|
T12165 |
NAChR agonist 1
|
DUN71755 |
AChR
|
|
nAChR agonist 1 (DUN71755) is a brain-permeable and orally efficacious positive allosteric α7 nicotinic acetylcholine receptor (α7 nAChR)modulator. |
|
T14389 |
AZD 9272
|
|
GluR
|
|
AZD 9272 is a brain-permeable mGluR5 antagonist for the study of gastroesophageal reflux. |
|
TQ0026 |
MDR-1339
|
DWK-1339 |
Beta Amyloid
,
Gamma-secretase
|
|
|
|
T22972 |
Methoxy-X04
|
|
Others
|
|
Methoxy-X04, a derivative of Congo red and Chrysamine-G, is a brain-permeable fluorescent probe for amyloid-β (Aβ). |
|
T9956 |
VK-28
|
|
Mitochondrial Metabolism
,
Lipid
|
|
VK-28 is a brain permeable iron chelator with neuroprotection. VK-28 inhibits basal as well as iron-induced mitochondrial lipid peroxidation. |
|
T1741 |
AZD1080
|
|
GSK-3
|
|
AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor. |
|
T6679 |
SRT 2104
|
SRT2104,sirtuin modulator,GSK2245840 |
Sirtuin
|
|
SRT 2104 (GSK2245840) is a selective and brain-permeable SIRT1 activator. |
|
T5490 |
AK-7
|
|
Sirtuin
|
|
AK-7 is a brain-permeable SIRT2 inhibitor and to characterize its cholesterol-reducing properties in neuronal models with an IC50 of 15.5 μM. |
|
TQ0238 |
Lanabecestat
|
LY3314814,AZD3293 |
BACE
|
|
Lanabecestat (AZD3293) is a highly potent and highly permeable, orally active BACE1 inhibitor (Ki: 0.4 nM) that crosses the blood-brain barrier.Lanabecestat can be used for the study of neurological diseases such as Alzh... |
|
T10355 |
Apyramide
|
|
COX
|
|
Apyramide is an anti-inflammatory agent (NSAID) and behaves as a prodrug of indomethacin. Indomethacin is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2. |
|
T5468 |
YF-2
|
|
Others
,
Epigenetic Reader Domain
,
Histone Acetyltransferase
|
|
YF-2 is blood-brain-barrier permeable histone acetyltransferase activator, acetylates H3 in the hippocampus, CBP, PCAF, and GCN5 with EC50s of 2.75 μM, 29.04 μM and 49.31 μM , respectively |
|
T73177 |
HCAII-IN-9
|
|
Carbonic Anhydrase
|
|
hCAII-IN-9 is a potent carbonic anhydrase inhibitor that inhibits hCA II, hCA IX, and hCA XII with IC50s of 1.18 μM and 0.17 μM , and 2.99 μM , respectively. hCAII-IN-9 is not blood-brain barrier permeable. |
|
T8702 |
SKF-83566
|
|
Dopamine Receptor
,
5-HT Receptor
,
AChR
|
|
SKF-83566 is a blood-brain permeable and orally active antagonist of D1-like dopamine receptor and a weaker competitive 5-HT2 receptor antagonist with Ki of 11 nM |
|
T13298 |
Verubulin hydrochloride
|
MPC-6827 hydrochloride |
Microtubule Associated
|
|
Verubulin hydrochloride (MPC-6827 hydrochloride) is an agent of blood brain barrier permeable microtubule-disrupting, with potent and broad-spectrum cytotoxic activities,with potent anticancer activity in human MX-1 brea... |
|
T72420 |
MTK458
|
EP-0035985 |
PTEN
|
|
MTK458 (EP-0035985) is a brain-permeable and orally active PINK1 activator.MTK458 selectively activates PINK1 by stimulating dimerization and stabilization of the PINK1/TOM complexMTK458 drives the clearance of alpha-syn... |
|
T33514 |
MSC 2032964A
|
MSC-2032964A,MSC2032964A |
ASK
|
|
MSC 2032964A is a potent selective ASK1 inhibitor (IC50 = 93 nM) that is oral bioavailable and brain permeable. It inhibited neuroinflammation in mouse EAE models and blocked LPS-induced phosphorylation of ASK1 and p38 i... |
|
T4494 |
CLOZAPINE N-OXIDE
|
|
Dopamine Receptor
,
5-HT Receptor
,
AChR
,
Drug Metabolite
|
|
Clozapine N-oxide is the major metabolite of Clozapine and is blood-brain barrier permeable. Clozapine N-oxide is an agonist of DREADDs and activates the DREADD receptors hM3Dq and hM4Di. Clozapine N-oxide is also a dopa... |
|
T4019 |
Cambinol
|
SIRT1/2 Inhibitor IV,NSC 112546 |
Apoptosis
,
Phospholipase
,
Sirtuin
|
|
Cambinol (SIRT1/2 Inhibitor IV) is a cell-permeable b-naphthol compound that inhibits the NAD-dependent deacetylase activity of SIRT1/2 (IC50: 56/59 μM, respectively) in a substrate-, but not NAD-, competitive manner. Ca... |
|
T77341 |
GSK-3 inhibitor 4
|
|
GSK-3
,
CDK
|
|
GSK-3 inhibitor 4 is an orally active and brain-permeable triple inhibitor of GSK-3, CDK2 and CDK5 with inhibitory effects on GSK-3β, GSK-3α, CDK2 and CDK5, with IC50 values of 0.56 nM, 0.45 nM, 0.47 μM, 0.68 μM, respect... |
|
T77342 |
GSK-3 inhibitor 3
|
|
GSK-3
,
Microtubule Associated
|
|
GSK-3 inhibitor 3 is a selective, orally active, brain-permeable GSK-3 inhibitor that inhibits GSK-3α and GSK-3β with IC50s of 0.35 nM and 0.25 nM, respectively.GSK-3 inhibitor 3 reduces the phosphorylation level of tau ... |
|
T13001 |
SRT3657
|
|
Sirtuin
|
|
SRT3657 is a brain-permeable SIRT1 activator, has neuroprotective effect. |
|
T14334 |
ASP2535
|
|
GlyT
|
|
ASP2535 is a potent, selective, orally bioavailable, brain permeable and centrally-active glycine transporter-1 (GlyT1) inhibitor.ASP2535 can improve cognitive impairment in animal models of schizophrenia and Alzheimer's... |
|
T15408 |
GNE 5729
|
|
Others
|
|
GNE 5729 is an NMDAR of brain permeable positive allosteric modulator (EC50: 37 nM for GluN2A; 4.7 and 9.5 μM for GluN2C and GluN2D, respectively). |
|
T15407 |
GNE-0723
|
|
Others
|
|
GNE 0723 is an NMDAR brain permeable positive allosteric modulator (EC50: 21 nM for GluN2A; 7.4 and 6.2 μM for GluN2C and GluN2D, respectively). |
|
T10688 |
Casopitant mesylate
|
GW679769B |
P450
,
Neurokinin receptor
|
|
Casopitant mesylate (GW679769B) is a selective, brain permeable, and orally active antagonist of neurokinin 1 (NK1) receptor. It is a second in the class of antiemetics. |
|
T70807 |
Lanabecestat HCl
|
|
|
|
Lanabecestat, also known as AZD3293 and LY3314814, is a potent, highly permeable, orally active, blood-brain barrier (BBB) penetrating, BACE1 inhibitor with unique slow off-rate kinetics. AZD3293 displayed significant do... |
|
T40046 |
UGT8-IN-1
|
UGT8-IN-1 |
|
|
UGT8-IN-1 is a brain-permeable and orally-active inhibitor that specifically targets the ceramide galactosyltransferase enzyme (UGT8). By inhibiting UGT8, this compound has the potential to be employed in research pertai... |
|
TQ0075 |
ML314
|
|
Neurotensin Receptor
|
|
ML314 is a brain-permeable nonpeptide β-inhibin-biased neurotensin NTR1 receptor agonist (EC50: 1.9 μM), a biased neurotensin receptor ligand for methamphetamine abuse that inhibits NTR2 and GPR35. |
|
T61611 |
α-Synuclein inhibitor 4
|
|
|
|
α-Synuclein inhibitor 4 (compound 3gh) is a highly effective and blood-brain barrier-permeable inhibitor of α-Synuclein aggregation. It displays potent activity, with an IC50 value of 0.98 μM, and exhibits a remarkable i... |
|
T41159 |
NCT 501 hydrochloride
|
|
|
|
NCT 501 hydrochloride is a potent and selective ALDH1A1 inhibitor (IC50 = 40 nM). Exhibits >1000-fold selectivity for ALDH1A1 over ALDH3A1, ALDH1B1, ALDH2, HPGD and HSD17β4. Also selective over a panel of 168 GPCRs. Bloo... |
|
T69609 |
TG11-77 free base
|
|
|
|
TG11-77 free base is a novel, Potent, Selective, Water Soluble, Brain-Permeable EP2 Receptor Antagonist. TG11-77 free base has a Schild KB of 9.7 nM on EP2, a water solubility of 2.5 mM, a brain-to-plasma ratio of 0.4, ... |
|
T11185 |
EML741
|
|
Histone Methyltransferase
|
|
EML741 also inhibits DNMT1 (IC50, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barrier penetrated. EML741 is a histone lysine methyltransferase... |
|
T69608 |
TG11-77 HCl
|
|
|
|
TG11-77 HCl is a novel, Potent, Selective, Water Soluble, Brain-Permeable EP2 Receptor Antagonist. TG11-77 HCl has a Schild KB of 9.7 nM on EP2, a water solubility of 2.5 mM, a brain-to-plasma ratio of 0.4, and a plasma... |
|
T35563 |
PF-5274857 hydrochloride
|
|
|
|
PF-5274857 hydrochloride is a potent, orally active, selective, blood-brain barrier permeable Smo antagonist with IC50=5.8 nM and Ki=4.6 nM. It has research potential in a variety of tumors including brain tumors and bra... |
|
T61644 |
α-Synuclein inhibitor 6
|
|
|
|
α-Synuclein inhibitor 6 (compound 3ge) is a highly effective and blood-brain barrier-permeable inhibitor that targets the aggregation of α-Synuclein (α-Syn). It exhibits a potent inhibitory activity, with an IC50 value o... |
|
T62142 |
COX-2-IN-17
|
|
|
|
COX-2-IN-17 is a potent, blood-brain barrier permeable COX-2 (cyclooxygenase-2) inhibitor (IC50: 0.02 μM) with anti-inflammatory and analgesic activity. |
|
T79253 |
HAT-IN-8
|
|
Parasite
|
|
HAT-IN-8 (Compound 38), a blood-brain barrier-permeable inhibitor of Trypanosoma brucei with an EC50 of 0.18 μM, is utilized in the study of Human African trypanosomiasis [1]. |
|
T78969 |
PB131
|
|
HDAC
|
|
PB131, a selective and brain-permeable HDAC6 inhibitor, exhibits high binding affinity (IC50: 1.8 nM) and potent anti-inflammatory activity, making it suitable for inflammation research, particularly in neuroinflammation... |
|
T41143 |
PCPA methyl ester hydrochloride
|
4-Chloro-DL-phenylalanine methyl ester hydrochloride |
5-HT Receptor
,
Hydroxylase
|
|
pCPA methyl ester hydrochloride (4-Chloro-DL-phenylalanine methyl ester hydrochloride) is an inhibitor of tryptophan hydroxylase inhibitor and 5-HT synthesis. pCPA methyl ester hydrochloride is permeable across the blood... |
|
T62202 |
MGluR2 modulator 1
|
|
|
|
mGluR2 modulator 1 (compound 95) is a potent, blood-brain-barrier permeable modulator of mGluR2 (metabotropic glutamate receptor-2) positive transmutation (EC50: 0.03 μM). mGluR2 modulator 1 can be used in the study of p... |
|
T62898 |
Glucosylceramide synthase-IN-1
|
|
|
|
Glucosylceramide synthase-IN-1 (T-036) is a potent, orally active, blood-brain barrier permeable glucosylceramide synthase (GCS) inhibitor that acts on human GCS (IC50: 31 nM) and mouse GCS (IC50: 51 nM). Glucosylceramid... |
|
T69632 |
VRT-043198
|
|
|
|
VRT-043198, the drug metabolite of VX-765 (Belnacasan), is a potent, selective, and blood-brain barrier permeable inhibitor of the interleukin-converting enzyme/caspase-1 subfamily caspases, displaying Ki values of 0.8 n... |
|
T37577 |
Glycogen Phosphorylase Inhibitor
|
|
|
|
Glycogen phosphorylase in the liver, muscle, and brain initiate glycogenolysis by releasing glucose-1-phosphate from glycogen. Glycogen phosphorylase inhibitor is a cell-permeable acyl urea first identified as an inhibit... |
|
T83469 |
10m/ZS44
|
|
|
|
10m/ZS44, a blood-brain barrier-permeable Glioblastoma (GBM) inhibitor, significantly suppresses tumor growth in mouse xenograft models and induces apoptosis through activation of the SIRT1/p53-mediated pathway, thereby ... |
|
T74781 |
UT-11
|
|
|
|
UT-11 is a potent brain-permeable inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1), exhibiting IC50 values of 0.10 μM and 2.00 μM for the inhibition of PGE2 production in human (SK-N-AS) and murine (BV2) cell... |
|
T62578 |
BuChE-IN-1
|
|
|
|
BuChE-IN-1 (Compound 23) is a potent, highly blood-brain barrier-permeable, low cytotoxicity inhibitor of butyrylcholinesterase (BuChE). BuChE-IN-1 is a BuChE inhibitor that has the potential to be used in the study of A... |
|
T78603 |
Sotuletinib dihydrochloride
|
BLZ945 dihydrochloride |
c-Fms
|
|
Sotuletinib (BLZ945) dihydrochloride is an orally administered, blood-brain barrier-permeable inhibitor specifically targeting CSF1-R with an IC50 of 1 nM. It promotes apoptosis in tumor cells and significantly restricts... |
|
T62674 |
LSD1-IN-21
|
|
|
|
LSD1-IN-21 is a potent, blood-brain barrier permeable LSD1 (lysine specific demethylase-1) inhibitor (IC50: 0.956 μM).LSD1-IN-21 significantly reduces the pro-inflammatory cytokine TNF-α and exhibits good anti-cancer and... |
|
T62062 |
MAO-B-IN-7
|
|
|
|
MAO-B-IN-7 is a potent and blood-brain barrier permeable MAO-B and AChE inhibitor. MAO-B-IN-7 exhibits IC50 s of 41 nM, 87 nM and 0.3 μM for human AChE, electric eel AChE and MAO-B, respectively. MAO-B-IN-7 effectively a... |
|
T62664 |
Glucosylceramide synthase-IN-2
|
|
|
|
Glucosylceramide synthase-IN-2 (compound T-690) is a potent, blood-brain barrier-permeable, orally active inhibitor of glucosylceramide synthase (GCS) that acts on human GCS (IC50: 15 nM) and mouse GCS (IC50: 190 nM). Gl... |
