lazucirnon [Ligand Id: 10653] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3670800 (Akst4290, AKST-4290, AKST4290, ALK-429, ALK429, Alk-4290, Alk4290, ALK-4290, ALK4290, BI144807, Lazucirnon) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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| CCR3/C-C chemokine receptor type 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3473] [GtoPdb: 60] [UniProtKB: P51677] | ||||||||
| GtoPdb | Dissociation constant determined in a scintillation proximity binding assay using recombinant human [125]l-eotaxin-1 as radioligand and cell membranes prepared from K562 cells transfected with hCCR3. | - | 8.49 | pKi | 3.2 | nM | Ki | WO2012045803A1. Co-crystals and salts of ccr3-inhibitors (2012) |
| ChEMBL | Scintillation Proximity Assay: The CCR3 receptor binding assay was performed in a Scintillation Proximity Assay (SPA) design with the radioligand recombinant human 125Iodine-eotaxin-1. Cell membranes of hCCR3 C1 cells were again homogenized by passing through a single use needle (Terumo, 23Gx1'') and diluted in SPA incubation buffer in suitable concentrations (0.5-10 ug protein/well) in 96 well microtiter plates (1450-514, Perkin Elmer). The SPA assay was set up in the SPA incubation buffer with a final volume of 200 ul and final concentration of 25 mM HEPES, 25 mM MgCl2 6H2O, 1 mM CaCl2 2H2O and 0.1% bovine serum albumin. The SPA assay mixture contained 60 ul of the membrane suspension, 80 ul of Wheat Germ Agglutinin coated PVT beads (organic scintillator, GE Healthcare, RPNQ-0001) 0.2 mg/well), 40 ul of recombinant human 125Jodine-eotaxin-1 (Biotrend), diluted in SPA buffer to a final concentration of 30.000 dpm per well. | B | 8.49 | pKi | 3.2 | nM | Ki | US-8742115-B2. Co-crystals and salts of CCR3-inhibitors (2014) |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
