Foxy-5 is a novel Wnt-5A mimicking hexapeptide that inhibits breast cancer metastasis in vivo by targeting cell motility.

FRAX1036 is a novel ATP-competitive small molecule inhibitor of group I p21-activated Kinases (PAKs).

Danicopan (ACH-4471, ACH-0144471) is a highly potent, orally active Factor D inhibitor with Kd of 0.54 nM, inhibits the proteolytic activity of purified Factor D against substrate Factor B in complex with C3b, blocking production of Bb fragment IC50 of 15 nM.

FK962 is an enhancer of somatostatin release, exerts cognitive-enhancing actions. Anti-dementia properties.

TH-263 is an inactive analog control for the type III allosteric LIM-kinase (LIMK) inhibitors TH-257, TH-255 and TH-251. LIM kinases belong to the family of cytoplasmic tyrosine-like kinases with dual specificity (serine/threonine and tyrosine). However, known LIMK substrate are usually phosphorylated at serine and threonine residues LIM kinases comprises LIM kinase 1 (LIMK1) and LIM kinase 2 (LIMK2) which show 50% sequence identity in human. Both LIMK1 and LIMK2 present with a unique domain organization containing two N-terminal LIM domains, a PDZ domain, a proline/serine-rich domain and a C-terminal kinase domain.

NTP42 is a thromboxane A2 (TXA2) receptor antagonist with an IC50 of 3.278 nM for antagonizing T prostanoid receptor (TP)- mediated [Ca2+] mobilization following stimulation of cells with the alternative TP agonist U46609. NTP42 can be used for the treatment of pulmonary arterial hypertension (PAH).

GS-4361 is a potent and selective IDO1 inhibitor with an EC50 of 17 nM, GS-4361 was first reported in patent WO2019040102A.

VUN34002, also known as Vanin-1-IN-1 is an inhibitor of vanin-1 enzyme which is a cell surface associated, giycosyiphosphatidyS inositol (GPi) anchored protein and plays an important role in metabolism and inflammation. VUN34002 has CAS#2173134-00-2 without formal code name. According to Hodoodo Chemical Nomenclature, it is named as VUN34002.

A potent, selective, non-RGD-mimetic αIIbβ3 integrin receptor antagonist with IC50 of 45 nM, with no activity on αVβ3 receptors. .

THZ1 is a novel selective and potent covalent CDK7 inhibitor with IC50(binding affinity) of 3.2 nM; inhibits Jurkat cell's proliferation with IC50 of 50 nM.

JA2131 is a selective bioavailable poly(ADP-ribose) glycohydrolase (RARG) inhibitor with IC50 of 0.4 μM.

ζ(ZETA)-Stat (1,3,6-Naphthalenetrisulfonic acid) is a novel PKC-zeta (PKC-ζ) specific inhibitor with IC50 of 5 uM, showed only 13% inhibition on PKC-I at 20 uM.

NI-42 is a potent, selective and orally active BRPF1 bromodomain inhibitor with IC50 of 7.9 nM, with excellent selectivity over nonclass IV BRDs; weakly inhibits BRPF2 (BRD1), BRPF3, BRD9 and BRD4 (BD1) with IC50 of 48, 260, 310 and 4500 nM respectively, and no activity for ATAD2A/2B (IC50>100 uM); shows a modest (GI50=1-10 uM) and selective inhibition of proliferation of certain cancer lines, particularly those lines exhibiting monocytic lineage differentiation; a novel, structurally orthogonal chemical probe for the BRPFs suitable for cellular and in vivo studies.

A potent, orally bioactive 20S proteasome inhibitor with IC50 of 1.3 nM (inhibition of proteasomal chymotrypsin-like proteolytic activity).

A novel anti-TB agent that has an MIC range of 0.06-0.5 ug/mL..

OGG1 inhibitor O8 is a potent, selective inhibitor of 8-oxoguanine DNA glycosylase 1 (OGG1) with IC50 of 0.22 uM, displays no significant activity against other DNA Glycosylases (NEIL1, NTH1, Fpg, IC50>50 uM)..

MYC inhibitor DC-34 is a potent small molecule that selectively inhibits MYC at the transcriptional level only when a G-quadruplex (G4) is present in the promoter, binds to MYC G4 with Kd of 9.4 uM.

Dopamine D2 and 5-HT1A partial agonist in development as a potential treatment for schizophrenia and other psychotic indications; Pharmacoloy profile makes it an atypical antipsychotic and a new approach for the treatment of schizophrenia.

SUVN-911 (compound 9h) is a Novel, Potent, Selective, and Orally Active Neuronal Nicotinic Acetylcholine α4β2 Receptor Antagonist for the Treatment of Depression.Compound 9h is a potent α4β2 receptor ligand with a Ki value of 1.5 nM. It showed >10 μM binding affinity toward the ganglionic α3β4 receptor apart from showing selectivity over 70 other targets. It is orally bioavailable and showed good brain penetration in rats. Marked antidepressant activity and dose-dependent receptor occupancy in rats support its potential therapeutic utility in the treatment of depression. It does not affect the locomotor activity at doses several folds higher than its efficacy dose. It is devoid of cardiovascular and gastrointestinal side effects. Successful long-term safety studies in animals and phase-1 evaluation in healthy humans for safety, tolerability, and pharmacokinetics paved the way for its further development.

A homoisoflavanone found in Caesalpinia sappan, a potent, selective IMPDH2 inhibitor that covalently binds to Cys140 with Kd of 3.944 nM, almost 10 times lower than the Kd of binding to IMPDH1.

R enantiomer of Hydroxychloroquine. Hydroxychloroquine is a potent drug for the COVID-19 trement.

S enantiomer of Hydroxychloroquine. Hydroxychloroquine is a potent drug for the COVID-19 trement.

BKI-1369 is a bumped kinase inhibitor (BKI). BKI-1369 increases human Ether-a-go-go-related gene (hERG)-inhibitory activity with an IC50 of 1.52 μM. BKI-1369 reduces the parasite burden and diseases severity in the gnotobiotic pig model. BKI-1369 has been well characterized for potency, stability, metabolism, toxicity, pharmacokinetics and is potent against C. parvum in infected mice and calves.

NGP555 is a γ-secretase modulator.

Mitochonic acid 5 binds mitochondria and ameliorates renal tubular and cardiac myocyte damage. Mitochonic acid 5 modulates mitochondrial ATP synthesis.

BF 227 is a candidate for an amyloid imaging probe for PET, with a Ki of 4.3 nM for Aβ1-42 fibrils.

BNC105 is a novel tubulin polymerization inhibitor that selectively disrupts tumor vasculature and displays single-agent antitumor efficacy.

SBI-553 is a potent and brain penetrant NTR1 allosteric modulator with EC50 of 0.34μM.

Ibrolipim (NO-1886) is an orally active lipoprotein lipase (LPL)-promoting agent. Ibrolipim decreases plasma triglycerides, increases high-density lipoprotein cholesterol levels. Ibrolipim has renoprotective and hypolipidemic effects.

AUT-1 is a novel specific, cell permeant modulator of Kv3 channels with EC50 of 4.7 and 4.9 uM for Kv3.1b and Kv3.2a, respectively.