Crystal Structures of Human ADAMTS-1 Reveal a Conserved Catalytic Domain and a Disintegrin-like Domain with a Fold Homologous to Cysteine-Rich Domains

S. Gerhardt, G. Hassall, Paul Hawtin, +8

Journal of Molecular Biology

Protein FunctionProtein AssemblyProtein FoldingNatural SciencesProtein X-ray Crystallography +7

The PARP Inhibitor AZD2461 Provides Insights into the Role of PARP3 Inhibition for Both Synthetic Lethality and Tolerability with Chemotherapy in Preclinical Models

Lenka Oplustil O’Connor, Stuart L. Rulten, Aaron Cranston, +16

Cancer Research

Chemoprevention StrategyParp3 InhibitionPharmacotherapyCancer BiologyTumor Biology +20

Learning Medicinal Chemistry Absorption, Distribution, Metabolism, Excretion, and Toxicity (ADMET) Rules from Cross-Company Matched Molecular Pairs Analysis (MMPA)

Christian Krämer, Attilla Ting, Hao Zheng, +10

Journal of Medicinal Chemistry

Pharmaceutical ScienceDrug TargetMedicinal ChemistryDrug PurityBioanalysis +19

The Discovery of 7-Methyl-2-[(7-methyl[1,2,4]triazolo[1,5-<i>a</i>]pyridin-6-yl)amino]-9-(tetrahydro-2<i>H</i>-pyran-4-yl)-7,9-dihydro-8<i>H</i>-purin-8-one (AZD7648), a Potent and Selective DNA-Dependent Protein Kinase (DNA-PK) Inhibitor

Frederick W. Goldberg, M. Raymond V. Finlay, Attilla Ting, +13

Journal of Medicinal Chemistry

PharmacotherapyChemical BiologyDna-pk Catalytic SubunitPharmaceutical ChemistryPre-clinical Pharmacology +18

1-Substituted (Dibenzo[<i>b,d</i>]thiophen-4-yl)-2-morpholino-4<i>H</i>-chromen-4-ones Endowed with Dual DNA-PK/PI3-K Inhibitory Activity

Céline Cano, Kappusamy Saravanan, Chris Bailey, +14

Journal of Medicinal Chemistry

Molecular PharmacologyMedicinal ChemistryPharmaceutical ScienceDerivative (Chemistry)Medicine +12

Discovery of Clinical Candidate AZD0095, a Selective Inhibitor of Monocarboxylate Transporter 4 (MCT4) for Oncology

Frederick W. Goldberg, Jason G. Kettle, Gillian M. Lamont, +13

Journal of Medicinal Chemistry

Discovery of a Thiadiazole–Pyridazine-Based Allosteric Glutaminase 1 Inhibitor Series That Demonstrates Oral Bioavailability and Activity in Tumor Xenograft Models

M. Raymond V. Finlay, Mark J. Anderton, Andrew Bailey, +32

Journal of Medicinal Chemistry

Oral BioavailabilityPharmacotherapyGls1 Inhibitor Bis-2-Pharmaceutical ChemistryMedicinal Chemistry +14

Potent enantioselective inhibition of DNA-dependent protein kinase (DNA-PK) by atropisomeric chromenone derivatives

K.M. Clapham, Tommy Rennison, Gavin O. Jones, +9

Organic & Biomolecular Chemistry

Pharmaceutical ScienceChromen-4-one PharmacophoreBioorganic ChemistryChiral HplcMolecular Biology +19

DNA-dependent protein kinase (DNA-PK) inhibitors: Structure–activity relationships for O-alkoxyphenylchromen-4-one probes of the ATP-binding domain

K.M. Clapham, Julia Bárdos, M. Raymond V. Finlay, +9

Bioorganic & Medicinal Chemistry Letters

BiochemistryNatural SciencesMolecular BiologyBiochemical InteractionDna-dependent Protein Kinase +5

Selective non zinc binding inhibitors of MMP13

Chris De Savi, Andrew Morley, Attilla Ting, +13

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryMedicineMetalloproteinSelective Non ZincPharmacotherapy +3