Novel inhibitors

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Cat. No.	Product Name	Field of Application
DC24073	LY-2584702 hydrochloride Featured	LY2584702 is a potent, selective, ATP-competitive inhibitor of P70S6 kinase-1 (p70S6K1) with IC50 of 4 nM.
DC22140	LY2623091	LY2623091 (LY-2623091) is an orally administered mineralocorticoid receptor antagonist for the treatment of essential hypertension and chronic kidney disease..
DC23444	LY2624803	LY2624803 is a novel potent histamine H1 and 5HT-2A receptor modulator in the pipeline for treating insomnia..
DC7665	Gandotinib(LY2784544) Featured	LY2784544 is a potent JAK2 inhibitor with IC50 of 3 nM, effective in JAK2V617F, 8- and 20-fold selective versus JAK1 and JAK3. Phase 2.
DC23510	LY2794193 Featured	LY2794193 is a highly potent and selective mGlu3 receptor agonist with Ki of 0.93 nM and EC50 of 47 nM, >100-fold selectivity over mGlu2 receptor..
DC22595	LY2857785	LY2857785 is a potenrt, reversible and ATP-competitive CDK9 inhibitor with IC50 of 11 nM, also inhibits CDK8 (IC50=16 nM) and weakly inhibits CSK7 (IC50=246 nM).
DC11681	LY2922470	LY2922470 (LY-2922470) is a potent, selective, orally available GPR40 agonist with EC50 of 7 nM.
DC21340	LY 2979165	LY2979165 (MP-101) is the alanine prodrug of LY2812223, a selective orthosteric mGlu2 receptor agonist.
DC23688	LY-3000328 Featured	LY 3000328 is a potent and selective Cathepsin S (Cat S) inhibitor with IC50s of 7.7 and 1.67 nM for hCat S and mCat S, respectively.
DC7210	LY-303511(Nv-128) Featured	LY303511, an inactive analogue of LY294002, is a mTOR inhibitor that did not inhibit PI3-K.
DC7776	LY-3039478	LY3039478 a orally bioavailable, novel small molecule Notch inhibitor with an IC50 of ~1nM in most of the tumor cell lines tested.
DC23718	LY305	LY305 (LY-305) is a non-steroidal selective androgen receptor modulator (SARM) with Ki of 2.03 nM, demonstrates potent agonist activity in the aforementioned C2C12 cellular assay (EC50=0.499 nM).
DC21259	LY 3130481 Featured	LY3130481 (CERC611) is a potent, selective, noncompetitive TARP γ8-associated AMPA receptors with IC50 of 65.3 nM (GluA1/TARP γ-8), with no activity for γ-2 (cerebellum) or other TARP members.
DC12507	LY3143921	LY3143921 (LY-3143921) is an orally available, potent, selective inhibitor of Cdc7 kinase inhibitor, inhibits CDC7/DBF4 I and pMCM2 (S53) with IC50 values of 3.3 nM and 290 nM, respectively..
DC11330	LY320135 Featured	LY320135 is a selective cannabinoid (CB) receptor 1 antagonist (Kis = 224 and >10,000 nM for CB1 and CB2, respectively, in vitro).
DC21253	N-(3-((4aR,7aS)-2-amino-6-(5-fluoropyrimidin-2-yl)-4a,5,6,7-tetrahydropyrrolo[3,4-d][1,3]thiazin-7a(4H)-yl)-4-fluorophenyl)-5-methoxypyrazine-2-carboxamide Featured	LY3202626 is a small molecule non-selective BACE1 inhibitor, causes dose-dependent reductions in CSF and plasma Aβ concentrations, shows potential for the treatment of Alzheimer's disease..
DC10640	LY3214996 Featured	LY3214996 is a selective and novel ERK1/2 inhibitor with IC50 of 5 nM for both enzymes in biochemical assays. It potently inhibits cellular phospho-RSK1 in BRAF and RAS mutant cancer cell lines.
DC12261	LY3295668 (AK-01)	LY3295668 is a potent, orally active and highly specific Aurora-A kinase inhibitor, with Ki values of 0.8 nM and 1038 nM for AurA and AurB, respectively.
DC9314	LY 344864	LY344864 is a selective receptor agonist with an affinity of 6 nM (Ki) at the recently cloned 5-HT1F receptor.
DC22784	LY-345899 Featured	LY-345899 (LY345899) is a novel potent, cytoplasmic and mitochondrial methylenetetrahydrofolate dehydrogenase MTHFD1 and MTHFD2 inhibitor with IC50 of 96 nM and 663 nM, respectively; MTHFD2 is a novel target for drug development.
DC11323	LY354740	LY354740 is an agonist of the group II metabotropic glutamate receptor (mGluR) subtypes mGluR2 and mGluR3 (Kis = 99 and 94 nM, respectively).
DC23829	LY379196	LY379196 is a highly specific PKCβ inhibitor with IC50 of 30-50 nM for PKCβI and PKCβII, displays >10-fold selectivity of PKCα, δ, η, and γ (>600 nM).
DC23597	LY-404187	LY-404187 is a potent, selective, positive allosteric modulator of AMPA receptor (AMPAR) with EC50 of 1.3 uM.
DC22435	LY487379 Featured	LY-487379 is a potent, selective positive allosteric modulator of mGluR2 (EC50=0.27 uM) without activity at mGluR3; shows no intrinsic agonist or antagonist activity at hmGluR2, markedly potentiates glutamate-stimulated [35S]GTPgammaS binding at hmGluR2; potentiates synaptically evoked mGluR2 responses in rat hippocampal slices, modulates excitatory synaptic transmission in the rat globus pallidus.
DC22420	LY-487379 hydrochloride	LY-487379 is a potent, selective positive allosteric modulator of mGluR2 (EC50=0.27 uM) without activity at mGluR3.
DC7459	LY500307	LY500307 is a potent, selective estrogen receptor β agonist with EC50 of 0.66 nM, 32-fold selectivity against estrogen receptor α. Phase 2.
DC23636	LY-503430	LY-503430 is a novel AMPA receptor (AMPAR) potentiator that selectively enhances glutamate-induced calcium influx into HEK293 cells transfected with human GLUA1, GLUA2, GLUA3, or GLUA4 AMPA receptors with EC50 of 0.1-4 uM.
DC21260	LY-83583	LY-83583 is an inhibitor of soluble guanylate cyclase (sGC) and of cGMP production, inhibits sGC in human platelets with IC50 of 2 uM.
DC24081	Lyn-IN-1 (Synonyms: Bafetinib analog) Featured	Lyn-IN-1 is a potent and selective dual Bcr-Abl/Lyn inhibitor..
DC20440	LYPLAL1-IN-11	LYPLAL1-IN-11 is a potent, selective, covalent inhibitor of lysophospholipase-like 1 (LYPLAL1) with IC50 of 6 nM.

Novel inhibitors

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