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FTI-2153 is a potent and highly selectiveof farnesyltransferase (FTase) inhibitor and a highly potent antagonist of oncogenic H-Ras signaling.
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IPR-803 is a potent inhibitor of the uPAR•uPA protein-protein interaction, and binds directly to uPAR with sub-micromolar affinity.
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OTS964 is an orally active, high affinity and selective TOPK inhibitor and is also a potent inhibitor of the cyclin-dependent kinase CDK11.
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JTE-013 is a potent and specific S1P2 antagonist and increases the excitability of sensory neurons independently of the receptor.
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BI-167107 is a high affinity, full agonist that binds to the β2 adrenergic receptor (β2AR) with a dissociation constant Kd of 84 pM.
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Tasisulam is an anticancer agent and induces apoptosis, which also inhibits mitotic progression and induces vascular normalization.
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sAJM589 is a Myc inhibitor which potently disrupts the Myc-Max heterodimer in a dose dependent manner with an IC50 of 1.8 μM.
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CD161 is a potent and orally bioavailable bromodomain and extra-terminal bromodomain inhibitor with an IC50 of 28.2 nM and a Ki of 8.2 nM for BRD4 BD1.
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NV03 is a potent and selective antagonist of UHRF1-H3K9me3 interaction by binding to UHRF1 TTD with a Kd of 2.4 μM and has anticancer activity.
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CG-200745 is a potent and pan HDAC inhibitor. CG200745 inhibits the deacetylation of histone H3 and tubulin, inducing p53 accumulation.
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