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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 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]