MLchartDataset catalogue

Lead validation

Term · Chemistry · MLC-T-CHM-006500

The process of confirming that a chemical compound identified as a "hit" in a primary screening assay exhibits the desired biological activity and physicochemical properties to be considered a viable starting point for drug discovery. This involves retesting the compound in orthogonal assays, assessing its dose-response relationship, and evaluating its selectivity against related targets. A validated lead compound typically demonstrates micromolar or nanomolar potency and acceptable solubility.

Table 1. Record
IdentifierMLC-T-CHM-006500
FieldChemistry
SubjectChemistry and Human Health
ReferencesPAC, 2013, 85, 1725. 'Glossary of terms used in medicinal chemistry. Part II (IUPAC Recommendations 2013)' on page 1739 (https://doi.org/10.1351/PAC-REC-12-11-23)
See alsoLead
Record as JSON
{
  "id": "MLC-T-CHM-006500",
  "term": "Lead validation",
  "field": "Chemistry",
  "definition": "The process of confirming that a chemical compound identified as a \"hit\" in a primary screening assay exhibits the desired biological activity and physicochemical properties to be considered a viable starting point for drug discovery. This involves retesting the compound in orthogonal assays, assessing its dose-response relationship, and evaluating its selectivity against related targets. A validated lead compound typically demonstrates micromolar or nanomolar potency and acceptable solubility.",
  "subject": "Chemistry and Human Health",
  "see_also": [
    "lead"
  ],
  "references": [
    "PAC, 2013, 85, 1725. 'Glossary of terms used in medicinal chemistry. Part II (IUPAC Recommendations 2013)' on page 1739 (https://doi.org/10.1351/PAC-REC-12-11-23)"
  ],
  "url": "https://mlchart.com/terminology/chemistry/lead-validation/"
}

Record 6,892 of 13,678 in Chemistry terminology (MLC-0109). Request the full dataset.