| S1060 |
AZD2281 (Olaparib)
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Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1/2 with IC50 of 5 nM/1 nM in cell-free assays, 300-times less effective against tankyrase-1. Olaparib induces significant autophagy that is associated with mitophagy in cells with BRCA mutations.
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Cell, 2025, 188(18):5081-5099.e27
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Cancer Cell, 2025, 43(8):1530-1548.e9
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Cancer Cell, 2025, 43(4):776-796.e14
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| S7693 |
Ceralasertib (AZD6738)
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Ceralasertib (AZD6738) is an orally active and selective ATR kinase inhibitor with IC50 of 1 nM, currently in Phase 1/2 clinical trials.
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Cancer Cell, 2025, 43(8):1530-1548.e9
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Nat Cell Biol, 2025, 27(1):73-86
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Nat Commun, 2025, 16(1):8476
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| S7048 |
BMN-673 (Talazoparib)
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Talazoparib (BMN 673, LT-673) is a novel PARP inhibitor with IC50 of 0.57 nM for PARP1 in a cell-free assay. It is also a potent inhibitor of PARP-2, but does not inhibit PARG and is highly sensitive to PTEN mutation. Phase 3.
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Mol Cancer, 2025, 24(1):217
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Nat Commun, 2025, 16(1):8476
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Nat Commun, 2025, 16(1):6972
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| E1349 |
TNG908 (Ralometostat)
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Ralometostat (TNG908) is a potent, selective, and brain-penetrant inhibitor of PRMT5 with an IC50 of 4 μM, acting through an MTA-cooperative mechanism. It also shows antitumor activity in a xenograft model.
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| S8680 |
AZD1390
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AZD1390 is a first-in-class orally available and CNS penetrant ATM inhibitor with an IC50 of 0.78 nM in cells and >10,000-fold selectivity over closely related members of the PIKK family of enzymes and excellent selectivity across a broad panel of kinases.
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Cell Rep Med, 2025, 6(7):102202
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iScience, 2025, 28(2):111842
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Nature, 2024, 629(8011):443-449
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| S1180 |
XAV-939
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XAV-939 (NVP-XAV939) selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition with IC50 of 11 nM/4 nM in cell-free assays, regulates axin levels and does not affect CRE, NF-κB or TGF-β.
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Nat Biotechnol, 2025, 10.1038/s41587-025-02649-1
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Nat Cell Biol, 2025, 27(8):1240-1255
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Nat Cell Biol, 2025, NONE
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| S8664 |
GSK3326595 (Pemrametostat, EPZ015938)
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Pemrametostat (GSK3326595, EPZ015938) is an orally active, potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) and potently inhibits tumor growth in vitro and in vivo in animal models.
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MedComm (2020), 2025, 6(6):e70150
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J Med Chem, 2025, 68(4):4217-4236
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J Med Chem, 2025, 68(5):5097-5119
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| E1939 |
ART899
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ART899, a derivative of ART558 is a potent, specific allosteric inhibitor of DNA polymerase theta (Polθ), specifically inhibits Polθ MMEJ activity with IC50 of 180 nM. It specifically radiosensitizes tumor cells and have a potent stand-alone antitumor effect in cancer cells.
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| S7102 |
Berzosertib (VE-822)
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Berzosertib (VE-822, VX970, M6620) is an ATR inhibitor with IC50 of 19 nM in HT29 cells.
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Cancer Cell, 2025, 43(8):1530-1548.e9
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Nat Cell Biol, 2025, 27(1):59-72
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Nat Commun, 2025, 16(1):3613
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| S8883 |
LLY-283
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LLY-283 is a novel and selective inhibitor of protein arginine methyltransferase 5 (PRMT5). This compound inhibits PRMT5 enzymatic activity in vitro and in cells with IC50 of 22 nM and 25 nM, respectively. It shows antitumor activity.
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Nucleic Acids Research, 2026, gkag016
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Mol Cancer Res, 2025, 23(2):107-118
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Res Sq, 2025, rs.3.rs-5936706
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