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8‑Substituted Pyrido[3,4‑d]pyrimidin-4(3H)‑one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors

Journal of medicinal chemistry, 2016-02, Vol.59 (4), p.1388-1409

2016

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Aminopyrazine Inhibitors Binding to an Unusual Inactive Conformation of the Mitotic Kinase Nek2: SAR and Structural Characterization

Journal of medicinal chemistry, 2010-11, Vol.53 (21), p.7682-7698

2010

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Analysis of water patterns in protein kinase binding sites

Proteins, structure, function, and bioinformatics, 2011-07, Vol.79 (7), p.2109-2121

2011

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Application of Fragment Screening and Fragment Linking to the Discovery of Novel Thrombin Inhibitors

Journal of medicinal chemistry, 2006-02, Vol.49 (4), p.1346-1355

2006

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Benzimidazole Inhibitors Induce a DFG-Out Conformation of Never in Mitosis Gene A-Related Kinase 2 (Nek2) without Binding to the Back Pocket and Reveal a Nonlinear Structure−Activity Relationship

Journal of medicinal chemistry, 2011-03, Vol.54 (6), p.1626-1639

2011

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Benzimidazole inhibitors of the protein kinase CHK2: Clarification of the binding mode by flexible side chain docking and protein–ligand crystallography

Bioorganic & medicinal chemistry, 2012-11, Vol.20 (22), p.6630-6639

2012

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C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays

European journal of medicinal chemistry, 2019-09, Vol.177, p.316-337

2019

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Crystal structure and assembly of a eukaryotic small heat shock protein

Nature structural & molecular biology, 2001-12, Vol.8 (12), p.1025-1030

2001

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Crystal structure of truncated human βB1‐crystallin

Protein science, 2003-11, Vol.12 (11), p.2606-2612

2003

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Crystallization of Enzyme IIB of the Cellobiose-specific Phosphotransferase System of Escherichia coli

Journal of molecular biology, 1994-06, Vol.239 (4), p.588-590

1994

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Current perspectives in fragment-based lead discovery (FBLD)

Essays in biochemistry, 2017-11, Vol.61 (5), p.453

2017

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Discovering cell-active BCL6 inhibitors: effectively combining biochemical HTS with multiple biophysical techniques, X-ray crystallography and cell-based assays

Scientific reports, 2022-11, Vol.12 (1), p.18633-18633, Article 18633

2022

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The discovery of potent ribosomal S6 kinase inhibitors by high-throughput screening and structure-guided drug design

Oncotarget, 2013-10, Vol.4 (10), p.1647-1661

2013

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Drugging the PI3 Kinome: From Chemical Tools to Drugs in the Clinic

Cancer research (Chicago, Ill.), 2010-03, Vol.70 (6), p.2146-2157

2010

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Evaluation of APOBEC3B Recognition Motifs by NMR Reveals Preferred Substrates

ACS chemical biology, 2018-09, Vol.13 (9), p.2427-2432

2018

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Exploiting Protein Conformational Change to Optimize Adenosine-Derived Inhibitors of HSP70

Journal of medicinal chemistry, 2016-05, Vol.59 (10), p.4625-4636

2016

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A fragment-based approach applied to a highly flexible target: Insights and challenges towards the inhibition of HSP70 isoforms

Scientific reports, 2016-10, Vol.6 (1), p.34701-34701, Article 34701

2016

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Fragment-based drug discovery and its application to challenging drug targets

Essays in biochemistry, 2017-11, Vol.61 (5), p.475

2017

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Fragment-based methods in drug discovery: it's the small things that matter

Current topics in medicinal chemistry, 2009, Vol.9 (18), p.1676

2009

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Fragment-based screening maps inhibitor interactions in the ATP-binding site of checkpoint kinase 2

PloS one, 2013-06, Vol.8 (6), p.e65689-e65689

2013

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High Proliferation Rate and a Compromised Spindle Assembly Checkpoint Confers Sensitivity to the MPS1 Inhibitor BOS172722 in Triple-Negative Breast Cancers

Molecular cancer therapeutics, 2019-10, Vol.18 (10), p.1696-1707

2019

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Identification of autophosphorylation inhibitors of the inositol-requiring enzyme 1 alpha (IRE1α) by high-throughput screening using a DELFIA assay

Journal of biomolecular screening, 2013-03, Vol.18 (3), p.298-308

2013

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8‑Substituted Pyrido[3,4‑d]pyrimidin-4(3H)‑one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors

Achieving In Vivo Target Depletion through the Discovery and Optimization of Benzimidazolone BCL6 Degraders

Aminopyrazine Inhibitors Binding to an Unusual Inactive Conformation of the Mitotic Kinase Nek2: SAR and Structural Characterization

Analysis of water patterns in protein kinase binding sites

Application of Fragment Screening and Fragment Linking to the Discovery of Novel Thrombin Inhibitors

Benzimidazole Inhibitors Induce a DFG-Out Conformation of Never in Mitosis Gene A-Related Kinase 2 (Nek2) without Binding to the Back Pocket and Reveal a Nonlinear Structure−Activity Relationship

Benzimidazole inhibitors of the protein kinase CHK2: Clarification of the binding mode by flexible side chain docking and protein–ligand crystallography

C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays

Crystal structure and assembly of a eukaryotic small heat shock protein

Crystal structure of truncated human βB1‐crystallin

Crystallization of Enzyme IIB of the Cellobiose-specific Phosphotransferase System of Escherichia coli

Current perspectives in fragment-based lead discovery (FBLD)

Discovering cell-active BCL6 inhibitors: effectively combining biochemical HTS with multiple biophysical techniques, X-ray crystallography and cell-based assays

Discovery of a Chemical Probe Bisamide (CCT251236): An Orally Bioavailable Efficacious Pirin Ligand from a Heat Shock Transcription Factor 1 (HSF1) Phenotypic Screen

Discovery of an In Vivo Chemical Probe for BCL6 Inhibition by Optimization of Tricyclic Quinolinones

The discovery of potent ribosomal S6 kinase inhibitors by high-throughput screening and structure-guided drug design

Drugging the PI3 Kinome: From Chemical Tools to Drugs in the Clinic

Evaluation of APOBEC3B Recognition Motifs by NMR Reveals Preferred Substrates

Exploiting Protein Conformational Change to Optimize Adenosine-Derived Inhibitors of HSP70

A fragment-based approach applied to a highly flexible target: Insights and challenges towards the inhibition of HSP70 isoforms

Fragment-based drug discovery and its application to challenging drug targets

Fragment-based methods in drug discovery: it's the small things that matter

Fragment-based screening maps inhibitor interactions in the ATP-binding site of checkpoint kinase 2

High Proliferation Rate and a Compromised Spindle Assembly Checkpoint Confers Sensitivity to the MPS1 Inhibitor BOS172722 in Triple-Negative Breast Cancers

Identification of autophosphorylation inhibitors of the inositol-requiring enzyme 1 alpha (IRE1α) by high-throughput screening using a DELFIA assay

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