The DOI matches its Crossref record; 5 of the 5 references it cites were found in a registry or an index.
Identification of N-(4-Piperidinyl)-4-(2,6-dichlorobenzoylamino)-1 H-pyrazole-3-carboxamide (AT7519), a Novel Cyclin Dependent Kinase Inhibitor Using Fragment-Based X-Ray Crystallography and Structure Based Drug Design
Open accessAbstract
The application of fragment-based screening techniques to cyclin dependent kinase 2 (CDK2) identified multiple (>30) efficient, synthetically tractable small molecule hits for further optimization. Structure-based design approaches led to the identification of multiple lead series, which retained the key interactions of the initial binding fragments and additionally explored other areas of the ATP binding site. The majority of this paper details the structure-guided optimization of indazole (6) using information gained from multiple ligand-CDK2 cocrystal structures. Identification of key binding features for this class of compounds resulted in a series of molecules with low nM affinity for CDK2. Optimisation of cellular activity and characterization of pharmacokinetic properties led to the identification of 33 (AT7519), which is currently being evaluated in clinical trials for the treatment of human cancers.
Overview
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Integrity signals
Registry
Cites
Statistics
Verification
Claims the paper makes
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Self-check
Percentages, sums and reported differences re-computed from the paper’s own numbers.
The self-check needs the paper’s full text.
Citations
Cites
Sherr, C. J. (1996) · Science · doi:10.1126/science.274.5293.1672 · Cited by 5,379
The retinoblastoma protein and cell cycle control
Weinberg, R. A. (1995) · Cell · doi:10.1016/0092-8674(95)90385-2 · Cited by 4,862
Mammalian cells cycle without the D-type cyclin-dependent kinases Cdk4 and Cdk6
Malumbres, M., Sotillo, R., Santamarı́a, D., Galán, J., Cerezo, A., Ortega, S., Dubus, P., & Barbacid, M. (2004) · Cell · doi:10.1016/j.cell.2004.08.002 · Cited by 793
Genetic alterations of cyclins, cyclin-dependent kinases, and Cdk inhibitors in human cancer
(1996) · Advances in cancer research · doi:10.1016/s0065-230x(08)60352-8 · Cited by 752
Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6
Toogood, P. L., Harvey, P. J., Repine, J. T., Sheehan, D. J., VanderWel, S. N., Zhou, H., Keller, P. R., McNamara, D. J., Sherry, D., Zhu, T., et al. (2005) · Journal of Medicinal Chemistry · doi:10.1021/jm049354h · Cited by 513
Cited by
Fragment-Based Approaches in Drug Discovery and Chemical Biology
Scott, D. E., Coyne, A. G., Hudson, S. A., & Abell, C. (2012) · Biochemistry · doi:10.1021/bi3005126 · Cited by 460
Halogen bonding (X‐bonding): A biological perspective
Scholfield, M. R., Zanden, C. M. V., Carter, M., & Ho, P. S. (2013) · Protein Science · doi:10.1002/pro.2201 · Cited by 451
Inhibitors of cyclin-dependent kinases as cancer therapeutics.
Whittaker, S. R., Mallinger, A., Workman, P., & Clarke, P. A. (2017) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2017.02.008 · Cited by 384
Activation pathway of Src kinase reveals intermediate states as targets for drug design
Shukla, D., Meng, Y., Roux, B., & Pande, V. S. (2014) · Nature Communications · doi:10.1038/ncomms4397 · Cited by 333
Transcriptional repression of DNA repair genes is a hallmark and a cause of cellular senescence
Collin, G., Huna, A., Warnier, M., Flaman, J.-M., & Bernard, D. (2018) · Cell Death & Disease · doi:10.1038/s41419-018-0300-z · Cited by 71
Metadata
- Authors
- Wyatt, P. G., Woodhead, A. J., Berdini, V., Boulstridge, J. A., Carr, M. G., Cross, D. M., Davis, D. J., Devine, L. A., Early, T. R., Feltell, R. E., Lewis, E. J., McMenamin, R. L., Navarro, E. F., O’Brien, M. A., O’Reilly, M., Reule, M., Saxty, G., Seavers, L. C. A., Smith, D.-M., Squires, M. S., Trewartha, G., Walker, M. T., & Woolford, A. J.-A.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2008-07-26
- Volume
- 51
- Issue
- 16
- Pages
- 4986-4999
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2149658883
- Cited by
- 340
- References
- 5
- FWCI
- 27.87
- Type
- journal article
- Language
- en
- Open access
- green
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
Are you an author, or do you see a problem with this page? Request a review
How to cite
Cite CoChat for the checks on this page, and the paper for its own findings.
- This page
- CoChat. (2026). Citation check: Identification of N-(4-Piperidinyl)-4-(2,6-dichlorobenzoylamino)-1 H-pyrazole-3-carboxamide (AT7519), a Novel Cyclin Dependent Kinase Inhibitor Using Fragment-Based X-Ray Crystallography and Structure Based Drug Design. https://app.cochat.ai/papers/10.1021/jm800382h
- The paper
- Wyatt, P. G., Woodhead, A. J., Berdini, V., Boulstridge, J. A., Carr, M. G., Cross, D. M., Davis, D. J., Devine, L. A., Early, T. R., Feltell, R. E., Lewis, E. J., McMenamin, R. L., Navarro, E. F., O’Brien, M. A., O’Reilly, M., Reule, M., Saxty, G., Seavers, L. C. A., Smith, D.-M., . . . Woolford, A. J.-A. (2008). Identification of N-(4-Piperidinyl)-4-(2,6-dichlorobenzoylamino)-1 H-pyrazole-3-carboxamide (AT7519), a Novel Cyclin Dependent Kinase Inhibitor Using Fragment-Based X-Ray Crystallography and Structure Based Drug Design. Journal of Medicinal Chemistry. https://doi.org/10.1021/jm800382h
Data sources
Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
