PD-305: Novel PTPN2-Selective Degrader Compound Data

PD-305 is a novel alkynylbenzene scaffold-based PROTAC exhibiting subnanomolar degradation potency against the PTPN2 protein. The dataset, shared by Linghao Hu on figshare in May 2026, describes a compound with a DC50 of 0.25 nM and over 20-fold selectivity for PTPN2 over PTPN1. It shows nanomolar antiproliferation potency in cell lines and suppressed tumor growth in mice.

Use Cases

• Benchmarking new PTPN2 degraders based on the reported subnanomolar DC50 value.
• Analyzing structure-activity relationships for PROTACs based on the alkynylbenzene scaffold.
• Comparing physicochemical properties like molecular weight and cLogP against other candidate degraders.
• Evaluating in vivo efficacy for cancer immunotherapy based on the described tumor suppression results.

Strengths

• Specific potency metrics are provided, including a DC50 of 0.25 nM and >20-fold subtype selectivity.
• Comparative data against prior compounds PVD-06 and AC484 is included, showing an 868-fold and 80-fold improvement, respectively.
• The description details specific molecular improvements like lower molecular weight and reduced cLogP.

Limitations

• The dataset is very small at 5.0 KB, suggesting limited scope.
• Column-level documentation is absent; field semantics must be inferred after download.
• Row count is unknown, which may limit suitability assessment.

Provenance

Source

Linghao Hu via figshare.

Collection Method

Likely contains experimental data from a medicinal chemistry study employing a ring-opening scaffold-hopping strategy.

Freshness

Last updated 2026-05-14 12:38:41; freshness should be verified.