | ||||||||
ChEMBL | Displacement of [3H]diprenorphine from human opioid delta receptor expressed in HEK293 cells after 120 mins by scintillation counting | B | 6.78 | pKi | 166 | nM | Ki | J Med Chem (2011) 54: 8000-8012 [PMID:21958337] |
GtoPdb | - | - | 6.81 | pKi | 155 | nM | Ki | Neuropharmacology (2014) 77: 131-44 [PMID:24071566] |
ChEMBL | Binding affinity to human cloned DOR in presence of Na+/GDP | B | 6.91 | pKi | 122 | nM | Ki | J Med Chem (2013) 56: 2178-2195 [PMID:23360448] |
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
ChEMBL | Displacement of [3H]diprenorphine from human opioid kappa receptor expressed in CHO cells after 120 mins by scintillation counting | B | 9.02 | pKi | 0.95 | nM | Ki | J Med Chem (2011) 54: 8000-8012 [PMID:21958337] |
GtoPdb | - | - | 9.09 | pKi | 0.81 | nM | Ki | Neuropharmacology (2014) 77: 131-44 [PMID:24071566] |
ChEMBL | Antagonist activity at kappa opioid receptor (unknown origin) | B | 9.1 | pKi | 0.8 | nM | Ki | Eur J Med Chem (2015) 90: 742-750 [PMID:25513968] |
ChEMBL | Binding affinity to human cloned KOR in presence of Na+/GDP | B | 9.22 | pKi | 0.6 | nM | Ki | J Med Chem (2013) 56: 2178-2195 [PMID:23360448] |
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
GtoPdb | - | - | 7.62 | pKi | 24 | nM | Ki | Neuropharmacology (2014) 77: 131-44 [PMID:24071566] |
ChEMBL | Displacement of [3H]diprenorphine from human opioid mu receptor expressed in CHO cells after 120 mins by scintillation counting | B | 7.64 | pKi | 22.7 | nM | Ki | J Med Chem (2011) 54: 8000-8012 [PMID:21958337] |
ChEMBL | Binding affinity to human cloned MOR in presence of Na+/GDP | B | 7.79 | pKi | 16.4 | nM | Ki | J Med Chem (2013) 56: 2178-2195 [PMID:23360448] |
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]