cns-penetrant — TargetMol Chemicals

Cat No.	Product Name	Synonyms	Targets
T9786	Lu AF27139		P2X Receptor
	Lu AF27139 is an effective and selective antagonist of P2X7 receptor (IC50s of 12 and 2.4 nM for human and rat, Kis of 22, 54, and 13 nM for mouse, human, and rat, respectively). Lu AF27139 can be used in CNS diseases st...		P2X Receptor
T9697	ASK1-IN-1		ASK
	ASK1-IN-1 is an inhibitor of apoptosis signal-regulating kinase 1 which is a key mediator in the apoptotic and inflammatory cellular stress response with an IC50 of 21 nM in biochemica assays.		ASK
T7388	GSK805		ROR
	GSK805 is a potent, orally bioavailable retinoid-related orphan receptor gamma t (RORγt) inverse agonist that interacts with the receptor's putative ligand binding domain without exerting significant effects on DNA bindi...		ROR
T16849	SB-222200		Neurokinin receptor
	SB-222200 is a selective, reversible, and competitive antagonist of the human NK-3 receptor(Ki=4.4 nM).		Neurokinin receptor
T13323	VU6012962		GluR
	VU6012962 is an orally bioavailable negative allosteric modulator of CNS-penetrant metabotropic glutamate receptor 7(mGlu7; IC50: 347 nM).		GluR
T5353	ABX-1431	Elcubragistat	Lipase
	ABX-1431 (Elcubragistat) is a selective and orally available CNS-penetrant monoacylglycerol lipase (MAGL/MGLL) inhibitor (IC50: 14 nM).		Lipase
T14947	CHDI-390576		HDAC
	CHDI-390576 is a CNS penetrant class IIa HDAC inhibitor (IC50s: 54 nM, 60 nM, 31 nM, 50 nM for class IIa HDAC4, HDAC5, HDAC7, HDAC9). It shows >500-fold selectivity over class I HDACs (1, 2, 3) and ~150-fold selectivity ...		HDAC
T28069	ML380	ML 380,ML-380	AChR
	ML380 is a highly potent and the first CNS penetrant M5 positive allosteric modulator (PAM).		AChR
T13321	VU6005649		GluR
	VU6005649 is an agonist of CNS penetrant mGlu7/8 receptor (EC50s: 0.65 μM and 2.6 μM for mGlu7 receptor and mGlu8 receptor, respectively).		GluR
T5494	MW-150	MW01-18-150SRM	p38 MAPK , Autophagy
	MW-150 (MW01-18-150SRM) is a unique protein kinase inhibitor, is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM.		p38 MAPK , Autophagy
T13318	VU0650786		GluR
	VU0650786 is a selective and potent CNS penetrant negative allosteric modulator of metabotropic glutamate receptor subtype 3 (mGlu3 NAM) (IC50: 392 nM), with antidepressant and anxiolytic activity in rodents.		GluR
T15387	GLP-1R Antagonist 1		Glucagon Receptor
	GLP-1R Antagonist 1 is an orally active, CNS penetrant and non-competitive glucagon-like peptide 1 receptor (GLP-1R) antagonist (IC50: 650 nM).		Glucagon Receptor
T23000	ML289	VU0463597,ML 289	GluR
	ML289 (VU0463597) is a potent, selective, and CNS-penetrant negative allosteric modulator of mGlu3 (IC50=0.66 μM), demonstrating over 15-fold selectivity compared to mGlu2 and showing no activity against mGlu5.		GluR
T5956	VP3.15 dihydrobromide		GSK-3 , PDE
	VP3.15 dihydrobromide is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE7- glycogen synthase kinase (GSK)3 inhibitor(with IC50s of 1.59 μM , 0.88 μM,respectively.)		GSK-3 , PDE
T10393	AT-007		Reductase
	AT-007 is an orally active CNS penetrant Aldose Reductase inhibitor for the treatment of Galactosemia (IC50: 100 pM). It reduces toxic galactitol levels and prevents disease complications in GALT deficiency rats.		Reductase
T35028	Valiglurax	VU2957,VU 0652957,VU 2957,VU-0652957,VU0652957,VU-2957	GluR
	Valiglurax (VU2957), also known as VU0652957 and VU2957, is a potent, selective, CNS penetrant, and orally bioavailable mGlu4 PAM. VU2957 possessed attractive in vitro and in vivo pharmacological and DMPK properties acro...		GluR
T61025	GSK-1482160		P2X Receptor
	GSK-1482160 is a CNS-penetrant negative allosteric modulator of P2X7 receptor with oral activity. The P2X7 receptor is involved in the production of pro-inflammatory cytokines by central and peripheral immune cells, so G...		P2X Receptor
T24616	PF-04781340
	PF-04781340 is an effective, selective, and CNS penetrant agonist of 5-HT2C receptor.
T28364	PF-03463275 2HCl	PF3463275,PF 3463275,PF03463275,PF-3463275
	PF-03463275 is an orally available, CNS-penetrant inhibitor of SLC6A9, a GlyT1 glycine transporter.
T28068	ML375	ML 375,ML-375
	ML375 is a potent, selective and CNS penetrant M5 negative allosteric modulator (NAM).