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Updated: Jul 4, 2026

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
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Published on: October 26, 2015

随性聚合物基抑制剂的固体测量和物理化学

Kristin E D Coan1, Brian K Shoichet

  • 1Department of Pharmaceutical Chemistry & Graduate Group in Chemistry and Chemical Biology, 1700 Fourth Street, University of California at San Francisco, San Francisco, California 94158-2550, USA.

Journal of the American Chemical Society
|July 1, 2008
PubMed
概括

有机分子聚合物在药物发现中引起虚假阳性. 这项研究量化了聚合物度和结构,揭示了临界聚合度 (CAC) 和密集的颗粒包装,影响了酶结合.

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The Equilibrium Binding Constant and Binding Strength02:18

The Equilibrium Binding Constant and Binding Strength

The equilibrium binding constant (Kb) quantifies the strength of a protein-ligand interaction. Kb can be calculated as follows when the reaction is at equilibrium:
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Heterogeneous Catalysis

Heterogeneous catalysis involves a catalyst in a different phase from the reactants. It is a process where the catalyst and the reactants are in distinct phases, typically solid and gas or liquid.Most heterogeneous catalysts are metals, metal oxides, or acids. The list includes transition metals like iron (Fe), cobalt (Co), nickel (Ni), palladium (Pd), platinum (Pt), chromium (Cr), manganese (Mn), tungsten (W), silver (Ag), and copper (Cu). These metals possess partially vacant d orbitals that...
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Enzyme Inhibition

Inhibitors are molecules that reduce enzyme activity by binding to the enzyme. In a normally functioning cell, enzymes are regulated by a variety of inhibitors. Drugs and other toxins can also inhibit enzymes. Some inhibitors bind to the enzyme’s active site, while others inhibit enzymatic activity by binding to other sites on the protein structure.
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Quantitative Aspects of Drug-Receptor Interaction

The receptor occupancy theory connects a drug's response to the number of occupied receptors. With higher drug concentrations, more receptors are occupied, leading to increased responses. The formation of drug-receptor complexes involves association and dissociation rates, which reach equilibrium when the forward and backward reactions are equal. The equilibrium association constant (Ka) and its inverse, the equilibrium dissociation constant (Kd), indicate drug affinity. Higher Ka and lower Kd...
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Deleterious Substances in Aggregate

Deleterious substances in aggregates can be detrimental to the quality and durability of concrete. These substances include organic impurities like loam, which interfere with cement hydration and are usually present in the sand. These prevent a good bond between aggregate and cement paste. Organic impurities can be detected using the colorimetric test, where the darkness of a solution after agitation indicates the level of organic content.
Another type of impurity is clay and fine material that...