CZL-149: Potency and Bioavailability Data for a Dual BET/p300/CBP Bromodomain Inhibitor

A 2026 study describes CZL-149, a novel dual inhibitor targeting BET and p300/CBP bromodomains. The dataset likely contains potency metrics, such as an IC50 of 3.3 nM against OPM-2 cells, and pharmacokinetic data, including 107% oral bioavailability in mice. The data was uploaded by Zonglong Chen to figshare.

Use Cases

• Compare in vitro potency of novel bromodomain inhibitors based on reported IC50 values.
• Evaluate oral bioavailability and metabolic profiles of preclinical drug candidates.
• Benchmark antitumor efficacy against reference compounds like NEO2734 using reported tumor growth inhibition (TGI) data.
• Inform structure-activity relationship (SAR) studies for dual BET/p300/CBP inhibitors.

Strengths

• Includes specific potency metrics, such as an IC50 of 3.3 nM against multiple myeloma OPM-2 cells.
• Reports concrete pharmacokinetic results, including 107% oral bioavailability in mice.
• Provides comparative efficacy data, showing CZL-149 outperformed NEO2734 with a TGI of 78%.

Limitations

• Column-level documentation is absent; field semantics must be inferred after download.
• Row count is unknown, which may limit suitability assessment.
• The dataset is very small (3.5 KB), indicating limited scope.

Provenance

Source

Zonglong Chen

Collection Method

Likely contains results from systematic structure-activity relationship exploration and in vitro/in vivo testing described in the associated study.

Freshness

Last updated 2026-05-18 17:41:37; freshness should be verified.