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ChEMBL ligand: CHEMBL513136 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] | ||||||||
GtoPdb | Radioligand binding assay | - | 5.54 | pKi | 2854 | nM | Ki | J Pharmacol Exp Ther (2008) 326: 672-82 [PMID:18492950] |
ChEMBL | Displacement of [3H]diprenorphine from human delta opioid receptor expressed in CHO cells | B | 5.54 | pKi | 2854 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 2519-2523 [PMID:19339177] |
GPR183/G-protein coupled receptor 183 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3259470] [GtoPdb: 81] [UniProtKB: P32249] | ||||||||
ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183 | F | 5.17 | pIC50 | 6769 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
H2 receptor/Histamine H2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021] | ||||||||
ChEMBL | PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 5.57 | pKi | 2670.85 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
GtoPdb | Radioligand binding assay | - | 6.88 | pKi | 131 | nM | Ki | J Pharmacol Exp Ther (2008) 326: 672-82 [PMID:18492950] |
ChEMBL | Displacement of [3H]diprenorphine from human kappa opioid receptor expressed in CHO cells | B | 6.88 | pKi | 131 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 2519-2523 [PMID:19339177] |
ChEMBL | PDSP Secondary Binding target: OPRK1 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 7.12 | pKi | 76.12 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
ChEMBL | PDSP Secondary Binding target: OPRM1 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 6.49 | pKi | 321 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
ChEMBL | Displacement of [3H]diprenorphine from human mu opioid receptor expressed in CHO cells | B | 7.19 | pKi | 65 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 2519-2523 [PMID:19339177] |
GtoPdb | Radioligand binding assay | - | 7.19 | pKi | 65 | nM | Ki | J Pharmacol Exp Ther (2008) 326: 672-82 [PMID:18492950] |
ChEMBL | Agonist activity at human mu opioid assessed as stimulation of GDP-induced [35S]GTPgammaS binding | F | 6.16 | pEC50 | 693 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 2519-2523 [PMID:19339177] |
NOP receptor/Nociceptin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2014] [GtoPdb: 320] [UniProtKB: P41146] | ||||||||
GtoPdb | Radioligand binding assay | - | 9.52 | pKi | 0.3 | nM | Ki | J Pharmacol Exp Ther (2008) 326: 672-82 [PMID:18492950] |
ChEMBL | Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells | B | 9.52 | pKi | 0.3 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 2519-2523 [PMID:19339177] |
GtoPdb | Stimulation of GTP-γ35S binding | - | 7.92 | pEC50 | 12 | nM | EC50 | J Pharmacol Exp Ther (2008) 326: 672-82 [PMID:18492950] |
ChEMBL | Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding | F | 7.92 | pEC50 | 12 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 2519-2523 [PMID:19339177] |
NOP receptor in Mouse [GtoPdb: 320] [UniProtKB: P35377] | ||||||||
GtoPdb | Radioligand binding assay | - | 8.94 | pKi | 1.15 | nM | Ki | J Pharmacol Exp Ther (2008) 326: 672-82 [PMID:18492950] |
NOP receptor in Rat [GtoPdb: 320] [UniProtKB: P35370] | ||||||||
GtoPdb | Radioligand binding assay | - | 9.38 | pKi | 0.42 | nM | Ki | J Pharmacol Exp Ther (2008) 326: 672-82 [PMID:18492950] |
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]