LEO 39652 is a novel PDE4 inhibitor with IC50 of 3.8 nM and selected as a clinical candidate as it is potent and rapidly degraded by blood and liver to inactive metabolites.

MyD88-IN-1 is a potent MyD88 inhibitor.

TRPC6-PAM-C20 is a selective TRPC6 positive allosteric modulator. TRPC6-PAM-C20 selectively activates TRPC6 over other TRP channels and also activates TRPA1. TRPC6-PAM-C20 induces transient increase in intracellular Ca2+ in HEK cells expressing TRPC6 (EC50=2.37 μM).

Osunprotafib (ABBV-CLS-484) is a potent PTPN1 and PTPN2 inhibitor with subnanomolar activity. Osunprotafib has antitumor activity, enhances the immune response and increases the sensitivity of tumors to immune-mediated killing.

Trotabresib (CC-90010) is a reversible and orally active BET inhibitor. CC-90010 is applied in the study for advanced solid tumors.

Pacritinib Citrate is the citrate salt form of pacritinib, an orally bioavailable inhibitor of Janus kinase 2 (JAK2).

SMN2 splicing modulator TEC-1 is a novel specific, CNS penetrant small molecule SMN2 splicing modulator, increases the expression level of FL-SMN2 mRNA and decreases the expression level of Δ7 mRNA.TEC-1 showed higher selectively (>60-fold) on galactosylceramidase and huntingtin gene expression compared to previously reported compounds (e.g., SMN-C3) due to off-target effects on cryptic exon inclusion and nonsense-mediated mRNA decay.TEC-1 modulates SMN2 splicing and displays disease-modifying effects in motor neurons derived from SMA patient iPSCs (GM24468).|TEC-1 rescues the phenotype in a murine model of spinal muscular atrophy (SMA).

Remibrutinib (LOU064) is a potent, highly selective covalent inhibitor of bruton tyrosine kinase (BTK) with IC50 of 1.3 nM, 2.5 nM and 18 nM for BTK, FcγR-induced IL8 and anti-IgM/IL4-induced CD69, respectively. Remibrutinib (LOU064) exhibits an exquisite kinase selectivity due to binding to an inactive conformation of BTK and has the potential for the treatment of autoimmune diseases.

A non-selective agonist of the dopamine D3 receptor (Ki=0.71 nM).

MtUng-IN-1 (Compound 18a) is a Uracil DNA glycosylase of Mycobacterium (MtUng) inhibitor (IC50: 300 μM). MtUng-IN-1 can be used for research of cancers and infectious diseases.

Anticancer agent 118, a N‑acylated ciprofloxacin derivative, has anti-bacterial and anticancer activities.

Zandelisib is a phosphatidylinositol 3-kinase (PI3K) extracted from patent WO2019183226 A1, Compound Example 1. Zandelisib selectively inhibits p110δ with an IC50 of 3.5 nM. Zandelisib functions as an antineoplastic.

Bentiamine is also known as Dibenzoyl Thiamine. Dibenzoyl Thiamine (Bentiamine), a derivative of thiamine, is rapidly absorbed into the body and converted to thiamine.

Nicotinamide ascorbate is a bioactive chemical.

Lateritin is a potent inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT), isolated from the mycelial cake of Gibberella lateritium IFO 7188[1]. Lateritin also inhibits the growth of a mini-panel of human cancer cell lines, gram-positive bacteria, and Candida albicans[2].

ENMD-2076 Tartrate is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.

AhR modulator-1 (compound 6-MCDF) is a selective and orally active aryl hydrocarbon receptor (AhR) modulator. AhR modulator-1 inhibits metastasis, in part, by inhibiting prostatic VEGF production prior to tumor formation. AhR modulator-1 also possess anti-estrogenic properties in rat uterus.

Molnupiravir, also known as EIDD-2801 and MK-4482, is an orally bioavailable form of a highly potent ribonucleoside analog that inhibits the replication of multiple RNA viruses including SARS-CoV-2, the causative agent of COVID-19. EIDD-2801 has been show

4,5-Dicaffeoylquinic acid ( Isochlorogenic acid C) possesses potent hepatoprotective and anti-HBV effects.IC50 value:Target: Anti-hepatitis natural produce.In vitro: To study anti-hepatitis effect of isochlorogenic acid C, anti-apoptotic and anti-injury properties of test compound were evaluated. The results showed that test compound at concentrations of 10 to 100 μg/ml significantly reduced the caspase-3 and transformed growth factor β1 (TGFβ1) levels of the D-GalN-challenged hepatocytes. Also, test compound improved markedly cell viability of the D-GalN-injured hepatocytes and produced a maximum protection rate of 47.28% at a concentration of 100 μg/ml. Furthermore, test compound significantly inhibited productions of HBsAg and HBeAg. Its maximum inhibitory rates on the HBsAg and HBeAg expressions were 86.93 and 59.79%, respectively. In addition, test compound significantly induced the HO-1 expression of HepG2.2.15 cells [1]. In vivo:

EPZ031686 is a noncompetitive inhibitor for SMYD3 and MEKK2 with a Ki=1.2 and 1.1 nM respectively.

RP-6685 is a potent, selective and orally active DNA polymerase theta (Polθ) inhibitor with an IC50 value of 5.8 nM (PicoGreen assay). RP-6685 shows antitumor efficacy in mouse tumor xenograft model.

UCM1306 is a potent and orally active human dopamine D1 receptor allosteric modulator (PAM). UCM-1306 increases the endogenous dopamine (DA) maximal effect both in human and mouse D1 receptors. UCM-1306 is not only for improving motor symptoms but also for addressing the key comorbid cognitive impairment associated with long-term Parkinson’s disease (PD).

VE-822 is a selective ATR inhibitor with an Ki value of 0.2 nM, >150 fold selectivity over ATM (Ki=34 nM), DNA-PK (Ki >4 uM) and mTOR (Ki >1 uM).

CCR4-IN-38 (CCR4-351) is a potent, selective, orally bioavailable CCR4 antagonist with IC50 of 50 nM (Chemotaxis inhibition).CCR4-IN-38 inhibits the recruitment of Treg into the tumor microenvironment (TME).CCR4-IN-38 elicits antitumor responses as a single agent or in combination with an immune checkpoint blockade.

TNG908 is a MTAP-cooperative PRMT5 inhibitor that can pass through the blood-brain barrier. TNG908 is 15 times more selective for MTAP null cell lines than MTAPWT cell lines, and can be used in cancer research.

AOH1996 is a proliferating cell nuclear antigen (PCNA) inhibitor. AOH1996 enhances PCNA and RPB1 interaction and interferes with TRC resolution and induces DNA double-stranded breaks in a transcription dependent manner. AOH1996 almost completely inhibits the growth of xenograft tumors without causing any discernible toxicity to experimental animals.AOH1996 has superior metabolic stability as compared to the AOH1160 parent molecule. 

Isoniazid is an antibacterial agent used primarily as a tuberculostatic.Target: AntibacterialIsoniazid is a prodrug and must be activated by a bacterial catalase-peroxidase enzyme that in M. tuberculosis is called KatG [1]. KatG couples the isonicotinic acyl with NADH to form isonicotinic acyl-NADH complex. This complex binds tightly to the enoyl-acyl carrier protein reductase known as InhA, thereby blocking the natural enoyl-AcpM substrate and the action of fatty acid synthase. This process inhibits the synthesis of mycolic acid, required for the mycobacterial cell wall. A range of radicals are produced by KatG activation of isoniazid, including nitric oxide, which has also been shown to be important in the action of another antimycobacterial prodrug PA-824 [2, 3]. Isoniazid is bactericidal to rapidly dividing mycobacteria, but is bacteriostatic if the mycobacteria are slow-growing [4].

EPZ-719 is a novel and potent SETD2 inhibitor ( IC50 = 0.005 μM) with a high selectivity over other histone methyltransferases.

PSMA-I&T is a PSMA-based radioligand. [177Lu]Lu-PSMA I&T can be uused for potential treatment of metastatic castration-resistant prostate cancer. 67 Ga-PSMA I&T can be used for Radioguided Surgery of Lymph Node Metastases With Biochemical Recurrence of Prostate Cancer