cns penetration

Ganciclovir (2'-Nor-2'-deoxyguanosine) is an ACYCLOVIR analog that is a potent inhibitor of the Herpesvirus family including cytomegalovirus. Ganciclovir is used to treat complications from AIDS-associated cytomegalovirus infections.

Lamivudine (BCH-189) is a reverse transcriptase inhibitor and ZALCITABINE analog in which a sulfur atom replaces the 3' carbon of the pentose ring. It is used to treat HIV disease.

Ganciclovir sodium (Cytovene IV sodium) is the sodium salt of Ganciclovir with antiviral activity, especially against cytomegalovirus (CMV) and herpes simplex virus type 1 (HSV-1).

Entrectinib (RXDX-101) is a Trk, ROS1, and ALK inhibitor that inhibits TrkA, TrkB, TrkC, ROS1, and ALK (IC50=1 3 5 12 7 nM) with oral activity and blood-brain-barrier penetration. Entrectinib exhibits both antitumor and CNS activity.

(Rac)-VU 6008667 is a selective negative allosteric modulator of the muscarinic acetylcholine receptor subtype 5 (M5 NAM), with an IC50 of 1.8 μM and a pIC50 of 5.75, exhibiting high CNS penetration.

Etilevodopa hydrochloride (L-DOPA ethyl ester) is a prodrug of levodopa. It also has greater gastric solubility and significant brain penetration.

RO3 is a selective antagonist of homomeric P2X3 and heteromeric P2X2 3 receptor

TAK-285 is a novel dual HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, >10-fold selectivity for HER1 2 than HER4, less potent to MEK1 5, c-Met, Aurora B, Lck, CSK etc. Phase 1.

Auglurant is a novel and selective mGlu5 antagonist (IC50: 11 nM (rat) and an IC50: 14 nM (human)). Auglurant has an acceptable CNS penetration.

A-784168, a potent and orally active inhibitor of vanilloid receptor type 1 (TRPV1), acts on a ligand-gated nonselective cation channel pivotal in integrating pain stimuli including endogenous lipids, capsaicin, heat, and low pH. It demonstrates commendable central nervous system (CNS) penetration upon oral administration [1].

AZ599 is a full agonist of CB1 with good solubility and low CNS penetration.

ML350 (CYM-50202) is a KOR (IC50: 12.6 nM) antagonist with good and moderate selectivity against the DOR and MOR. CYM-50202 displayed high solubility and excellent CNS penetration. CYM-50202 did not display long-lasting pharmacodynamic effects observed wi

AZD7268 is a potent, selective, reversible, and orally bioavailable agonist of δ-opioid receptor with CNS penetration.

GSK-345931A, an EP(1) receptor antagonist, shows measurable CNS penetration in the mouse and rat and potent analgesic efficacy in acute and sub-chronic models of inflammatory pain.

ML372 is a potent and selective SMN Modulator (EC50 = 12 nM, 325% increase inSMN2) with good potency, pharmacokinetics, tolerance, and CNS penetration.

VU6001966 is a potent and selective mGlu2 inhibitor (mGlu2 IC50 = 78 nM) and negative allosteric modulator. VU6001966 exhibits excellent central nervous system (CNS) penetration.

WAY267464 is a nonpeptide small-molecule OT agonists with anxiolytic activity. WAY267464 may be used for modulation of potency, selectivity over the structurally similar vasopressin receptors, CNS penetration, and oral bioavailability.

PF-06767832 is a high quality M1 selective PAM (M1 PAM EC50 = 60 nM; M2-M5 PAM EC50 > 10 microM; CNS MPO = 4.9). PF-06767832 has well aligned physicochemical properties, good brain penetration and pharmacokinetic properties. Extensive safety profiling

VU0486321 is a potent mGlu1 PAM with moderate rat PK (CLp = 13.3. mL/min/kg,t1/2 = 54 min), good free fraction (human fu = 0.05, rat fu =0.03) and excellent CNS penetration (Kp = 1.02).

MW-150 hydrochloride (MW01-18-150SRM hydrochloride) is a potent and selective inhibitor of p38α MAPK with a Ki value of 101 nM. It exhibits excellent CNS penetration and oral bioavailability, and effectively suppresses the phosphorylation of MK2, a substrate of endogenous p38α MAPK, in activated glial cells.

TTBK1-IN-1 (compound 31) is a potent and selective tau microtubule protein kinase 1 (TTBK1) inhibitor (IC50=315 nM) with central nervous system (CNS) penetration that inhibits tau phosphorylation at the disease-associated Ser 422 epitope, and can be used to study Alzheimer's disease.

AC1-IN-1 is a selective inhibitor of adenylyl cyclase type 1 (AC1, IC50 = 0.54 µM).

R-PSOP is a potent and selective nonpeptidic NMUR2 antagonist, exhibiting binding affinity to human and rat NMUR2 with Ki values of 52 nM and 32 nM, respectively. This compound demonstrates moderate central nervous system (CNS) penetration and is valuable in the study of eating disorders, obesity, pain, and stress-related disorders [1].

Rho-Kinase-IN-2 (Compound 23) is an orally active and selective inhibitor of Rho Kinase (ROCK) with CNS penetration, exhibiting a high affinity for ROCK2 with an IC50 of 3 nM. This compound is of potential interest for further investigations in Huntington's disease research [1].