GRP-60367 is a first-in-class direct-acting RABV inhibitor with EC50 from 2 to 52 nM (different host cell lines) that blocks RABV G protein-mediated viral entry.

Tegoprazan, a potassium-competitive acid blocker, is a potent, oral active and highly selective inhibitor of gastric H+/K+-ATPase that could control gastric acid secretion and motility, with IC50 values ranging from 0.29-0.52 μM for porcine, canine, and human H+/K+-ATPases in vitro.

BIA 10-2474 is an inhibitor of fatty acid amide hydrolase (FAAH) with IC50 values of 50 to 70mg/kg in various rat brain regions.

DT2216 is a selective B-cell lymphoma extra large (BCL-XL) proteolysis-targeting chimera (PROTAC). DT2216 targets BCL-XL to the Von Hippel-Lindau (VHL) E3 ligase for degradation. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells but considerably less toxic to platelets.

JC-1 is a membrane-permeable cationic dye that is used to study mitochondrial integrity in the context of cellular apoptosis.

YUN27078, also known as EGFR inhibitor, is an EGFR inhibitor. It directly depolymerizes microtubules and is used as a chemical probe to investigate both the EGFR pathway and microtubule dynamics. YUN27078 hax CAS#879127-07-8, no formal name For the convenience of scientific communication, we named it as YUN27078 (combined from Inchi key plus CAS#) according to Hodoodo Chemical Nomenclature

Homo-PROTAC cereblon degrader 1, is a cereblon degrader.

Fmoc-Val-Ala-PAB-OH is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

DCC-2036 is a conformational control Bcr-Abl inhibitor for Abl1(WT) and Abl1(T315I) with IC50 of 0.8 nM and 4 nM, also inhibits SRC, LYN, FGR, HCK, KDR, FLT3, and Tie-2, and low activity to seen towards c-Kit. Phase 1/2.

MW-150 is a novel potent, selective, CNS penetrant and orally active inhibitor of p38α MAPK with Ki of 101 nM

Capsazepine is a synthetic analogue of the sensory neurone excitotoxin, capsaicin; potent TRPV1 receptor antagonist with IC50 of 562 nM.

(Rac)-Benpyrine, a racemate of Benpyrine, is a potent and orally active TNF-α inhibitor. (Rac)-Benpyrine has the potential for TNF-α mediated inflammatory and autoimmune disease research.

DIMBOA, an antibiotic, is a benzoxazinoid, part of the chemical defense system of graminaceous plants such as maize, wheat, and rye. DIMBOA possess growth inhibitory properties against many strains of studied bacteria and fungi, such as Staphylococcus aureus, Escherichia coli as well as against Saccharomyces cerevisiae. DIMBOA exhibits a potent free-radical scavenging activity and a weaker iron (III) ions reducing activity. Antioxidant activity.

Glabrescione B (GlaB) is a small molecule binding to Gli1 zinc finger and impairing Gli1 activity by interfering with Gli1/DNA interaction, inhibits Hh signaling by impairing Gli1 function; inhibits the growth of Hedgehog-dependent tumor cells in vitro and in vivo, inhibits Gli1-dependent growth of cerebellum-derived normal progenitors; inhibits the growth of Gli-dependent medulloblastoma and tumor-derived stem-like cells; inhibits the growth of Gli-dependent basal cell carcinoma in vitro and in vivo.

Zamicastat (BIA 5-1058) is a dopamine β-hydroxylase (DBH) inhibitor and can cross the blood-brain barrier (BBB) to cause central as well as peripheral effects. Zamicastat is also a concentration-dependent dual P-gp and BCRP inhibitor with IC50 values of 7

GSK2334470 is a novel PDK1 inhibitor with IC50 of ~10 nM, with no activity at other close related AGC-kinases.

VU 0365114 is a mAChR M5 positive allosteric modulator, with an EC50 of 2.7 μM.

TP0586532 is a non-hydroxamate LpxC inhibitor (IC50=0.101 μM). TP0586532 as a compound with a low cardiovascular risk that is effective against K. pneumoniae, including resistant strains.

RC-3095 is a gastrin-releasing peptide receptor antagonist, synergizes with gemcitabine to inhibit the growth of human pancreatic cancer CFPAC-1 in vitro and in vivo. RC-3095 inhibit the growth of human glioblastomas in vitro and in vivo. RC3095 inhibits tumor growth and decrease the levels and mRNA expression of epidermal growth factor receptors in H-69 small cell lung carcinoma.R,BRS-1) antagonist.

GW1929 is a synthetic peroxisome proliferator-activated receptor-γ (PPARγ) agonist with IC50 of 6.2 nM and 13 nM for human and mouse, respectively.

USP25 and 28 inhibitor AZ-1 (AZ1) is a potent, selective, dual USP25/28 inhibitor with IC50 of 0.7/0.6 uM, respectively; shows a high degree of selectivity over other deubiquitinases (USP4,7 etc.); demonstrates target engagement against both USP25 and USP28 in cells, elicits modulation of both the total levels and the half-life of the c-Myc oncoprotein in cells, and also induces apoptosis and inhibits cell viability in a range of cancer cell lines.

MRL-871 (MRL871) is a potent, selective inhibitor of RORγt via allosteric inverse agonism, inhibits coactivator binding with IC50 of 7 nM; significantly reduces the IL17a mRNA levels in EL4 murine lymphoblast cell line at 10 uM.

PF-03715455 is a potent inhaled p38 MAPK inhibitor. PF-03715455 shows some selectivity for p38α over p38β with respective IC50 values of 0.88 and 23 nM. PF-03715455 potently inhibits LPS-induced TNFα production in human whole blood (IC50=1.7 nM). PF-03715455 has potential for the treatment of COPD (chronic obstructive pulmonary disease)[1][2].PF-03715455 is a moderate inhibitor of CYP1A2, CYP2C19, and CYP2D6 and a potent inhibitor of CYP’s 2C9 and CYP3A4[2].PF-03715455 treatment shows that the Vss and T1/2 are 0.19 L/kg, 1 hour, respectively[2]. Animal Model: Male CD Sprague Dawley rats (300-450 g)[2] Dosage: 1 mg/kg Administration: I.v. (Pharmacokinetic Analysis) Result: The Vss, and T1/2 were 0.19 L/kg, 1 hour, respectively.

CDN1163 (CDN-1163) is a small molecule, allosteric activator of SERCA2, dose-dependently increases the Vmax of SERCA2 Ca2+-ATPase activity in ER microsomes; increases Ca2+-ATPase activity and significantly enhances Ca2+ uptake into the ER, attenuates H2O2-stimulated cell death in HEK cells; improves glucose homeostasis and metabolic parameters, increases glucose tolerance in ob/ob mice; CDN1163 reduces lipid accumulation and decreases lipogenesis in obese mice livers.

AX20017 is a small-molecule protein kinase G (PknG) inhibitor with an IC50 of 0.39 μM.

Ciliobrevin D is a cell-permeable, reversible, specific inhibitor of cytoplasmic dynein, blocks dynein-dependent microtubule gliding and ATPase activity while sparing kinesin dependent cellular trafficking.

BAM15 is a potent and selective mitochondrial uncoupler or protonophore. Chemical mitochondrial uncouplers are lipophilic weak acids that transport protons into the mitochondrial matrix via a pathway that is independent of ATP synthase, thereby uncoupling nutrient oxidation from ATP production. These uncouplers have potential for the treatment of diseases such as obesity, Parkinson’s disease, and aging.

UC-1728 is a potent rabbit soluble epoxide hydrolase (sEH) inhibitor, with an IC50 of 2 nM on rabbit liver.

Azilsartan medoxomil is an angiotensin II receptor antagonist indicated for the treatment of mild to moderate essential hypertension.

AZD-0156 is an orally bioavailable ataxia telangiectasia mutated (ATM) kinase inhibitor, with potential chemo-/radio-sensitizing and antineoplastic activities.