oliceridine [Ligand Id: 7334] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2443262 (Oliceridina, Oliceridine, Olinvyk, Olynvik, TRV-130, TRV130) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] | ||||||||
| ChEMBL | Agonist activity at human delta opioid receptor expressed in HEK293 assessed as increase in calcium mobilization incubated for 60 mins by FLIPR assay | F | 5 | pEC50 | >10000 | nM | EC50 | Eur J Med Chem (2022) 228: 113986-113986 [PMID:34802839] |
| ChEMBL | Agonist activity at human delta opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay | F | 5.55 | pEC50 | 2800 | nM | EC50 | J Med Chem (2013) 56: 8019-8031 [PMID:24063433] |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Displacement of [3H]N-methylspiperone from human D2L receptor expressed in HEK293T cell membrane assessed as inhibition constant incubated for 60 mins by MicroBeta scintillation counting method | B | 4.08 | pKi | 83200 | nM | Ki | J Med Chem (2023) 66: 10304-10341 [PMID:37467430] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | Displacement of [3H]N-methylspiperone from human D3R receptor expressed in HEK293T cell membrane assessed as inhibition constant incubated for 60 mins by MicroBeta scintillation counting method | B | 5.16 | pKi | 6860 | nM | Ki | J Med Chem (2023) 66: 10304-10341 [PMID:37467430] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG channel expressed in HEK293 cells by whole-cell patch clamp technique | B | 5.21 | pIC50 | 6200 | nM | IC50 | J Med Chem (2013) 56: 8019-8031 [PMID:24063433] |
| κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in HEK293 assessed as increase in calcium mobilization incubated for 60 mins by FLIPR assay | F | 5 | pEC50 | >10000 | nM | EC50 | Eur J Med Chem (2022) 228: 113986-113986 [PMID:34802839] |
| ChEMBL | Agonist activity at human kappa opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay | F | 5.85 | pEC50 | 1400 | nM | EC50 | J Med Chem (2013) 56: 8019-8031 [PMID:24063433] |
| μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| ChEMBL | Binding affinity to human mu opioid receptor by radio-ligand binding assay | B | 8.22 | pKi | 6 | nM | Ki | J Med Chem (2013) 56: 8019-8031 [PMID:24063433] |
| ChEMBL | Displacement of [3H]-DAMGO from human MOR receptor expressed in HEK293T cell membrane assessed as inhibition constant incubated for 60 mins by MicroBeta scintillation counting method | B | 8.36 | pKi | 4.38 | nM | Ki | J Med Chem (2023) 66: 10304-10341 [PMID:37467430] |
| ChEMBL | Displacement of [3H]-Diprenorphine from human mu opiod receptor expressed in CHO cells incubated for 1 hr by competition binding assay | B | 8.84 | pKi | 1.46 | nM | Ki | Eur J Med Chem (2022) 228: 113986-113986 [PMID:34802839] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as beta-arrestin recruitment by chemiluminescence assay | B | 7.3 | pEC50 | 50.12 | nM | EC50 | J Med Chem (2013) 56: 8019-8031 [PMID:24063433] |
| ChEMBL | Agonist activity at mu opioid receptor (unknown origin) assessed as beta arrestin-2 recruitment incubated for 3 days by PathHunter assay | F | 7.92 | pEC50 | 12 | nM | EC50 | Eur J Med Chem (2022) 228: 113986-113986 [PMID:34802839] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay | F | 8.1 | pEC50 | 8 | nM | EC50 | J Med Chem (2013) 56: 8019-8031 [PMID:24063433] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay | F | 8.1 | pEC50 | 7.94 | nM | EC50 | J Med Chem (2013) 56: 8019-8031 [PMID:24063433] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in HEK293 assessed as increase in calcium mobilization incubated for 60 mins by FLIPR assay | F | 8.17 | pEC50 | 6.7 | nM | EC50 | Eur J Med Chem (2022) 228: 113986-113986 [PMID:34802839] |
| ChEMBL | Agonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometry | F | 8.74 | pEC50 | 1.8 | nM | EC50 | Eur J Med Chem (2022) 228: 113986-113986 [PMID:34802839] |
| μ receptor/Mu opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866] | ||||||||
| ChEMBL | Partial agonist activity at Rluc8 fused mouse MOR transfected in HEK293T cells assessed as Nb33 recruitment using coelenterazine as substrate incubated for 40 mins by BRET assay | F | 7.23 | pEC50 | 58.88 | nM | EC50 | J Med Chem (2023) 66: 10304-10341 [PMID:37467430] |
| ChEMBL | Partial agonist activity at Rluc8 fused mouse MOR transfected in HEK293T cells assessed as Nb33 recruitment using coelenterazine as substrate incubated for 40 mins by BRET assay | F | 7.23 | pEC50 | 58.5 | nM | EC50 | J Med Chem (2023) 66: 10304-10341 [PMID:37467430] |
| ChEMBL | Partial agonist activity at Rluc8 fused mouse MOR transfected in HEK293T cells coexpressing wild type GRK2 assessed as arrestin-3 recruitment using coelenterazine as substrate incubated for 40 mins by BRET assay | F | 7.49 | pEC50 | 32.5 | nM | EC50 | J Med Chem (2023) 66: 10304-10341 [PMID:37467430] |
| ChEMBL | Partial agonist activity at Rluc8 fused mouse MOR transfected in HEK293T cells coexpressing wild type GRK2 assessed as arrestin-3 recruitment using coelenterazine as substrate incubated for 40 mins by BRET assay | F | 7.49 | pEC50 | 32.36 | nM | EC50 | J Med Chem (2023) 66: 10304-10341 [PMID:37467430] |
| ChEMBL | Partial agonist activity at SNAP-tagged mouse MOR transfected in HEK293T cells coexpressing wild type Galpha-i2, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-i2 activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay | F | 8.62 | pEC50 | 2.4 | nM | EC50 | J Med Chem (2023) 66: 10304-10341 [PMID:37467430] |
| ChEMBL | Partial agonist activity at SNAP-tagged mouse MOR transfected in HEK293T cells coexpressing wild type Galpha-i2, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-i2 activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay | F | 8.62 | pEC50 | 2.4 | nM | EC50 | J Med Chem (2023) 66: 10304-10341 [PMID:37467430] |
| Nav1.5/Sodium channel protein type V alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524] | ||||||||
| ChEMBL | Inhibition of human Nav 1.5 tonic ion channel expressed in HEK293 cells by whole-cell patch clamp technique | B | 4.78 | pIC50 | 16500 | nM | IC50 | J Med Chem (2013) 56: 8019-8031 [PMID:24063433] |
| ChEMBL | Inhibition of human Nav 1.5 phasic ion channel expressed in HEK293 cells by whole-cell patch clamp technique | B | 5.33 | pIC50 | 4700 | nM | IC50 | J Med Chem (2013) 56: 8019-8031 [PMID:24063433] |
| Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936] | ||||||||
| ChEMBL | Inhibition of human Cav 1.2 ion channel expressed in HEK293 cells by whole-cell patch clamp technique | B | 4.44 | pIC50 | 36000 | nM | IC50 | J Med Chem (2013) 56: 8019-8031 [PMID:24063433] |
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]
