BTK inhibitor 1, a pyrazolo[3,4-d]pyrimidine analog, is a novel and potent inhibitor of Btk kinase extracted from PCT Int. Appl. (2012), WO 2012158843 A2 20121122..

Erteberel (also known as LY500307) is a novel, potent and selective estrogen receptor beta (ERβ) inhibitor with Ki and EC50 of 1.54 nM and 3.61 nM, respectively. It has anti-tumor activities and was developed for the treatment of benign prostatic hyperplasia. LY500307 was well tolerated in BPH patients with LUTS at doses up to 25 mg […]

Calcium methyltetrahydrofolate (NSC173328), a synthetic derivative of folic acid, is the calcium salt of levomefolic acid, which has the potential for treatment of cardiovascular disease and advanced cancers such as breast and colorectal cancers. Calcium methyltetrahydrofolate is the predominant, naturally occurring form of folate. It is synthesized by reduction of folic acid to tetrahydrofolic acid […]

GSTO-IN-2 is a novel and potent glutathione S-transferase inhibitor with IC50s of 3.6, 16.3, and 1.4 μM for GSTA2, GSTM1, and GSTP1-1.

AMG2850 is a novel, potent, orally bioavailable and selective small molecule antagonist of transient receptor potential melastatin 8 (TRPM8). TRPM8 has been implicated in pain and migraine based on dorsal root- and trigeminal ganglion-enriched expression, upregulation in preclinical models of pain, knockout mouse studies, and human genetics. AMG2850 is potent in vitro at rat TRPM8 […]

LY-222306 is a novel and potent glycinamide ribonucleotide formyltransferase (GARFT) inhibitor with a Ki of 0.77 nM.

Fumonisin B1 (HSDB7077; RT-013063; HSDB-7077; RT013063) is a naturally occuring mycotoxin/fungal metabolite isolated from Fusarium moniliforme. It acs as a novel and potent inhibitor of sphingosine N-acyltransferase (ceramide synthase) which disrupts de novo sphingolipid biosynthesis.

JNJ4796 is a novel, potent and oral bioactive fusion inhibitor of influenza virus, which neutralizes influenza A group 1 viruses by inhibiting hemagglutinin (HA)-mediated fusion. JNJ4796 was identified through structural knowledge of the interactions and mechanism of anti-stem bnAb CR6261. It mimics the functionality of the broadly neutralizing antibodies (bnAbs). Recent characterization of broadly neutralizing […]

PR-104, a novel, potent, non-toxic, small-molecule, hypoxia-activated, 3,5-dinitrobenzamide nitrogen mustard, is a drug from the class of hypoxia-activated prodrugs (HAPs), which is being researched as a potential anti-cancer therapeutic agent. It is a phosphate ester “pre-prodrug” that is rapidly converted to the HAP PR-104A in the body. PR-104A is in turn metabolised to reactive nitrogen […]

Rimeporide (also known as EMD-87580) is a novel, potent and selective inhibitor of the sodium/hydrogen Na+/H+ exchanger (NHE-1) with a potential to be used as a therapeutic agent for the treatment of heart failure and for patients with Duchenne muscular dystrophy.