Anti-inflammatory agent 51 (compound 11d) is an amide/sulfonamide derivative with anti-inflammatory activities.

Tubulin inhibitor 35 (compound 6b) is a dual inhibitor of topoisomerase I and tubulin polymerization.

Eg5-IN-1 (compound 6c) is a potent kinesin family motor protein (Eg5) inhibitor

Manidipine 2Hcl (CV-4093) is a dihydropyridine compound and a calcium channel blocker for Ca2+ current with IC50 of 2.6 nM. IC50 value: 2.6 nMTarget: calcium channelManidipine is described to block T-type Ca2+ channels specifically and is also described to have a high selectivity for the vasculature, presenting negligible cardiodepression as compared to other Ca2+ channel antagonists. Manidipine is also described to not significantly affect norepinephrine levels, suggesting a lack of sympathetic activation with this compound. Manidipine reduces pro-inflammatory cytokines secretion in human endothelial cells and macrophages. Manidipine, unlike other third-generation dihydropyridine derived drugs, blocks T-type calcium channels present in the efferent glomerular arterioles, reducing intraglomerular pressure and microalbuminuria.

VVD-118313 (compound 5a) is a potent, selective JAK1 inhibitor. VVD-118313 targets an isoform-restricted allosteric cysteine to block JAK1-dependent trans-phosphorylation and cytokine signaling. VVD-118313 can be used for research of cancer.

IPN-60090 is an orally active and highly selective inhibitor of glutaminase 1 (GLS1; IC50=31 nM), with no activity observed against GLS-2. IPN-60090 exhibits excellent physicochemical and pharmacokinetic properties in vivo. IPN-60090 can be used for solid tumors research, such as lung and ovarian cancers.

DX-308 is a potent, selective dual CYP26A1/B1 inhibitor and retinoic acid metabolism blocking agent.DX308 does not interact with off‐target nuclear receptors or CYP450s, is not genotoxic, and is stable in skin, despite vigorous hepatic metabolism.Topical DX308 induces comedolysis and epidermal thickening without apparent adverse effects in vivo.DX308 shows potent modulation of retinoid‐responsive genes by DX308 in both healthy and keratinization disorder keratinocytes (KCs).DX 308 may present an improved therapeutic alternative for the treatment of keratinization disorders and other retinoid‐responsive skin ailments.

DX314 is a potent, specific CYP26B1 inhibitor with IC50 of 108 nM, >15-fold selectivity over CYP26A1.DX314 potentiates all-trans-RA (atRA) gene expression effects in healthy and diseased reconstructed human epidermis (RHE).DX314 potentiates the effects of atRA on the expression and localization of keratin 10 (KRT10), protects barrier function in RHE.DX314 reduces comedonal number, induces epidermal thickening, and increases comedonal profile, while having no effect on transepidermal water loss (TEWL) in treated rhino mice.

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.

ARD-2585 is an exceptionally potent and orally active PROTAC degrader of androgen receptor.

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.

Ibezapolstat (ACX-362E) is a first-in-class, orally active DNA polymerase IIIC (pol IIIC) inhibitor, with a Ki of 0.325 μM for the DNA pol IIIC from C. difficile. Ibezapolstat is developed for the research of C. difficile infection(CDI).

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

M-110 is a potent, selective inhibitor of PIM kinase family with preference for PIM-3 with IC50 of 0.047, 2.5 and 2.5 uM for PIM3, PIM1 and PIM2, respectively.

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).

CTOP is a potent and highly selective μ-opioid receptor antagonist. CTOP antagonizes the acute morphine-induced analgesic effect and hypermotility. CTOP enhances extracellular dopamine levels in the nucleus accumbens. CTOP dose-dependently enhances locomotor activity.

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.

Parabulin is a novel potent, parasite-specific tubulin inhibitor, inhibits growth of parasites while displaying no effects on human cells.

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.