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, GRT6005, GRT-6005)
  • 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 32:

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]