T6147

Nortadalafil (Demethyl Tadalafil) is demethyl Tadalafil, which is a PDE5 inhibitor, treating erectile dysfunction (ED) ; and under the name Adcirca for the treatment of pulmonary arterial hypertensio.

NMDA receptor antagonist 5 (Compound 10e), a potent and non-toxic agent with brain permeability, is significant for studying neurological disorders [1].

Antitubercular agent-13 (Compound 3d) is an antitubercular compound with MIC values of 0.007 μg/mL against MTB H37Rv and 1.851 μg/mL against MDR-MTB 16833, respectively, and exhibits metabolic instability [1].

Tubulin inhibitor 18 (compound 5j) is a highly potent chalcone compound that effectively inhibits tubulin, making it a promising candidate for cancer research [1].

FGFR2-IN-2 is a specific FGFR2 inhibitor that inhibits FGFR1, FGFR2, and FGFR3, and can be used in the study of cancer and cardiovascular disease.

HDAC6-IN-13 (Compound 35m) is a potent and highly selective orally active inhibitor of HDAC6, with an IC50 of 0.019 μM. It also inhibits HDAC1, HDAC2, and HDAC3, with IC50 values of 1.53 μM, 2.06 μM, and 1.03 μM, respectively. HDAC6-IN-13 exhibits substantial blood-brain barrier permeability and anti-inflammatory properties [1].

Ropivacaine mesylate, a long-acting amide local anaesthetic, is used for spinal block and effectively mitigates neuropathic pain. It achieves analgesia by reversibly inhibiting sodium ion influx in nerve fibers, thus blocking impulse conduction. Additionally, Ropivacaine acts as an inhibitor of the K2P (two-pore domain potassium channel) TREK-1, exhibiting an IC50 of 402.7 μM in COS-7 cell membranes.

Thioridazine is a chemical compound characterized by its potent anti-psychotic and anti-anxiety activities. As an antagonist of the dopamine receptor D2 family proteins, it exhibits a strong inhibitory effect on the PI3K-Akt-mTOR signaling pathways, resulting in anti-angiogenic effects. It also demonstrates significant antiproliferative and apoptosis induction effects in a diverse range of cancer cells, specifically targeting cancer stem cells (CSCs) [1] [2] [3] [4].

dCeMM2 is a glue degrader. dCeMM2 prompts an interaction of CDK12-cyclin K with a CRL4B ligase complex, leading to the ubiquitination and degradation of cyclin K.

ROS1-IN-1 (Compound 31) is a highly effective and specific ROS1 kinase inhibitor, with an inhibitory concentration (IC50) of 0.097 μM [1].

LOX-IN-3 dihydrochloride monohydrate (Compound 33) is an orally active lysyl oxidase (LOX) inhibitor, intended for research in fibrosis, cancer, and angiogenesis [1].