CZL-149: Structural and Efficacy Data for a Dual BET/p300/CBP Bromodomain Inhibitor

A dataset describes the discovery of CZL-149, a novel dual inhibitor targeting BET and p300/CBP bromodomains. The data includes structural information (PDB files) and preclinical results showing an IC50 of 3.3 nM against OPM-2 cells, 107% oral bioavailability in mice, and 78% tumor growth inhibition. The dataset was authored by Zonglong Chen and last updated on 2026-05-18.

Use Cases

• Analyzing structure-activity relationships based on the pyrrolo[2,3-c]pyridinone fragment replacement.
• Comparing in vitro potency based on the reported IC50 value of 3.3 nM against multiple myeloma cells.
• Evaluating in vivo antitumor efficacy based on the reported 78% tumor growth inhibition (TGI).
• Assessing drug-like properties based on the reported oral bioavailability of 107% in mice.

Strengths

• Includes specific potency metrics, such as an IC50 of 3.3 nM against OPM-2 cells.
• Reports concrete in vivo efficacy results, including a tumor growth inhibition (TGI) of 78%.
• Provides a direct comparison to the clinical candidate NEO2734, highlighting superior performance.

Limitations

• Row count is unknown, which may limit suitability assessment.
• Column-level documentation is absent; field semantics must be inferred after download.
• The dataset is very small (166.4 KB), indicating limited scope.

Provenance

Source

figshare

Collection Method

Likely contains experimental results from a medicinal chemistry study.

Freshness

Last updated 2026-05-18 17:41:36; freshness should be verified.