Designing Antibiotics with Inherent Efflux Resistance: ERB-Modified Fluoroquinolones

Mark Laws reports a novel Efflux Resistance Breaker (ERB) strategy for designing antibiotics intrinsically resistant to efflux. The dataset includes results for lead compounds KSN-L22 and BL-7, showing up to a 512-fold reduction in MIC against multidrug-resistant bacteria and efficacy in a murine thigh infection model. The data was last updated on 2026-05-29.

Use Cases

• Training predictive models for antibiotic activity based on MIC reduction data mentioned in the description
• Analyzing structure-activity relationships for ERB-modified fluoroquinolones based on the reported lead compounds
• Evaluating pharmacokinetic/pharmacodynamic (PK/PD) profiles for oral and intravenous dosing based on the favorable profiles described

Strengths

• Includes specific MIC90 values ranging from 0.03–2 μg/mL against multidrug-resistant bacteria
• Reports in vivo efficacy with a > 4-log bacterial load reduction in a murine thigh infection model at 50 mg/kg oral dose
• Demonstrates favorable safety profile with no toxicity observed at 1200 mg/kg/day and no hERG, CYP450, or off-target liabilities

Limitations

• Column-level documentation is absent; field semantics must be inferred after download
• Row count is unknown, which may limit suitability assessment
• Data may reflect experimental bias inherent to the specific research methodology

Provenance

Source

Mark Laws via figshare

Collection Method

Likely contains experimental results from a pharmacological study.

Freshness

Last updated 2026-05-29 04:48:40; freshness should be verified