SCH221510 [Ligand Id: 8868] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL513136
  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
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  • GPR183/G-protein coupled receptor 183 in Human [ChEMBL: CHEMBL3259470] [GtoPdb: 81] [UniProtKB: P32249]
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  • H2 receptor/Histamine H2 receptor in Human [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
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  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
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  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
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  • NOP receptor/Nociceptin receptor in Human [ChEMBL: CHEMBL2014] [GtoPdb: 320] [UniProtKB: P41146]
  • NOP receptor in Mouse [GtoPdb: 320] [UniProtKB: P35377]
  • NOP receptor in Rat [GtoPdb: 320] [UniProtKB: P35370]
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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]
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]