ArticleMolecules (Basel, Switzerland)2020
Comparative Assessment of Protein Kinase Inhibitors in Public Databases and in PKIDB.
Article in Molecules (Basel, Switzerland), 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 41 papers.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
41 citing papers in PubMed.
- Single-cell transcriptomics identifies a p21-activated kinase important for survival of the zoonotic parasiteiScience · 2026Article
- An Experimentally Validated Structure-Based Virtual Screening Approach to Identify Nucleotide-Binding Protein Inhibitors as a New Source of Kinase Inhibitors.Pharmaceuticals (Basel, Switzerland) · 2026Article
- Mapping the Brain Interaction Network of the Dual-Specificity, Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A) Targeted by Leucettinib-21 Using Affinity Chromatography.ACS pharmacology & translational science · 2026Article
- Polypharmacology is an enduring and nearly universal property of kinase inhibitors.bioRxiv : the preprint server for biology · 2026Article
- Pharmacophore-driven kinase profiling applied to the PKIS2 chemogenomic dataset.Scientific reports · 2026Article
- Natural Product-like Fragments Unlock Novel Chemotypes for a Kinase Target─Exploring Options beyond the Flatland.Journal of chemical information and modeling · 2026Article
- Frags2Drugs: A Novel In Silico Fragment-Based Approach to the Discovery of Kinase Inhibitors.Pharmaceuticals (Basel, Switzerland) · 2026Article
- Curation of the Fasciola hepatica kinome as a resource for drug target discovery.BMC genomics · 2026Article
- Article
- Graph neural networks driven acceleration in drug discovery.Acta pharmaceutica Sinica. B · 2025Review
- Advances in reversible covalent kinase inhibitors.Medicinal research reviews · 2025Review
- Oncofusions - shaping cancer care.The oncologist · 2025Article
- Article
- Research towards selective inhibition of the CLK3 kinase.Beilstein journal of organic chemistry · 2025Article
- The NIMA-related kinase family and cancer.Frontiers in oncology · 2025Review
- Molecular Chimera in Cancer Drug Discovery: Beyond Antibody Therapy, Designing Grafted Stable Peptides Targeting Cancer.International journal of peptide research and therapeutics · 2025Review
- Review
- KinomeMETA: a web platform for kinome-wide polypharmacology profiling with meta-learning.Nucleic acids research · 2024Article
- Proteomics and AQP2 regulation.The Journal of physiology · 2024Review
- Article
Corrections and comments
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Authors and funding
7 authors.
Funding
Abstract
Since the first approval of a protein kinase inhibitor (PKI) by the Food and Drug Administration (FDA) in 2001, 55 new PKIs have reached the market, and many inhibitors are currently being evaluated in clinical trials. This is a clear indication that protein kinases still represent major drug targets for the pharmaceutical industry. In a previous work, we have introduced PKIDB, a publicly available database, gathering PKIs that have already been approved (Phase 4), as well as those currently in clinical trials (Phases 0 to 3). This database is updated frequently, and an analysis of the new data is presented here. In addition, we compared the set of PKIs present in PKIDB with the PKIs in early preclinical studies found in ChEMBL, the largest publicly available chemical database. For each dataset, the distribution of physicochemical descriptors related to drug-likeness is presented. From these results, updated guidelines to prioritize compounds for targeting protein kinases are proposed. The results of a principal component analysis (PCA) show that the PKIDB dataset is fully encompassed within all PKIs found in the public database. This observation is reinforced by a principal moments of inertia (PMI) analysis of all molecules. Interestingly, we notice that PKIs in clinical trials tend to explore new 3D chemical space. While a great majority of PKIs is located on the area of "flatland", we find few compounds exploring the 3D structural space. Finally, a scaffold diversity analysis of the two datasets, based on frequency counts was performed. The results give insight into the chemical space of PKIs, and can guide researchers to reach out new unexplored areas. PKIDB is freely accessible from the following website: http://www.icoa.fr/pkidb.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.