A selctive small molecule inhibitor of the transcription factor GATA-binding protein 2 (GATA2).

A potent, selective, orally active neurokinin 3 (NK3R) antagonist for the treatment of schizophrenia.

Ibiglustat (succinate) is a selective inhibitor of glucosylceramide synthase.

ML390 is a human DHODH Inhibitor That Induces Differentiation in Acute Myeloid Leukemia. ML390 bioactivity: ER-HOX-GFP (EC50 μM) = 1.8 ± 0.6; U937 (EC50 μM) = 8.8 ± 0.8; THP-1 (EC50 μM) = 6.5 ± 0.9; DHODH (IC50, μM) = 0.56 ± 0.1. ML390 may offer insight into the mechanism of overcoming differentiation arrest, and will translate into a starting point for a much-needed new and potent treatment for patients with acute myeloid leukemia. Inhibitors of dihydroorotate dehydrogenase (DHODH) showed activity to induce differentiation in multiple animal models of AML in vitro and in vivo. DHODH inhibitors demonstrated effective at prolonging survival in animal models of leukemia.

A selective prostaglandin E receptor subtype 4 (EP4) antagonist with pKi of 8.5.

BIBF-1202 is the carboxylate metabolite of BIBF 1120, which is an oral triple angiokinase inhibitor targeting VEGFR, PDGFR, FGFR.

ML193 (CID 1261822) is a potent, selective GPR55 antagonist with IC50 of 221 nM, shows >27-, >145- and >145-fold selectivity for GPR55 over CB1, GPR35 and CB2, respectively.

PFKL activator NA-11 is a small-molecule, selective PFKL activator, inhibits the NOX2-dependent oxidative burst in neutrophils by activating the glycolytic enzyme phosphofructokinase-1 liver type (PFKL).

PDD 00017273 is the first-in-class, selective inhibitor of poly(ADP-ribose) glycohydrolase (PARG) with Kd, biochemical EC50 of 1.45 nM, 26 nM.

A xanthone derivative that fuctions as an EP and DP receptor antagonist.

MMV390048 is a novel potent Plasmodium PI4K inhibitor with IC50 of 28 nM against intraerythrocytic life cycle stages of P. falciparum (NF54 drug-sensitive strain).

PF-06446846 (PF-6446846) is a potent, highly selective inhibitor of PCSK9 translation with IC50 of 0.3 uM for inhibition the secretion of PCSK9 by Huh7 cells.

GZD856 is a novel and orally bioavailable PDGFRα/β inhibitor with IC50s of 68.6 and 136.6 nM, respectively. Anti-lung cancer activities. Also a Bcr-AblT315I inhibitor with IC50s of 19.9 and 15.4 nM for Bcr-Abl and T315I mutant.

Bruton tyrosine kinase inhibitor

TIC10 inactivates Akt and ERK to induce TRAIL through Foxo3a, possesses superior drug properties: delivery across the blood-brain barrier, superior stability and improved pharmacokinetics

NAcM-OPT is an orally bioavailable cullin neddylation 1 (DCN1) inhibitor, which potently inhibits the DCN1-UBE2M interaction.

LIT-001 trifluoroacetate (LIT001) is the first nonpeptide Oxytocin receptor (OT-R) agonist with EC50 of 55 nM, Emax=96%.

AMG 009 is an orally active, small molecule CRTH2 (chemoattractant receptor-homologous molecule expressed on Th2 cells) and DP (D prostanoid) dual antagonist, which was in preclinical development in the US for the treatment of asthma and allergic rhinitis.

SKLB-23bb is an orally bioavailable HDAC6-selective inhibitor and also has microtubule-disrupting ability.

NSC 663284 (SPS8I1;DA3003-1) is a potent inhibitor of the dual specificity protein phosphatase Cdc25 with Ki of 9/95//89 nM for Cdc25A/Cdc25B2/Cdc25C, displays 20- and 450-fold more selective over VHR or PTP1B phosphatases.

BAPTA/AM is a membrane permeable form of BAPTA, a selective chelator of Ca2+.

Daunomycinone (NSC-109351) is a metabolite of daunomycin. Daunomycin is an antibiotic with antitumor activity.

Carubicin HCl is an anthracycline antineoplastic antibiotic isolated from the bacterium Actinomadura carminata. Carubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis.

Zotarolimus (ABT-578, A 179578) is a semi-synthetic analogue of rapamycin, inhibits FKBP-12 binding with IC50 of 2.8 nM and shows less potent systemic immunosuppression than rapamycin.

Pristinamycin IA (Mikamycin B) is a cycle-peptidic macrolactone antibiotic. Pristinamycin IA is a substrate of P-glycoprotein and inhibits its function. Pristinamycin IA is active against StaphyloEoccus and Srreptococcus.

Photochlor, also known as HTTP, is a lipophilic, second-generation, chlorin-based photosensitizer. Upon intravenous administration, HPPH selectively accumulates in the cytoplasm of cancer or pre-cancerous cells. When laser light is applied, a photodynamic reaction between HPPH and oxygen occurs, resulting in the production of cytotoxic free radicals and singlet oxygen and free radical-mediated cell death. Compared to the first-generation photosensitizer porfimer sodium, HPPH shows improved pharmacokinetic properties and causes only mild skin photosensitivity which declines rapidly within a few days after administration.

Tildipirosin is a 16-membered macrolide used as an antibiotic in veterinary medicine. Like other macrolides, it inhibits protein synthesis in bacteria and blocks the production of biofilms.

Topotecan Hydrochloride (SKF 104864A Hydrochloride) is a Topoisomerase I inhibitor with potent antineoplastic activities.

Daptomycin is a lipopeptide antibiotic with rapid in vitro bactericidal activity against gram-positive organisms.

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