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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC23412 BMS-955829 A potent, selective, low glutamate fold shift (2.4) mGluR5 positive allosteric modulator with EC50 of 2.6 nM, without inherent mGluR5 agonist activity (EC50>30 uM).
DC22804 CMPD-1 A potent, selective, non-ATP-competitive inhibitor of p38α-mediated MK2a phosphorylation with apparent Ki of 330 nM.
DC22742 KAB-18 A potent, selective, noncompetitive human α4β2 nAChRs negative allosteric modulator with IC50 of 13.5 uM, displays no inhibitory activity on Hα3β4 nAChRs at 100 uM..
DC23195 CBR-5884 Featured A potent, selective, noncompetitive inhibitor of 3-phosphoglycerate dehydrogenase (PHGDH) with IC50 of 7 uM.
DC11746 JNJ-27141491 A potent, selective, noncompetitive, orally active CCR2 antagonist with IC50 of 172 nM.
DC22449 PD-146176 A potent, selective, non-competitve inhibitor of 15-lipoxygenase (15-LOX) with Ki of 197 nM.
DC22447 FAAH-IN-2 A potent, selective, noncovalent FAAH inhibitor with IC50 of 28 nM toward human FAAH and 100 nM toward rat FAAH.
DC11756 SR 140333 A potent, selective, non-peptide NK1 receptor antagonist with Ki of 0.74 nM, IC50 of 1.6 nM.
DC22680 Conivaptan A potent, selective, nonpeptide vasopressin V1A and V2 receptor antagonist with Ki of 0.48 nM and 3.04 nM respectively.
DC21738 TBC3486 A potent, selective, non-peptidic integrin α4β1 (VLA-4) antagonist with IC50 of 9 nM, displays 200-fold selectivity over α4β7 (IC50=2.1 uM).
DC20617 AA-CW236 Featured A potent, selective, non-pseudosubstrate inhibitor of O(6) -alkylguanine DNA methyltransferase (MGMT) with low-nanomolar potency.
DC21593 RUC-4 Featured A potent, selective, non-RGD-mimetic αIIbβ3 integrin receptor antagonist with IC50 of 45 nM, with no activity on αVβ3 receptors. .
DC23596 Luseogliflozin A potent, selective, orally acitve SGLT2 inhibitor with IC50 of 2.26 nM, 1650-fold selectivity over SGLT1.
DC21307 MKC-733 A potent, selective, orally active 5-HT3 receptor agonist with high affinity for canine intestinal smooth muscle 5-HT3 receptors.
DC11667 PF-592379 A potent, selective, orally active agonist of dopamine D3 receptor with EC50 of 21 nM.
DC21606 SB-357134 A potent, selective, orally active and CNS penetrant 5-HT6 receptor antagonist with pKi of 8.5, displays 1300-fold selectivity over other 13 5-HT receptor subtypes.
DC20774 VTP 37948 A potent, selective, orally active BACE1 inhibitor for the treatment of Alzheimer's disease..
DC20665 AMG 8718 A potent, selective, orally active BACE1 inhibitor with IC50 of 0.7 nM, demonstrates limited selectivity for over BACE2 and high selectivity both renin and pepsin.
DC20324 BRS-3 agonist Compound A A potent, selective, orally active bombesin receptor subtype-3 (BRS-3) agonist with EC50 of 250/100 nM for human/rat BRS-3, resp+H1437+M1438.
DC20325 BRS-3 agonist Compound A racemate A potent, selective, orally active bombesin receptor subtype-3 (BRS-3) agonist with EC50 of 270/130 nM for human/rat BRS-3, respectively.
DC21187 JTE907 Featured A potent, selective, orally active cannabinoid CB2 receptor inverse agonist with Ki of 35.9, 1.55 and 0.38 nM for human, mouse and rat CB2, respectively.
DC21793 VER-250840 A potent, selective, orally active Chk1 inhibitor with IC50 of < 1 nM, Ki=69 pM.
DC22898 L-365260 A potent, selective, orally active cholecystokinin receptor 2 (CCK2) antagonist with IC50 of 2 nM.
DC22485 Gefitinib hydrochloride Featured A potent, selective, orally active EGFR inhibitor with IC50 of 23 nM.
DC21443 ONO-5334 A potent, selective, orally active inhibitor of cathepsin K with Ki of 0.1 nM, 0.049 nM and 0.85 nM for human, rabbit and rat cathepsin K, respectively.
DC23340 CCT-251455 A potent, selective, orally active monopolar spindle 1 (MPS1) inhibitor with IC50 of 3 nM, with no activity for CDK2 and Aurora A (IC50>40 uM).
DC11704 CFI-401870 A potent, selective, orally active Mps1 (TTK) inhibitor with IC50 of 3.1 nM.
DC25200 PF-1355 Featured PF-1355 is a potent, selective, orally active Myeloperoxidase (MPO) inhibitor with EC50 of 1.47 uM.
DC22900 MLE-4901 Featured A potent, selective, orally active neurokinin 3 (NK3R) antagonist for the treatment of schizophrenia.
DC22664 Fezolinetant Featured Fezolinetant is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes.

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