Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compound...

Basic Information

ID: ALA3706065

Type: Binding

Description: Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).

Format: BAO_0000219

Cell type: CHO

Target:  C-C chemokine receptor type 2(ALA4015)

Document:  ALA3638389

BindingDB Source:  6587

Activity Charts

Compound Summary

Parent Molecular WeightALogPPolar Surface Area
508.593.233.23
508.593.233.23
508.593.233.23
508.593.233.23
509.572.632.63
509.572.632.63
522.613.573.57
522.613.623.62
582.675.425.42
582.675.425.42
522.613.543.54
509.572.632.63
509.572.632.63
525.593.983.98
525.593.983.98
521.624.154.15
525.593.983.98
507.603.843.84
521.624.154.15
492.043.613.61
526.583.373.37
508.593.233.23
521.624.154.15
521.624.154.15
525.593.983.98
508.593.233.23
509.572.632.63
532.613.713.71
523.603.723.72
514.613.293.29
537.623.853.85
543.033.893.89
508.593.233.23
508.593.233.23
475.032.872.87
532.613.713.71
532.613.713.71
522.613.543.54
532.613.713.71
508.494.134.13
522.613.623.62
532.613.713.71
575.594.864.86
499.063.343.34
532.613.713.71
542.044.494.49
499.063.343.34
562.686.206.20
538.665.725.72
575.594.864.86
556.074.834.83
589.625.205.20
546.634.054.05
546.634.054.05
589.625.205.20
546.634.054.05
546.634.054.05
513.083.693.69
464.533.173.17
463.622.552.55
492.593.853.85
492.593.853.85
492.593.853.85
492.593.853.85
506.614.244.24
506.614.244.24
479.594.414.41
465.564.074.07