cns penetration — TargetMol Chemicals

Cat No.	Product Name	Synonyms	Targets
T60003	AC1-IN-1		Adenylyl cyclase
	AC1-IN-1 is a selective inhibitor of adenylyl cyclase type 1 (AC1, IC50 = 0.54 µM).		Adenylyl cyclase
T5513	RO-3		P2X Receptor
	RO3 is a selective antagonist of homomeric P2X3 and heteromeric P2X2/3 receptor		P2X Receptor
T6039	TAK-285	TAK285,TAK 285	EGFR , MEK , HER , Aurora Kinase
	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.		EGFR , MEK , HER , Aurora Kinase
T0682	Lamivudine	GR109714X,BCH-189	HIV Protease , Reverse Transcriptase
	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.		HIV Protease , Reverse Transcriptase
T24047	Etilevodopa hydrochloride	Levodopa ethyl ester,Etilevodopa HCl, L-DOPA ethyl ester	Others , Dopamine Receptor , Drug Metabolite
	Etilevodopa hydrochloride (L-DOPA ethyl ester) is a prodrug of levodopa. It also has greater gastric solubility and significant brain penetration.		Others , Dopamine Receptor , Drug Metabolite
T0688	Ganciclovir	BW 759,RS-21592,2'-Nor-2'-deoxyguanosine	Nucleoside Antimetabolite/Analog , Others , Antibiotic , Antifection , HSV
	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 cytomegaloviru...
T22337	Ganciclovir sodium	RS-21592 sodium,Cytovene IV sodium,2'-Nor-2'-deoxyguanosine sodium,BW 759 sodium	Nucleoside Antimetabolite/Analog , Others , Antifection , HSV
	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).
T12679	(Rac)-VU 6008667		Others , AChR
	(Rac)-VU 6008667 is a selective negative allosteric modulator of muscarinic acetylcholine receptor subtype 5 (M5 NAM) with IC50 of 1.8 μM and pIC50 of 5.75, has high CNS penetration.		Others , AChR
T25124	AZ599	AZ-599,AZ 599
	AZ599 is a full agonist of CB1 with good solubility and low CNS penetration.
T28067	ML372	ML 372,ML-372
	ML372 is a potent and selective SMN Modulator (EC50 = 12 nM, 325% increase inSMN2) with good potency, pharmacokinetics, tolerance, and CNS penetration.
T26722	AZD7268	AZD-7268,AZD 7268
	AZD7268 is a potent, selective, reversible, and orally bioavailable agonist of δ-opioid receptor with CNS penetration.
T27474	GSK-345931A	GSK-345931A free acid,GSK 345931A free acid,GSK 345931A
	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.
T17241	Auglurant	VU0424238	Others
	Auglurant is a novel and selective mGlu5 antagonist (IC50: 11 nM (rat) and an IC50: 14 nM (human)). Auglurant has an acceptable CNS penetration.		Others
T29142	VU6001966	VU 6001966,VU-6001966
	VU6001966 is a potent and selective mGlu2 inhibitor (mGlu2 IC50 = 78 nM) and negative allosteric modulator. VU6001966 exhibits excellent central nervous system (CNS) penetration.
T35081	VU0486321	VU 0486321,VU-0486321
	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).
T29151	WAY267464 HCl	WAY267464,WAY-267464,WAY 267,464 dihydrochloride,WAY-267,464 dihydrochloride,WAY 267464 dihydrochloride,WAY 267464
	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 b...
T25819	ML350	SR-2311,SR 2311,SR2311,ML-350,ML 350
	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 ...
T36644	Rezivertinib
	Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI) with potent activity against both common activation EGFR and resistance T790M mutations...
T39343	MW-150 hydrochloride	MW01-18-150SRM hydrochloride,MW-150 hydrochloride
	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. MW-150 hydrochloride (MW01-...
T61210	R-PSOP
	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 syste...