CHD1 Chromodomain Inhibitors: High-Affinity Compounds for Prostate Cancer

Holger Greschik published a dataset on figshare in May 2026 detailing the development of quinoline-based inhibitors targeting the CHD1 chromatin remodeler. The dataset likely contains experimental results for compounds 2n and 2s, which achieved submicromolar binding affinity with Kd values of 0.15 μM and 0.14 μM, respectively. These compounds were tested for selectivity against methyl-lysine readers and showed impairment of prostate cancer cell viability.

Use Cases

• Analyzing binding affinity data for CHD1 chromodomain inhibitors based on reported Kd values.
• Comparing structural interactions of quinoline-based compounds based on co-crystal structure findings.
• Evaluating selectivity profiles against methyl-lysine readers based on the panel test mentioned.
• Assessing compound effects on cell viability based on impairment results in prostate cancer cells.

Strengths

• Includes specific binding affinity measurements (Kd values of 0.15 μM and 0.14 μM) for two compounds.
• Describes a defined binding mode from co-crystal structures, providing mechanistic insight.
• Reports evidence of selectivity against a panel of epigenetic enzymes and engagement in cell lysates.

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 (4.2 KB), indicating limited scope.

Provenance

Source

figshare

Collection Method

Likely contains experimental data from biochemical and cellular assays.

Freshness

Last updated 2026-05-05 21:04:07; freshness should be verified.