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ChEMBL ligand: CHEMBL2364605 (Cebranopadol, GRT-6005, GRT6005) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 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]