A potent tyrosine kinases inhibitor with IC50 of 13/9/3/26/2 nM for Lck/Btk/Lyn/Syk/Txk..

YM-244769 dihydrochloride is a potent Na+/Ca2+ exchange (NCX) inhibitor that preferentially inhibits NCX3 (IC50=18 nM). Neuronal and renal protection.

NS3861 fumarate is an agonist of nicotinic acetylcholine receptors (nAChRs) and binds with high affinity to heteromeric α3β4 nAChR. The binding Ki values of 0.62, 25, 7.8, 55 nM for α3β4, α3β2, α4β4, α4β2, respectively.

KI-7 is an adenosine A2B receptor positive allosteric modulator.

TC-E 5003 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor.

Lazabemide(Ro 19-6327/000) is selective, reversible monoamine oxidase B (MAO-B) inhibitor (IC50 values are 0.03 and > 100 μM for MAO-B and MAO-A respectively).

SN-6 is a selective Na+/Ca2+exchange (NCX) inhibitor, displaying some selectivity for NCX1.

Lavendustin B is a Tyrosine Kinase Inhibitor amd an inhibitor of HIV-1 integrase (IN) interaction with its cognate cellular cofactor, lens epithelium-derived growth factor (LEDGF/p75).

Adipamidoxime(NSC 70868) is a new bioactive compoud.

Y16 is an inhibitor of G-protein–coupled Rho GEFs; works synergistically with Rhosin/G04 in inhibiting LARG-RhoA interaction, RhoA activation, and RhoA-mediated signaling functions.

SDZ285428 is a CYP51 inhibitor. SDZ285428 inhibits Trypanosoma cruzi (TC) CYP51 with I/E2 <1 (5 min) and I/E2=9 (1 h). SDZ285428 inhibits Trypanosoma brucei (TB) CYP51 with I/E2 <1 (5 min) and I/E2=35 (1 h).

Clanfenur is a substituted benzoylphenylurea and an analogue of the pesticide diflubenzuron with potential antineoplastic activity.

GK921 is a transglutaminase 2 (TGase 2) inhibitor with average GI50 of 0.9 uM in cancer cell lines.

4-oxo-4-HPR is a recently identified fenretinide metabolite, induces marked G2-M cell cycle arrest and apoptosis in fenretinide-sensitive and fenretinide-resistant cell lines.

Lu AF21934 is a brain-penetrating positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu4),reduces the harmaline-induced hyperactivity

Lvguidingan is a potent anticonvulsant agent. Lvguidingan also has sedative-hypnotic, tranquilizing, and muscle-relaxing actions. Lvguidingan can be used as antiepileptic agent.

Valrocemide (TV1901,VGD)) has a broad spectrum of anticonvulsant activity and promising potential as a new AED.

CPI-1189 prevents apoptosis and reduces glial fibrillary acidic protein immunostaining in a TNF-alpha infusion model for AIDS dementia complex.

AZD1283 is a potent antagonist of the P2Y12 receptor with EC50 of 3.0 ug/kg/min, TI >10; with binding IC50 of 11 nM.

ADT-OH is a derivative of anethole dithiolethione (ADT) and synthetic hydrogen sulfide (H2S) donor.

trans-Tranilast (trans-MK-341) is an antiallergic drug, used to treat bronchial asthma, allergic rhinitis and atopic dermatitis.

2,4-Pyrimidinediamine with linker is a patent compound in WO2013055780A1, Page 71; multikinase inhibitor and has a -NH2 terminal linker for further synthesis.

JIB-04 Z-isomer, also known as NSC 693627, is an isomer of JIB-04. JIB-04 is a Jumonji histone demethylase inhibitor. JIB-04 selectively blocks cancer cell growth in vitro and diminishes tumor growth in H358 and A549 mouse xenograft models in vivo. JIB-04 can prolong survival in a mouse model of breast cancer.

Digitonin, a glycoside obtained from Digitalis purpurea, could increase cell permeability by binding to cholesterol molecules and reduce tumor growth.

TG8-69 is a peripherally restricted, highly potent, selective, aqueous-soluble EP2 antagonist with Kb of 48.5 nM.

Isoindigotin is a potential antileukemic agent.

MK-6240 is a positron emission tomography (PET) tracer for neurofibrillary tangles (NFTs), exhibiting high specificity and selectivity for binding to NFTs.

Rheb inhibitor NR1 is a small molecule that binds Rheb in the switch II domain (IC50=2.1 uM, Kd=1.5 uM) and selectively blocks mTORC1 signaling, potently inhibits mTORC1 driven phosphorylation of S6K1 but does not inhibit phosphorylation of AKT or ERK.

DS55980254 (DS 55980254) is potent, selective and orally active PTDSS1 (phosphatidylserine synthetase 1) inhibitor, suppresses phosphatidylserine (PS) production activity of PTDSS1 (IC50=100 nM) in cell-free assays, but not that of PTDSS2.

Taspoglutide is a glucagon-like peptide-1(GLP-1) agonist for treatment of type 2 diabetes.