YYSW001 JAK1 Inhibitor Preclinical Data with 61.8% Oral Bioavailability

Structural and pharmacological data for YYSW001, a highly selective JAK1 inhibitor with an IC50 of 6 nM and >50-fold selectivity over JAK2. It includes results from pharmacokinetic evaluation showing 61.8% oral bioavailability and efficacy data from rat collagen-induced arthritis (CIA) and adjuvant-induced arthritis (AIA) models. The data supports the compound's preclinical development profile.

Use Cases

• Compare JAK1 inhibition potency (IC50 = 6 nM) and JAK2 selectivity (>50-fold) of YYSW001 against other inhibitors.
• Analyze the relationship between oral bioavailability (61.8%) and therapeutic efficacy in rat arthritis models (CIA, AIA).
• Benchmark the efficacy-tolerability profile of YYSW001 relative to upadacitinib using preclinical study data.
• Model the structure-activity relationship of imidazopyrrolopyridine compounds using the provided PDB file.

Strengths

• Includes specific, quantitative pharmacological metrics: JAK1 IC50 of 6 nM and >50-fold selectivity over JAK2.
• Reports concrete pharmacokinetic results, including 61.8% oral bioavailability.
• Contains efficacy data from two established preclinical arthritis models (rat CIA and AIA).

Limitations

• The dataset is small in scale at 388.8 KB, limiting the scope for extensive statistical analysis.
• Data is derived from preclinical animal models (rats), which may not directly translate to human outcomes.
• The specific data format (PDB) and lack of defined columns may require specialized tools for analysis.

Provenance

Source

figshare, authored by Kaiyong Hu.

Collection Method

Data generated from the design, optimization, and preclinical evaluation of a series of imidazopyrrolopyridines.

Freshness

Last updated on 2026-03-20.