Discovering cell-active BCL6 inhibitors: effectively combining biochemical HTS with multiple biophysical techniques, X-ray crystallography and cell-based assaysSCIENTIFIC REPORTSIF3.92022-11-037OAAI
Structural Analysis and Development of Notum Fragment Screening HitsACS CHEMICAL NEUROSCIENCEIF3.92022-06-224OAAI
Design of a Potent, Selective, and Brain-Penetrant Inhibitor of Wnt-Deactivating Enzyme Notum by Optimization of a Crystallographic Fragment HitJOURNAL OF MEDICINAL CHEMISTRYIF6.82022-05-1010OAAI
Carboxylesterase Notum Is a Druggable Target to Modulate Wnt SignalingJOURNAL OF MEDICINAL CHEMISTRYIF6.82021-03-3030OAAI
5-Phenyl-1,3,4-oxadiazol-2(3H)-ones Are Potent Inhibitors of Notum Carboxylesterase Activity Identified by the Optimization of a Crystallographic Fragment Screening HitJOURNAL OF MEDICINAL CHEMISTRYIF6.82020-10-3015OAAI
Screening of a Custom-Designed Acid Fragment Library Identifies 1-Phenylpyrroles and 1-Phenylpyrrolidines as Inhibitors of Notum Carboxylesterase ActivityJOURNAL OF MEDICINAL CHEMISTRYIF6.82020-07-2917OAAI
Achieving In Vivo Target Depletion through the Discovery and Optimization of Benzimidazolone BCL6 DegradersJOURNAL OF MEDICINAL CHEMISTRYIF6.82020-04-1046OAAI
High Proliferation Rate and a Compromised Spindle Assembly Checkpoint Confers Sensitivity to the MPS1 Inhibitor BOS172722 in Triple-Negative Breast CancersMOLECULAR CANCER THERAPEUTICSIF5.52019-10-0134OAAI
Introduction of a Methyl Group Curbs Metabolism of Pyrido[3,4-d]pyrimidine Monopolar Spindle 1 (MPS1) Inhibitors and Enables the Discovery of the Phase 1 Clinical Candidate N2-(2-Ethoxy-4-(4-methyl-4H-1,2,4-triazol-3-yl)phenyl)-6-methyl-N8-neopentylpyrido[3,4-d]pyrimidine-2,8-diamine (BOS172722)JOURNAL OF MEDICINAL CHEMISTRYIF6.82018-09-1028OAAI
In vitro and in vivo profile of the preclinical candidate and MPS1 kinase inhibitor CCT289346CANCER RESEARCHIF16.62018-07-010PRE
Inhibitors of MPS1: Discovery of CCT289346, a highly potent, selective and orally available preclinical candidateCANCER RESEARCHIF16.62017-07-011PRE
Induction of detrimental aneuploidy in basal breast cancer cells treated by MPS1 inhibitors in combination with paclitaxelCANCER RESEARCHIF16.62017-07-011PRE
Characterisation of CCT271850, a selective, oral and potent MPS1 inhibitor, used to directly measure in vivo MPS1 inhibition vs therapeutic efficacyBRITISH JOURNAL OF CANCERIF6.82017-03-2324OAAI
Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization ApproachJOURNAL OF MEDICINAL CHEMISTRYIF6.82016-04-0730OAAI
Discovery of Novel Small-Molecule Inhibitors of BRD4 Using Structure-Based Virtual ScreeningJOURNAL OF MEDICINAL CHEMISTRYIF6.82013-10-03132OAAI
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