LY2456302 [Ligand Id: 9194] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL1921847 (Aticaprant, Cerc-501, CERC-501, Jnj-67953964, JNJ-67953964-AAA, JSPA-0658, JSPA0658, Ly2456302, LY-2456302, LY2456302)
  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
There should be some charts here, you may need to enable JavaScript!
  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
There should be some charts here, you may need to enable JavaScript!
  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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]