AVex-73 is a muscarinic M1 agonist potentially for the treatment of Alzheimer's disease

Avitinib is an orally available, irreversible, epidermal growth factor receptor (EGFR) mutant-selective inhibitor, with potential antineoplastic activity.

Avitinib is an orally available, irreversible, epidermal growth factor receptor (EGFR) mutant-selective inhibitor, with potential antineoplastic activity.

NIK SMI1 is a potent, selective small molecule inhibitor of NF-κB inducing kinase (NIK) with Ki of 230±170 pM; only inhibits 3 out of 222 off-target kinases (KHS1, LRRK2, and PKD1) with >75% inhibition at 1 uM; potently inhibits anti-LTβR-induced nuclear p52 levels in anti-LTβR-stimulated HeLa cells, with no effect on canonical signaling; inhibits BAFF and CD40 signaling, suppresses immune responses in vivo; suppresses disease biomarkers and improves survival and renal function in NZB/W F1 mice.

ILK-IN-2 (OSU-T315 analog) is a ILK inhibitor.

AZ191 is a potent and selective DYRK1B inhibitor with IC50 of 17 nM, about 5- and 110-fold selectivity over DYRK1A and DYRK2, respectively.

AZ304 is a novel potent, dual BRAF inhibitor targeting the kinase domains of wild type BRAF, V600E mutant BRAF and wild type CRAF with IC50 of 79 nM, 38 nM and 68 nM, respectively.

AZ31 is a novel ATM inhibitor.

CYM50308 is a potent, selective and high affinity sphingosine-1-phosphate receptor 4 (S1P4-R) agonist with an EC50 of 56 nM. CYM50308 displays 37-fold more selective for S1P4-R than S1P5-R. CYM50308 has no activity at S1P1-R, S1P2-R and S1P3-R subtypes at concentrations up to 25 μM.

Unique F-box/LRR-repeat protein 2 (FBXL2) activator

AZ505 ditrifluoroacetate is a potent and selective SMYD2 inhibitor with IC50 of 0.12 μM.

BMS 191011 is an activator of large-conductance calcium-activated potassium (BKCa) channels that increases maximum potassium current to 126% of control in X. laevis oocytes expressing human BKCa channels when used at a concentration of 1 μM.

PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor, binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site.

AZ876 is a novel high-affinity LXR agonist.

AZD0865 is a potent agent that inhibits gastric H(+),K(+)-ATPase activity and acid formation in vitro, with a fast onset of effect.

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.

Nisoxetine hydrochloride is a potent and selective inhibitor of noradrenaline transporter (NET), with a Kd of 0.76 nM. Nisoxetine hydrochloride is an antidepressant and local anesthetic, it can block voltage-gated sodium channels.

AZD-3463 is an ALK/IGF1R inhibitor which overcomes multiple mechanisms of acquired resistance to crizotinib.

AZD5582 is a novel class of dimeric Smac mimetics as potent IAP antagonist; binds potently to the BIR3 domains of cIAP1, cIAP2, and XIAP (IC50 = 15, 21, and 15 nM, respectively).

AZD-9291 is a potent and selective mutated forms EGFR inhibitor(Exon 19 deletion EGFR IC50=12.92 nM, L858R/T790M EGFR IC50= 11.44 nM, wild type EGFR IC50= 493.8 nM).

CRT5 is a pyrazine benzamide that prevents activation of all three isoforms of PKD in endothelial cells treated with VEGF (IC50s = 1, 2, and 1.5 nM for PKD1, PKD2, and PKD3, respectively).

BMS-189453 (BMS189453, BMS453) is a synthetic retinoid that acts as an agonist of RARβ and an antagonist of RARα and RARγ.

RO2959 is a novel, potent and selective CRAC current inhibitor. RO2959 completely inhibited cytokine production as well as T cell proliferation mediated by TCR stimulation or MLR (mixed lymphocyte reaction). RO2959 potently blocked TCR triggered gene expression and T cell functional pathways similar to CsA and another calcineurin inhibitor FK506.

TCPOBOP is an agonist of the constitutive androstane receptor (CAR) (EC50 = 20 nM). TCPOBOP enhances the nuclear receptor CAR transactivation of cytochrome P450 (CYP), as dose-dependent direct agonist of CAR. The most potent known member of the phenobarbital-like class of CYP-inducing agents. TCPOBOP has been used for enhancing Mcl-1-Italics promoter functions in mouse hepatoma cells. TCPOBOP has also been used to study constitutive androstane receptor(CAR)-induced gene expression in mouse hepatocytes.

A potent, selective inhibitor of human LIMK1 with IC50 of 38 nM .

PF-05150122 is a potent, state-dependent, subtype selective Nav1.7 inhibitor with IC50 of 21 nM, no significant activity against Nav1.5..

LGD-2226 (LGD2226) is an orally active, selective androgen receptor modulator (SARM) with binding Ki of 1 nM, >1000-fold selectivity over GR,PR, MR and ER.

Pyrrolnitrin is an antibiotic isolated from Pseudomonas pyrrocinia. Pyrrolnitrin shows a broad spectrum of antibiotic activity against fungi, yeast and gram-positive bacteria.

Azoramide is a small-molecule modulator of the unfolded protein response with antidiabetic activity.

Azoxystrobin is a systemic, broad-spectrum fungicide belonging to the class of methoxyacrylates,which are derived from the naturally-occurring strobilurins.