cebranopadol [Ligand Id: 8866] activity data from GtoPdb and ChEMBL
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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 |
|---|---|---|---|---|---|---|---|---|
| δ receptor/Delta-type opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] | ||||||||
| GtoPdb | Radioligand binding assay | - | 7.74 | pKi | 18 | nM | Ki | J Pharmacol Exp Ther (2014) 349: 535-48 [PMID:24713140] |
| ChEMBL | Agonist activity at human DOR expressed in CHO-K1 cells assessed as decrease in cAMP level incubated for 30 mins in presence of forskolin by HitHunter cAMP analysis | F | 8.42 | pIC50 | 3.77 | nM | IC50 | J Med Chem (2024) 67: 9173-9193 [PMID:38810170] |
| κ receptor/Kappa-type opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [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] |
| ChEMBL | Agonist activity at human KOR expressed in CHO-K1 cells assessed as decrease in cAMP level incubated for 30 mins in presence of forskolin by HitHunter cAMP analysis | F | 6.78 | pEC50 | 166.02 | nM | EC50 | J Med Chem (2024) 67: 9173-9193 [PMID:38810170] |
| 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] |
| μ receptor/Mu-type 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 human MOR expressed in CHO-K1 cells assessed as decrease in beta-arrestin 2 recruitment incubated for 90 mins by HitHunter cAMP analysis | F | 7.95 | pEC50 | 11.28 | nM | EC50 | J Med Chem (2024) 67: 9173-9193 [PMID:38810170] |
| 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] |
| ChEMBL | Agonist activity at human MOR expressed in CHO-K1 cells assessed as decrease in cAMP level incubated for 30 mins in presence of forskolin by HitHunter cAMP analysis | F | 9.49 | pEC50 | 0.32 | nM | EC50 | J Med Chem (2024) 67: 9173-9193 [PMID:38810170] |
| 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 human NOR expressed in CHO-K1 cells assessed as decrease in cAMP level incubated for 30 mins in presence of forskolin by HitHunter cAMP analysis | F | 7.34 | pEC50 | 45.46 | nM | EC50 | J Med Chem (2024) 67: 9173-9193 [PMID:38810170] |
| 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] |
ChEMBL data shown on this page come from version 36:
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]
