DC8866DEL-22379 is an ERK dimerization Inhibitor. DEL-22379 readily binds to ERK2 with a Kd estimated in the low micromolar range, though binding is detectable even at low nanomolar concentrations. ERK2 dimerization is…
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DC7283SCH772984 potently inhibits ERK1 and ERK2 activity with IC50s of 4 and 1 nM, respectively.
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DC7242VX-11e is a potent, selective, and orally bioavailable inhibitor of ERK with Ki < 2 nM.
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DC11886Adavivint is a potent and selective inhibitor of canonical Wnt signaling, with an EC50 of 19.5 nM via a high-throughput TCF/LEF-reporter assay in SW480 colon cancer cells.
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DC5090WZ4002 is a mutant selective EGFR inhibitor with IC50s of 2, 8, 3 and 2 nM for EGFRL858R, EGFRL858R/T790M, EGFRE746_A750 and EGFRE746_A750/T790M, respectively.
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DC7146GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, and also inhibits TGF-β type II receptor and activin type II receptor activities, without inhibiting BMP type II receptor.
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DC6308Sofosbuvir (PSI-7977) is an HCV RNA replication inhibitor with an EC50 of 92 nM.
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DC8042Telaglenastat (CB-839) is a potent and selective inhibitor of glutaminase with an IC50 of less than 50 nM.
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DC7060AZD1152 is a pro-drug of Barasertib-hQPA, which is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay.
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DC22228Fluzoparib (SHR-3162) is a novel, potent and orally available inhibitor of PARP; potently inhibited PARP1 enzyme activity and induced DNA double-strand breaks, G2/M arrest and apoptosis in homologous recombination…
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