ODM-203 (ODM203) is a potent, selective, dual inhibitor of FGFR and VEGFR tyrosine kinases with approximately equal potency towards recombinant FGFR1, 2, 3 and 4, as well as VEGFR1, 2 and 3 (IC50=5-35 nM).

Deferasirox (Exjade)

Elagolix is a Gonadotropin-Releasing Hormone (GnRH) Antagonist.

Balixafortide(POL 6326) is a novel potent, selective, peptidic CXCR4 antagonist that interferes with the tumor-protective microenvironment and sensitizes tumor cells to chemotherapy.

CP-31398 is a small molecule p53 reactivator that protects p53 from thermal denaturation, not only reactivates mutant p53 but also induces stabilization of wild type p53.

PF-3450074 (PF74) is a small molecule HIV capsid protein, destabilized the viral capsid in vitro.

SNAP-94847 is a selective, high-affinity, and competitive MCH1 receptor (MCH1-R) antagonist with Ki of 1.69 nM.

PWT143 (ME-401), is an orally bioavailable inhibitor of the delta isoform of phosphatidylinositide 3-kinase (PI3K), with potential antineoplastic activity.

GDC-0623 is a potent, ATP-uncompetitive inhibitors of MEK1(Ki=0.13 nM, +ATP).

>98%,Standard References

A potent and selective antagonist of CXCR4 with IC50 of 13 nM in a CXCR4 125I-SDF inhibition binding assay.

NAB-14 is a potent, selective negative allosteric modulator of GluN2C/2D-containing NMDA receptors with IC50 of 580 nM, >800-fold selective over GluN2A/GluN2 receptors; inhibits triheteromeric (GluN1/GluN2A/GluN2C) NMDARs with modestly reduced potency and efficacy compared to diheteromeric (GluN1/GluN2C/GluN2C) receptors; inhibits GluN2D-mediated synaptic currents in rat subthalamic neurons and mouse hippocampal interneurons, but has no effect on synaptic transmission in hippocampal pyramidal neurons.

PF-915275 is a potent and selective inhibitor of human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) (Ki ＜ 1 nM) with good preclinical pharmacokinetic properties.IC50 value: ＜ 1 nM (Ki)[2]Target: 11βHSD1in vitro: PF-915275 maintains potency in our cellular assay against human 11βHSD1 (HEK293, EC50 = 5 nM) and is selective against human 11βHSD2 (HEK293, 1.5% inhibition 10 μM). PF-915275 displays only weak affinity for the rodent choline transporter (Ki = 9.6 μM) and the hamster melatonin MT3 receptor (Ki = 9.6 μM) in the Cerep Bioprint screening panel. PF-915275 has good in vitro pharmacokinetic properties. In particular, PF-915275 is categorized as a low clearance compound (liver microsome assays) with high permeability (Caco2 assay). [2]in vivo: As a prelude to in vivo studies with PF-915275, the rat pharmacokinetic properties of this compound were determined. PF-915275 has an excellent pharmacokinetic profile characterized by low clearance, long half-life and good oral bioavailability. [2]

Delafloxacin meglumine (ABT492 meglumine; RX-3341 meglumine; WQ-3034 meglumine) is a broad-spectrum fluoroquinolone antibiotic. Delafloxacin has a broad spectrum of activity that includes drug-resistant Staphylococcus aureus, Streptococcus pneumoniae, and

A potent, noncovalent SARS-CoV papain-like protease (PLpro) inhibitor with IC50 of 2.6 uM.

Pyronaridine tetraphosphate is a Mannich base anti-malarial with demonstrated efficacy against drug resistant Plasmodium falciparum, P. vivax, P. ovale and P. malariae.

CCG-50014 is the most potent against the regulator of G-protein signaling protein type 4 (RGS4) (IC50 =30 nM) and is >20-fold selective for RGS4 over other RGS proteins. CCG-50014 binds covalently to the RGS, forming an adduct on two cysteine residues located in an allosteric regulatory site. CCG50014, reduces nociceptive responses and enhances opioid-mediated analgesic effects in the mouse formalin test.

A potent, specific survivin inhibitor that inhibits survivin promoter activity with IC50 of 0.54 nM.

Lefamulin is a semi-synthetic compound that inhibits the synthesis of bacterial protein, which is required for bacteria to grow.

Clevudine (Levovir) is an antiviral drug for the treatment of hepatitis B,showed potent activity against COVID-19(SARS-COV-2) .

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

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

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

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.

MS4078 is a novel PROTAC (degrader) of ALK, potently decreases cellular levels of oncogenic active ALK fusion proteins in a concentration- and time-dependent manner in SU-DHL-1 lymphoma and NCI-H2228 lung cancer cells (DC50=11 nM).

JQ-35, (S)- is an inhibitor of the Bromodomain and Extra-Terminal (BET) family bromodomain-containing proteins with potential antineoplastic activity.

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

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.