adme

RO6889678 is HBV inhibitor with a complex ADME profile.

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.

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

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.

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

Emavusertib Maleate (also known as CA-4948) is a potent inhibitor of IRAK4 FLT3, demonstrating antitumor activity. In ABC DLBCL and AML cell lines, CA-4948 exhibited strong cellular activity. It showed moderate to high selectivity in a test against 329 kinases and demonstrated good oral bioavailability in ADME and PK profiles, with effective absorption in mice, rats, and dogs. In relevant tumor models, CA-4948 achieved over 90% tumor growth inhibition and showed excellent correlation with in vivo PD modulation.

Emavusertib Tosylate (also known as CA-4948) is a potent inhibitor of IRAK4 FLT3 with demonstrated antitumor activity. In cell lines such as ABC DLBCL and AML, CA-4948 exhibits strong cellular efficacy. Among 329 evaluated kinases, it shows medium to high selectivity. The compound has excellent oral bioavailability and favorable pharmacokinetic properties in ADME and PK profiles. In preclinical models involving mice, rats, and dogs, CA-4948 demonstrated good oral bioavailability and displayed over 90% tumor growth inhibition in relevant tumor models, correlating well with in vivo pharmacodynamic regulation.

Emavusertib Mesylate (also known as CA-4948) is a potent inhibitor of IRAK4 and FLT3, demonstrating antitumor activity. In cell lines of ABC DLBCL and AML, CA-4948 shows significant cellular activity. Moreover, it exhibits moderate to high selectivity in screening assays of 329 kinases and has impressive pharmacokinetic and pharmacodynamic profiles (ADME and PK), with good oral bioavailability in mice, rats, and dogs. In pertinent tumor models, CA-4948 achieves over 90% tumor growth inhibition and shows excellent correlation with in vivo PD modulation.

Emavusertib Phosphate (also known as CA-4948) is a potent inhibitor of IRAK4 and FLT3, exhibiting antitumor activity. In ABC DLBCL and AML cell lines, it demonstrates significant cellular efficacy. Furthermore, CA-4948 shows moderate to high selectivity across a panel of 329 kinases and possesses favorable ADME and PK profiles, including good oral bioavailability in mice, rats, and dogs. It achieves over 90% tumor growth inhibition in relevant tumor models and correlates excellently with in vivo PD modulation.

AHR antagonist 8 (compound SG-02) acts as a regulator of utrophin, a dystrophin analog, and serves as an AhR antagonist with a Kd of 41.68 nM. Studies demonstrate that 800 nM of AHR antagonist 8 can upregulate utrophin by 2.7 times. Additionally, AHR antagonist 8 enhances MyHC expression, indicating its potential to promote myogenesis. ADME evaluations reveal that AHR antagonist 8 possesses some oral bioavailability.

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

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

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

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

PF-06305591 dihydrate is a potent and highly selective voltage-gated sodium channel NaV1.8 blocker (IC50 = 15 nM) with excellent preclinical in vitro ADME and safety profiles [1].

Antitrypanosomal agent 6 (compound 18a) is a potent antitrypanosomal agent demonstrating good ADME properties, with an IC50 of 0.47 μM against Trypanosoma brucei (T. brucei), making it more than twice as active as Nifurtimox; it also exhibits a strong interaction with and selective binding to AT-rich DNA.

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.

BMS-986318 is a potent nonbile acid FXR agonist with EC50 values of 53 nM (FXR Gal4) and 350 nM (SRC-1 recruitment assays). It has a favorable ADME profile and demonstrates effectiveness in mouse models of liver cholestasis and fibrosis caused by bile duct ligation. BMS-986318 is used in research on nonalcoholic steatohepatitis.

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.

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.

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.

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.

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)

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).