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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 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]