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).

Tirilazad mesylate (U 74006F) is a non-glucocorticoid, lipid peroxidation inhibitor with antiviral and neuroprotective activities. It confines intracellular intramembranous foci, attenuates spinal cord injuries induced by trauma, stroke, and ischemia/reperfusion injuries, inhibits toxins in dogs, and is used in the study of neurological disorders.

LY2140023 has the potential for schizophrenia.LY2140023 is an orally active prodrug of LY404039. LY404039 is a selective metabotropic glutamate 2/3 receptor agonist.

Pomaglumetad methionil is an oral methionine prodrug of the potent specific agonist of mGlu2/3 receptor LY404039.

Alphamethadol is a synthetic opioid analgesic.

MTDIA (MT-DADMe-ImmA and methylthio-DADMe-Immucillin A) is an MTAP inhibitor.

Pomaglumetad methionine hydrochloride (LY2140023 hydrochloride) is a methionine prodrug of LY404039 with oral activity. LY404039 is a selective mGlu2/3 receptor agonist. Pomaglumetad methionil hydrochloride (LY2140023 hydrochloride) has research value in schizophrenia.

Tirilazad mesylate hydrate is the hydrated form of Tirilazad mesylate, a nonglucocorticoid, 21-aminosteroid known for inhibiting lipid peroxidation. It is used to mitigate brain or spinal cord injury resulting from trauma, stroke, ischemia, and reperfusion injury and exhibits antiviral activities against nCoV. Additionally, Tirilazad mesylate is noted for its neuroprotective properties in ischemic stroke and is utilized in subarachnoid hemorrhage research [1] [2] [3].

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.

NEDD4-IN-1 (Compound 32) is a potent inhibitor of NEDD4, with an IC50 of 0.12 μM. It demonstrates significant antiproliferative activity in the H292 cell line and exhibits high plasma protein binding and moderate to high in vitro clearance in both human and mouse models. The compound shows exceptional stability in mouse plasma, alongside excellent efficacy, selectivity, and favorable in vitro ADME properties. In mouse models, its systemic plasma clearance surpasses hepatic blood flow. NEDD4-IN-1 is applicable for anticancer research.

ARN25657 is a dual regulator of D3R/GSK-3β. It demonstrates partial agonist activity at the D3 receptor (EC50 = 15.2 nM, Ki = 1.5 nM) alongside potent inhibitor activity against GSK-3β (IC50 = 19.3 nM). ARN25657 shows excellent GSK-3β selectivity over FYN, PKA, and CDK5/p35. It inhibits P-gp-mediated efflux of acetoxymethyl calcein, enhancing in vitro ADME properties while maintaining balanced dual-target distribution. ARN25657 is applicable in the study of bipolar disorder and related neuropsychiatric conditions.

hCA-IN-1 (Compound 5u) is an hCA inhibitor with Ki values of 159.2 nM for hCA I, 4.8 nM for hCA II, 15.5 nM for CAIX, and 2 nM for CAXII. It demonstrates broad-spectrum anticancer activity against melanoma, breast cancer, and colon cancer cells. ADME predictions indicate that hCA-IN-1 has good solubility and oral bioavailability. This compound is useful in tumor research.

Y1693 is an orally active RANKL inhibitor with a Kd value of 5.03 μM for hRANKL. Y1693 inhibits activation of the downstream c-fos/NFATc1 signaling pathway by blocking the interaction between RANKL and RANK. Y1693 significantly inhibits RANKL-induced osteoclast differentiation, F-actin ring formation, and bone resorptive activity while downregulating the mRNA and protein expression levels of TRAP, cathepsin K, c-fos, and NFATc1. Y1693 demonstrates no obvious cytotoxicity toward bone marrow-derived macrophages and osteoclast precursor cells and exhibits favorable ADME properties. Y1693 improves ovariectomy-induced osteoporosis in mice and reverses ligation-induced periodontal alveolar bone loss. Y1693 is applicable to research involving osteoporosis, osteoclast biology, and periodontal disease-associated bone remodeling mechanisms.

OUL312 is a potent PARP10 inhibitor with an IC50 of 20 nM, demonstrating 75-fold greater selectivity for PARP10 over PARP15 (IC50= 1500 nM). It exhibits activity at least 18 times higher than all other human enzymes in the same family. OUL312 has favorable ADME properties, is cell-permeable, non-toxic, and effectively inhibits PARP10-induced apoptosis in human cells at submicromolar concentrations. OUL312 is applicable for research in cervical cancer.

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.