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

PSMA-BCH also known as NOTA-PSMA, is a PSMA- NOTA-conjugated precursor. 68Ga-PSMA-BCH can be used for prostate cancer imaging. Al18F-PSMA-BCH can be used for prostate cancer imaging as a novel 18F PET radiotracer. 64Cu-PSMA-BCH is a new radiotracer for delayed PET imaging of prostate cancer. 64Cu-PSMA-BCH was PSMA specific and showed high stability in vivo with lower uptake in liver than 64Cu-PSMA-617. Biodistribution in mice and PCa patients showed similar profile compared with other PSMA ligands and it was safe with moderate effective dosimetry.

HYNIC-PSMA is a PSMA based ligand, which can bind radio-active metal ion and used as a tumor-imaging agent in prostate cancer. 99mTc-HYNIC-PSMA is a novel technetium-99m-labeled small-molecule inhibitor of prostate-specific membrane antigen (PSMA) for detection of prostate cancer. 99mTc-HYNIC-PSMA showed high tracer uptake (with a tumor-to-background ratio of 9.42 ± 2.62) in the malignant lesions of PCa patients, making it a promising radiopharmaceutical imaging method for site-specific management of PCa.

WDR5-IN-6 is a WDR5 inhibitor.

Antibacterial agent 133 (4l) is an antimicrobial agent

TNF-α-IN-9 (compound 48) is a analog of NDM-1 inhibitor-3

PHGDH-IN-3 is an orally active phosphoglycerate dehydrogenase (PHGDH) inhibitor. PHGDH-IN-3 inhibits PHGDH with an IC50 value of 2.8 μM. PHGDH-IN-3 can be used for the research of cancer[1].

PARP10-IN-2 is a potent mono‐ADP‐ribosyltransferase PARP10 inhibitor with an IC50 of 3.64 μM for human PARP10. PARP10-IN-2 reveals potent inhibition on PARP2 and PARP15 with IC50s of 27 μM and 11 μM for human PARP2 and human PARP15, respectively[1].

S19-1035 is a highly potent and specific aldo-keto reductase 1C3 (AKR1C3) inhibitor. S19-1035 inhibits AKR1C3 with an IC50 value of 3.04 nM. S19-1035 can be used for the research of tumor.

PRMT6-IN-3 (compound 25) is a selective PRMT6 inhibitor

Skp2 inhibitor 1 (compound 14i) is a potent and selective Skp2 inhibitor

KIF18A-IN-3 is a potent KIF18A inhibitor (IC50=61 nM). KIF18A-IN-3 causes significant mitotic arrest and increases the number of mitotic cells in tumor tissues. KIF18A-IN-3 can be used for researching cancer[1].

LOX-IN-3 Dihydrochloride is an orally active and selective lysyl oxidase (LOX) inhibitor.

GFP16 is a low affinity antiprion compound.

GW6340 is an intestinal-specific LXR agonist.