adme

ZN-c3 is a potent and selective Wee1 inhibitor with balanced potency, ADME, and pharmacokinetic properties.

RO6889678 is HBV inhibitor with a complex ADME profile.

MK-8325 is a potent and orally available HCV NS5A inhibitor with replicative activity against a wide range of genotypes.MK-8325 has demonstrated bioavailability in in vitro and in vivo assays and has a favorable overall ADME profile.

MT-DADMe-ImmA (MTDIA) is an inhibitor of human 5'-methylthioadenosine phosphorylase (MTAP, Ki: 90 pM).

ML355, a specific, effective 12-Lipoxygenase(12-LOX) inhibitors(IC50=0.34 μM), possess favorable ADME properties.

BIIB068 is an selective, reversible and orally active BTK inhibitor (IC50 = 1 nM, Kd = 0.3 nM). BIIB068 is 400 times more selective for BTK than other kinases.

Poly(acrylic acid) serves as an effective corrosion inhibitor for pure cast aluminium in acidic environments through its adsorption onto the metal's surface. Additionally, this compound functions as an excipient within the pharmaceutical industry, utilized in roles such as a coating material and release blocker. Pharmaceutical excipients, also known as pharmaceutical auxiliaries, are chemical substances employed in drug formulation alongside the active pharmaceutical ingredients to enhance the stability, solubility, and manufacturability of the products. These excipients also influence the absorption, distribution, metabolism, and elimination (ADME) processes of drugs [1] [2].

MAGL-IN-10, a reversible monoacylglycerol lipase (MAGL) inhibitor, exhibits favorable ADME properties and low in vivo toxicity. It is applicable in the study of cancer, neurological disorders, and inflammatory pathologies [1].

GR-125487 is a 5-HT4R partial agonist. It also has favorable ADME properties and good in vivo efficacy.

Maltodextrin (dextrose equivalent 16.5-19.5) serves as an excipient in pharmaceutical applications. Excipients, also known as pharmaceutical auxiliaries, are chemical substances utilized in drug formulation alongside active pharmaceutical ingredients. They primarily enhance the stability, solubility, and processability of drug preparations, while also influencing the absorption, distribution, metabolism, and elimination (ADME) of co-administered drugs [1].

XEN445, a potent and selective endothelial lipase(EL) inhibitor (IC50=0.237 uM), exhibitis good ADME and PK properties.

ARRY-403, also known as AMG-151, is an orally available allosteric glucokinase (GK) activator developed for the treatment of type 2 diabetes mellitus (T2DM). ARRY-403 has many favorable physicochemical characteristics and ADME properties (low potential to cause drug–drug interactions (DDIs). ARRY-403 potently activates human glucokinase (GK) in vitro (EC50 = 79 nM at 5 mM glucose), with an S0.5 = 0.93 mM glucose (ARRY-403 at 5 mM) and Vmax = 134% compared to the no activator control. It possesses good in vitro drug-like properties (aqueous solubility, cell permeability, low low potential for drug-drug interactions, low predicted hepatic clearance), and selectivity against broad panels of receptors and enzymes.

Antitrypanosomal Agent 15 (Compound 26) is an orally active, brain-penetrant, selective inhibitor of the Trypanosoma cruzi proteasome, exhibiting a pIC50 of 7.4 for T. cruzi and <4 for the human proteasome. It possesses favorable ADME properties, rendering it useful for the study of Chagas disease [1].

IRAK4-IN-25 (compound 38), a potent oral IRAK4 inhibitor (IC50 = 7.3 nM) with low clearance (Cl = 12 mL/min/kg), effectively suppresses pro-inflammatory cytokine production and demonstrates favorable in vitro safety and ADME profiles. It is suitable for research on inflammatory and autoimmune disorders [1].

Polyoxyethylene Sorbitan Monostearate, an ester derived from the saturated fatty acid stearic acid (C18:0), serves multiple roles in pharmaceutical formulations, including as a surfactant, emulsifier, solubilizer, and wetting agent. As a pharmaceutical excipient—an inert substance that enhances the stability, solubility, and processability of drug formulations—it plays a crucial role in affecting the absorption, distribution, metabolism, and elimination (ADME) processes of drugs [1] [2].

BMS-986318 is a potent nonbile acid FXR agonist, displaying EC50 values of 53 nM and 350 nM in FXR Gal4 and SRC-1 recruitment assays, respectively. It exhibits a favorable ADME profile and shows effectiveness in mouse models of liver cholestasis and fibrosis caused by bile duct ligation. BMS-986318 is employed in research focusing on nonalcoholic steatohepatitis.

PF-06455943, a leucine rich repeat kinase 2 (LRRK2) inhibitor, exhibits an inhibition concentration (IC50) value of 3 nM and also functions as a PET radioligand. It is utilized in the research of ADME/neuro PK characterization and Parkinson's disease (PD).

GNE-3500 is a Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C (RORc or RORγ) Inverse Agonist. Retinoic acid receptor-related orphan receptor C (RORc, RORγ, or NR1F3) is a nuclear receptor that plays a major role in the production of interleukin (IL)-17. Considerable efforts have been directed toward the discovery of selective RORc inverse agonists as potential treatments of inflammatory diseases such as psoriasis and rheumatoid arthritis. GNE-3500 possessed favorable RORc cellular potency with 75-fold selectivity for RORc over other ROR family members and >200-fold selectivity over 25 additional nuclear receptors in a cell assay panel. The favorable potency, selectivity, in vitro ADME properties, in vivo PK, and dose-dependent inhibition of IL-17 in a PK/PD model support the evaluation of GNE3500 in preclinical studies (J. Med. Chem., 2015, 58 (13), pp 5308–5322)

LY3325656 is a GPR142 agonist suitable for clinical testing in human. LY3325656 demonstrated anti-diabetic benefits in pre-clinical studies and ADME/PK properties suitable for human dosing. LY3325656 is the first GPR142 agonist molecule advancing to phase 1 clinic trials for the treatment of Type 2 diabetes.

PF-06380101 is an auristatin microtubule inhibitor and is a cytotoxic Dolastatin 10 analogue. When compared to other synthetic auristatin analogues that are used in the preparation of ADCs, PF-06380101 displays excellent potencies in tumor cell proliferat

GSK1842799 is a selective S1P1 receptor agonist for multiple sclerosis. Upon phosphorylation, GSK1842799 showed subnanomole S1P1 agonist activity with >1000× selectivity over S1P3. GSK1842799 demonstrated good oral bioavailability. On the basis of the favorable in vitro ADME and in vivo PK/PD properties as well as broad toxicology evaluations, GSK1842799 was selected as a candidate for further clinical.

PF-06305591 dihydrate is a potent and highly selective voltage gated sodium channel NaV1.8 blocker (IC 50 = 15 nM) with an excellent preclinical in vitro ADME and safety profile [1].

Antitrypanosomal agent 6 (compound 18a) is a potent antitrypanosomal agent showing good ADME properties. Antitrypanosomal agent 6 is more than twice as active as Nifurtimox against Trypanosoma brucei (T. brucei) with an IC50 of 0.47 μM. Antitrypanosomal agent 6 has a strong interaction with DNA and selectively binds AT-rich DNA.

PF-05139962 is a novel potent mTOR inhibitor with excellent mTOR biochemical inhibition, cellular potency, kinase selectivity and in vitro ADME properties. PF-05139962 has pS473 and pS6 cellular IC50 = 48 and 6 nM respectively. PF-05139962 has great selectivity against other receptors and kinases. No genotoxicity was observed on this compound and no more than 25% inhibiton was observed for major CYP enzymes (3A4, 1A2, 2C9, 2D6) at 3 uM. This compound has LE = 0.35 and LipE up to 6.8 which is in a very desirable range for a kinase inhibitor.

The Antitrypanosomal agent 7 (compound 18c) is a potent anti-trypanosome agent and shows good ADME properties. The Antitrypanosomal agent 7 was more than two-fold more active against T. brucei (IC50: 0.71 μM) than Nifurtimox. Antitrypanosomal agent 7 has a strong interaction with DNA and can selectively bind to AT-rich DNA.

Trisodium phosphate dodecahydrate serves as a corrosion inhibitor for iron in 0.1 M NaClO4 solutions, effective under both aerated and deaerated conditions. Additionally, it acts as an excipient in pharmaceutical formulations, functioning primarily as a pH regulator and buffer. These excipients, also known as pharmaceutical auxiliaries, are substances utilized in the pharmaceutical manufacturing process besides the active pharmaceutical ingredients. They are crucial for enhancing the stability, solubility, and processability of pharmaceutical products. Moreover, pharmaceutical excipients play a significant role in influencing the absorption, distribution, metabolism, and elimination (ADME) of co-administered drugs, thereby affecting their efficacy and safety [1] [2].

Cellulose can be used as an excipient. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs [1] .

GNE-9822 is a potent selective ITK inhibitor that shows favorable ADME properties in preclinical species.