AKST4290 [Ligand Id: 10653] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3670800 (Alk-4290, ALK4290, Alk4290, ALK-4290)
  • CCR3/C-C chemokine receptor type 3 in Human [ChEMBL: CHEMBL3473] [GtoPdb: 60] [UniProtKB: P51677]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]