Category: Drug discovery

In 2019, drug-resistant bacterial infections were directly responsible for 1.27 million deaths globally. This stark statistic highlights the urgency of the antimicrobial resistance (AMR) crisis and brings into focus the critical question: why can't we find new antibiotics to replenish our diminishing arsenal?

Despite costing billions and taking over a decade to develop, only a fraction of drug candidates successfully reach the market. The core process that drives this scientific endeavor is drug design, and understanding its basic principle—molecular recognition—is fundamental to creating more effective and safer medicines.

Drugs interact with specific receptors in the body, with approximately 30% of all approved drugs targeting G-protein-coupled receptors alone. A drug's effectiveness hinges on its ability to bind and modulate one of the four major types of drug receptors with examples for each, initiating a cascade of cellular events that lead to a therapeutic effect.

Developing a new drug is a lengthy and challenging process, with statistics indicating that only about 1 out of 5,000 compounds entering the preclinical phase eventually becomes an approved drug. Understanding **what are the steps of drug design** is crucial for appreciating the immense scientific and financial investment required to bring new medicines to market.

Despite advances in research, the overall probability of success for new molecular entities is only about 12%. Rational drug design, a systematic and knowledge-based approach, directly addresses this challenge by meticulously defining what are the four steps in rational drug design to increase efficiency and success rates in creating new medications.

With a single drug discovery program costing hundreds of millions to billions of dollars and taking over a decade to complete, modern pharmacology has moved beyond trial-and-error. This shift has redefined **what is the primary goal of drug design**, which now focuses on the rational, data-driven creation of molecules that are highly effective, selective, and safe.

Up to 90% of drug candidates fail during development, largely due to issues with efficacy and safety. Understanding what is the key aspect of drug design—achieving a specific and effective interaction with a biological target—is crucial for improving these statistics and advancing new therapeutic treatments.

In pharmacology, the half-maximal inhibitory concentration (IC50) is a critical measure for assessing a drug's potency, representing the concentration required to inhibit a biological process by 50%. This value is fundamental to drug discovery and understanding inhibitory effectiveness. So, is high or low IC50 better for a medication?

An estimated 90% of drug candidates that enter clinical trials ultimately fail [1.8.2]. To improve success rates, researchers rely on key metrics like the half-maximal inhibitory concentration (IC50). So, what is the interpretation of IC50 values, and how does it guide drug discovery?

First isolated from coal tar in the 19th century, the chemical scaffold known as carbazole is not a drug itself, but its derivatives have proven remarkably versatile in modern medicine, with applications spanning oncology, cardiology, and more. This unique heterocyclic compound provides a core structure for developing a wide array of therapeutics.