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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC22895 VU0477573 A potent, selective, brain penetrant partial negative allosteric modulator of mGlu5 receptor with Ki of 14 nM, Ca assay IC50 of 32 nM.
DC22964 PQ-10 Featured A potent, selective, brain penetrant PDE10A inhibitor with Ki of 4 nM.
DC11660 PF-4181366 A potent, selective, brain penetrant PDE9A inhibitor with IC50 of 1.8 nM.
DC23695 PF-05085727 A potent, selective, brain penetrant phosphodiesterase 2A (PDE2A) inhibitor with IC50 of 2 nM, >4,000-fold selectivity over PDE1 and PDE3-11.
DC22920 AMN 082 dihydrochloride A potent, selective, brain penetrant, orally acitve mGluR7 allosteric agonist that inhibits forskolin-stimulated cAMP accumulation in mGluR7b CHO cells with EC50 of 64±32 nM.
DC23640 ASP2535 A potent, selective, brain permeable, orally available glycine transporter-1 (GlyT1) inhibitor with IC50 of 92 nM (rat GlyT1), 50-fold selectivity over GlyT2.
DC11895 Foliglurax hydrochloride A potent, selective, brain-penetrant and orally bioavailable mGluR4 positive allosteric modulator with EC50 of 79 nM.
DC11894 Foliglurax A potent, selective, brain-penetrant and orally bioavailable mGluR4 positive allosteric modulator with EC50 of 79 nM.
DC20549 SHP2 inhibitor 11a-1 A potent, selective, cell active SHP2 inhibitor with IC50 of 200 nM, displays >5-fold selectivity against 20 other mammalian PTPs.
DC11948 CK2 inhibitor D11 A potent, selective, cell permeab anti-apoptotic protein kinase CK2 with Ki of 5 nM.
DC11858 BAY-678 Featured BAY-678 is a cell-permeable inhibitor of human neutrophil elastase (HNE).
DC22877 CPI703 A potent, selective, cell-active CBP/EP300 bromodomain inhibitor with IC50 of 0.47 uM for CBP.
DC25052 Src I338G-IN-3g A potent, selective, cell-permeable I338G v-Src inhibitor with IC50 of 430 nM, shows no inhibition of wild-type v-Src at 300 uM.
DC21474 PF-04781340 A potent, selective, CNS penetrant 5-HT2C receptor agonist with Ki of 3 nM and EC50 of 9 nM, without significant P-gp efflux liability.
DC22708 VU 0255035 A potent, selective, CNS penetrant and competitive orthosteric antagonist of M1 mAChR with IC50 of 132 nM, >75-fold selectivity over M2-M5.
DC22667 mGlu5 PAM 4k A potent, selective, CNS penetrant and orally bioavailable mGlu5 positive allosteric modulator that potentiates human mGlu5 with EC50 of 130 nM.
DC22684 JNJ-46778212 Featured A potent, selective, CNS penetrant and orally bioavailable mGlu5 positive allosteric modulator that potentiates human mGlu5 with EC50 of 260 nM.
DC11558 DLK-IN-14 A potent, selective, CNS penetrant dual leucine zipper kinase (DLK, MAP3K12) inhibitor with Ki of 3 nM.
DC11870 RORγt-IN-9a A potent, selective, CNS penetrant, orally bioavailable RORγt with pIC50 of 8.3 in FRET assays.
DC22730 JNJ-42253432 A potent, selective, CNS-penetrant P2X7 antagonist with pKi of 9.1 and 7.9 for rat and huamn P2X7 channel, respectively.
DC22903 SW-106 Featured SW106 is a potent, selective, competitive PTH/PTH-related peptide receptor (PPR) antagonist with IC50 of 0.99 uM.
DC11898 Gosogliptin A potent, selective, competitive, orally active dipeptidyl peptidase-4 (DPP-4) inhibitor with IC50 of 13 nM.
DC11899 Gosogliptin dihydrochloride A potent, selective, competitive, orally active dipeptidyl peptidase-4 (DPP-4) inhibitor with IC50 of 13 nM.
DC23069 KRAS G12C inhibitor 1 A potent, selective, covalent KRAS G12C inhibitor that selectively inhibit KRAS G12C-dependent signaling and cancer cell growth at sub-micromolar concentrations..
DC21442 ONO 2050297 A potent, selective, dual CysLT1 and CysLT2 antagonist with IC50 of 17 and 0.87 nM, respectively..
DC11666 BMS-470539 A potent, selective, full agonist of human and murine MC1R with EC50 of 16.8 and 11.6 nM, respectively.
DC20736 AZD 9272 A potent, selective, highly CNS-penetrant and orally available mGluR5 negative allosteric modulator Kd of 2.8 nM.
DC20723 AZD 2066 A potent, selective, highly CNS-penetrant mGluR5 antagonist.
DC11721 PF-06747775 A potent, selective, irreversible EGFR mutants with IC50 of 12, 3, 4 and 5 nM for EGFR L858R-T790M, Del-T790M, L858R, and EGFR Del, respectively.
DC22679 CM 572 A potent, selective, irreversible sigma-2 receptor partial agonist with Ki of 14.6 nM, >700-fold selectivity over sigma-1 receptors.

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