Biosensor Analysis of Drug–Target Interactions: Direct and Competitive Binding Assays for Investigation of Interactions between Thrombin and Thrombin Inhibitors

摘要: The sensitivity of BIACORE technology is sufficient for detection and characterization binding events involving low-molecular-weight compounds their immobilized protein targets. requires no labeling provides information on the stability compound/target complex with a single injection compound. This useful qualifying hits obtained in primary screen lead optimization. Although targets can be reused, surface may slowly deteriorate, solvent effects distort levels during compounds, some exhibit broad selectivity rather than target specificity. A reliable direct assay to thrombin using combination two reference surfaces, dextran subtraction calibration identification that tend bind proteins, has been developed. Eleven known specificity 159 additional were investigated. All identified at 1 10 microM concentration. One compound was scored as positive. compared favorably competitive formats, inhibitor solution assay, examined parallel.