cebranopadol [Ligand Id: 8866] 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: CHEMBL2364605 (Cebranopadol, GRT-6005, GRT6005)
  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
  • μ receptor in Rat [GtoPdb: 319] [UniProtKB: P33535]
There should be some charts here, you may need to enable JavaScript!
  • NOP receptor/Nociceptin receptor in Human [ChEMBL: CHEMBL2014] [GtoPdb: 320] [UniProtKB: P41146]
  • NOP receptor in Rat [GtoPdb: 320] [UniProtKB: P35370]
There should be some charts here, you may need to enable JavaScript!
  • δ receptor in Human [GtoPdb: 317] [UniProtKB: P41143]
There should be some charts here, you may need to enable JavaScript!
  • κ receptor in Human [GtoPdb: 318] [UniProtKB: P41145]
  • κ receptor in Rat [GtoPdb: 318] [UniProtKB: P34975]
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
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
GtoPdb Radioligand binding assay - 9.15 pKi 0.7 nM Ki J Pharmacol Exp Ther (2014) 349: 535-48 [PMID:24713140]
ChEMBL Displacement of [N-allyl-2,3-3H]naloxone from recombinant human mu opioid receptor expressed in CHOK1 cell membranes after 90 mins by scintillation counting method B 9.15 pKi 0.7 nM Ki J Med Chem (2016) 59: 7011-7028 [PMID:26878436]
ChEMBL Agonist activity at recombinant human mu opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assay B 8.92 pEC50 1.2 nM EC50 J Med Chem (2016) 59: 7011-7028 [PMID:26878436]
μ receptor in Rat [GtoPdb: 319] [UniProtKB: P33535]
GtoPdb Radioligand binding assay - 8.62 pKi 2.4 nM Ki J Pharmacol Exp Ther (2014) 349: 535-48 [PMID:24713140]
NOP receptor/Nociceptin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2014] [GtoPdb: 320] [UniProtKB: P41146]
ChEMBL Displacement of [leucyl-3H]nociceptin from human nociceptin opioid receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting method B 9.05 pKi 0.9 nM Ki J Med Chem (2016) 59: 7011-7028 [PMID:26878436]
GtoPdb Radioligand binding assay - 9.05 pKi 0.9 nM Ki J Pharmacol Exp Ther (2014) 349: 535-48 [PMID:24713140]
ChEMBL Agonist activity at recombinant human nociceptin opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assay B 7.89 pEC50 13 nM EC50 J Med Chem (2016) 59: 7011-7028 [PMID:26878436]
GtoPdb Stimulation of GTP-γ35S binding - 7.89 pEC50 13 nM EC50 J Pharmacol Exp Ther (2014) 349: 535-48 [PMID:24713140]
NOP receptor in Rat [GtoPdb: 320] [UniProtKB: P35370]
GtoPdb Radioligand binding assay - 9 pKi 1 nM Ki J Pharmacol Exp Ther (2014) 349: 535-48 [PMID:24713140]
δ receptor in Human [GtoPdb: 317] [UniProtKB: P41143]
GtoPdb Radioligand binding assay - 7.74 pKi 18 nM Ki J Pharmacol Exp Ther (2014) 349: 535-48 [PMID:24713140]
κ receptor in Human [GtoPdb: 318] [UniProtKB: P41145]
GtoPdb Radioligand binding assay - 8.59 pKi 2.6 nM Ki J Pharmacol Exp Ther (2014) 349: 535-48 [PMID:24713140]
κ receptor in Rat [GtoPdb: 318] [UniProtKB: P34975]
GtoPdb Radioligand binding assay - 7.19 pKi 64 nM Ki J Pharmacol Exp Ther (2014) 349: 535-48 [PMID:24713140]

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]