|
T15275 |
Fenobam
|
|
GluR
|
|
Fenobam shows inverse agonist activity which blocks the mGlu5 receptor basal activity(IC50: 84 nM). Fenobam has anxiolytic activity. Fenobam is a selective and non-competitive mGluR5 antagonist acting at an allosteric mo... |
|
T9346 |
CVN424
|
|
GPR
|
|
CVN424 is a selective and novel GPR6 Inverse agonist effective in models of Parkinson Disease. |
|
T9466 |
RTICBM-189
|
|
Others
|
|
RTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB1) receptor with a pIC50 of 7.54 in Ca2+ mobilization assay. RTICBM-189 has pIC50s of 5.29 and 6.25 for hCB1 and mCB1, respectivel... |
|
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. |
|
T4081 |
MPTP hydrochloride
|
MPTP-hydrochloride |
Apoptosis
,
Dopamine Receptor
|
|
MPTP hydrochloride is a precursor of MPP+, a dopamine neurotoxin with blood-brain barrier permeability. MPTP hydrochloride is toxic to dopaminergic neurons, which can lead to Parkinson's disease, and is widely used in th... |
|
T9452 |
PW0787
|
|
GPR
|
|
PW0787 is a potent, selective, orally active, and brain-penetrant GPR52 agonist (EC50=135 nM). |
|
T12998 |
SR10067
|
|
Others
,
Autophagy
|
|
SR10067 is a potent, selective and brain penetrant agonist of Rev-Erbα/β(IC50 of 160 and 170 nM for Rev-Erbβ and Rev-Erbα, respectively),has anxiolytic activity. |
|
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... |
|
T21747 |
VU0483605
|
|
GluR
|
|
VU0483605 is an effective and selective positive allosteric modulator of mGluR1 with EC50s of 390 and 356 nM for human and rat, respectively. |
|
T16849 |
SB-222200
|
|
Neurokinin receptor
|
|
SB-222200 is a selective, reversible, and competitive antagonist of the human NK-3 receptor(Ki=4.4 nM). |
|
T8554 |
KCC-07
|
|
DNA Alkylator/Crosslinker
|
|
KCC-07 is a selective, potent and brain-penetrant inhibitor of methyl-CpG-binding domain protein 2(MBD2) with anticancer activity. KCC-07 prevents binding of MBD2 to methylated DNA and activates brain specific angiogenes... |
|
T3707 |
GNE-3511
|
GNE3511 |
DNA Alkylation
,
MAPK
|
|
GNE-3511 is a potent and selective dual leucine zipper kinase inhibitors. |
|
T7100 |
PLX5622
|
PLX-5622 |
c-Fms
,
CSF-1R
|
|
PLX5622 is a highly selective brain penetrant and oral active CSF1R inhibitor. |
|
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... |
|
T6031 |
GNE0877
|
GNE 0877,GNE-0877 |
LRRK2
|
|
GNE0877 (GNE 0877) is a highly effective and specific leucine-rich repeat kinase 2 (LRRK2) inhibitor (Ki: 0.7 nM). |
|
T27620 |
IP7e
|
IP 7e,IP-7e,isoxazolo-pyridinone 7e |
Others
|
|
IP7e (isoxazolo-pyridinone 7e) is a Nurr1 activator with an EC50 value of 3.9 nM. |
|
T21793 |
CGP 35348
|
|
GABA Receptor
|
|
CGP 35348 is a selective antagonist of GABAB receptor (EC50 = 34 μM). CGP 35348 can be used in studies of neuromuscular coordination and spatial learning after neonatal brain damage in albino mice. |
|
T21652 |
RN-1 dihydrochloride
|
|
Histone Demethylase
,
MAO
|
|
RN-1 dihydrochloride is an effective and selective irreversible inhibitor of lysine-specific demethylase 1 (LSD1, IC50 = 70 nM). |
|
T6504 |
Flupirtine maleate
|
Katadolon maleate |
Potassium Channel
,
NMDAR
,
iGluR
|
|
Flupirtine maleate (Katadolon maleate), a centrally acting non-opioid analgesia, is the salt form of Flupirtine. It is an NMDA receptor antagonist , and also a specific neuronal potassium channel opener. |
|
T15781 |
LP-935509
|
|
Serine/threonin kinase
,
AAK1 (AP2 associated kinase 1)
|
|
LP-935509 is highly brain-penetrant and reverses fully established pain behavior following the SNL procedure. LP-935509 is also an effective inhibitor of BIKE (IC50=14 nM) and a modest inhibitor of GAK (IC50=320 nM). LP-... |
|
T9157 |
GP130 receptor agonist-1
|
N-(4-Fluorophenyl)-4-phenyl-2-thiazolami |
Interleukin
|
|
GP130 receptor agonist-1 (N-(4-Fluorophenyl)-4-phenyl-2-thiazolami) is a potent, brain-penetrant and orally active GP130 receptor agonist. |
|
T9146 |
Ms48107
|
Benzenemethanol, 2-[4-amino-6-[[(4-phenoxyphenyl)methyl]amino]-1,3,5-triazin-2-yl]-3-fluoro- |
Others
|
|
MS48107 is a potent, selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68), demonstrating specificity for GPR68 over closely related proton GPCRs, neurotransmitter transporters, and hERG ion ch... |
|
T7476 |
AS057278
|
3-Methylpyrazole-5-carboxylic acid |
Others
|
|
AS057278 (3-Methylpyrazole-5-carboxylic acid) is an D-amino acid oxidase (DAAO) inhibitor. |
|
T22904 |
L-745870 trihydrochloride
|
L-745,870 trihydrochloride |
Dopamine Receptor
,
Sigma receptor
,
5-HT Receptor
,
Adrenergic Receptor
|
|
L-745870 trihydrochloride is a highly potent and selective D4 dopamine receptor antagonist. |
|
T3061 |
Lorlatinib
|
PF-6463922,PF-06463922,Loratinib |
Apoptosis
,
Tyrosine Kinases
,
ROS
,
ALK
,
ROS Kinase
|
|
Lorlatinib (PF-6463922) is an orally available, ATP-competitive inhibitor of the receptor tyrosine kinases, anaplastic lymphoma kinase (ALK) and C-ros oncogene 1 (Ros1), with potential antineoplastic activity. |
|
T16133 |
MRK-560
|
|
Gamma-secretase
|
|
MRK-560 is an effective and brain-penetrant inhibitor of γ-secretase. |
|
T16860 |
SBI-553
|
|
Neurotensin Receptor
|
|
SBI-553 is an effective and brain penetrant NTR1 allosteric modulator (EC50: 0.34 μM). |
|
T4087 |
S 38093 HCl
|
|
Histamine Receptor
|
|
S 38093 is a novel brain-penetrant antagonist/inverse agonist of H3 receptors. |
|
T16927 |
SR-3306
|
|
JNK
|
|
SR-3306 is a potent and highly inhibitor of brain penetrant JNK. |
|
T5472 |
PQR620
|
|
mTOR
|
|
PQR620 is a novel potent and selective, brain penetrant inhibitor of mTORC1/2. |
|
T3539 |
Lu AF21934
|
|
GluR
|
|
Lu AF21934 is a brain-penetrant and selective mGlu4 receptor positive allosteric modulator (IC50: 500 nM, human). |
|
T13323 |
VU6012962
|
|
GluR
|
|
|
|
T23349 |
SF 11
|
|
Others
|
|
SF 11 is a potent and brain penetrant neuropeptide Y Y2 receptor antagonist with IC50 of 199 nM. Antidepressant-like activity |
|
T15030 |
CycLuc1
|
|
Others
|
|
CycLuc1 is a brain penetrant luciferase substrate. CycLuc1 may be a superior BLI substrate as compared to D-luciferin for monitoring tumor growth of intracranial GBM xenografts. |
|
T4099 |
S 38093
|
S38093,S-38093 |
Histamine Receptor
|
|
S 38093 is a brain-penetrant antagonist of the H3 receptor (Ki: 8.8/1.44/1.2 μM, for rat/mouse/human). |
|
T1770 |
GNE-9605
|
|
LRRK2
|
|
GNE-9605 is a highly effective, specifical, and brain-penetrant LRRK2 inhibitor (IC50: 19 nM). |
|
T28069 |
ML380
|
ML 380,ML-380 |
AChR
|
|
ML380 is a highly potent and the first CNS penetrant M5 positive allosteric modulator (PAM). |
|
TQ0082 |
Aticaprant
|
LY-2456302,CERC-501 |
Opioid Receptor
|
|
Aticaprant (LY-2456302) (CERC-501) is a potent and centrally-penetrant antagonist of the kappa-opioid receptor (Ki: 0.807 nM). |
|
T14338 |
Atabecestat
|
JNJ-54861911 |
BACE
|
|
Atabecestat (JNJ-54861911) is a potent brain-penetrant and orally active β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor, achieves robust and high CSF Aβ reduction and it is tolerated and displays a ... |
|
T2050 |
PF-06447475
|
|
LRRK2
|
|
PF-06447475 is a highly effective, specific, brain penetrant LRRK2 inhibitor with IC0 of 3/11 nM for wild type LRRK2 and G2019S LRRK2 respectively. |
|
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. |
|
T5353 |
ABX-1431
|
Elcubragistat |
Lipase
|
|
ABX-1431 (Elcubragistat) is a selective and orally available CNS-penetrant monoacylglycerol lipase (MAGL/MGLL) inhibitor (IC50: 14 nM). |
|
T6639 |
RG2833
|
RGFP109 |
HDAC
|
|
RG2833 (RGFP109) (RGFP109), a brain-penetrant HDAC inhibitor, is with IC50 of 60 nM and 50 nM for HDAC1 and HDAC3, respectively. |
|
T23508 |
VU 0255035
|
|
AChR
|
|
muscarinic M1 antagonist |
|
T7549 |
Talnetant
|
SB 223412 |
Neurokinin receptor
|
|
Talnetant (SB 223412) is a selective, competitive, brain-penetrant NK3 receptor antagonist with the ability to modulate mesolimbic and mesocortical dopaminergic neurotransmission |
|
T0757 |
Omeprazole
|
Losec,Prilosec,H 16868,Antra |
Proton pump
,
Phospholipase
,
Antibacterial
,
Autophagy
|
|
Omeprazole (Losec) is a proton pump inhibitor (PPI), Omeprazole(Losec) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor). |
|
T8552 |
PSEM 89S TFA
|
|
AChR
|
|
PSEM 89S TFA is a brain-penetrant and selective ion channels agonist, and is orthogonally selective for Q79G and L141F, respectively. |
|
T15551 |
IDH889
|
|
Dehydrogenase
|
|
IDH889 is a brain penetrant, an allosteric and mutant specific IDH1 inhibitor. IDH889 has effective selectivity for IDH1 R132* mutations (IC50s: 0.02 μM, 0.072 μM, and 1.38 μM for IDH1R132H, IDH1R132C, and IDH1wt). |
|
T8431 |
JCN037
|
|
EGFR
|
|
JCN037 is potent, non-covalent and brain-penetrant inhibitor of EGFR(EGFR, p-wtEGFR and pEGFRvⅢ with IC50 of 2.49 nM, 3.95 nM, 4.48 nM , respectively). |
|
T10855 |
CO23
|
|
Thyroid hormone receptor(THR)
|
|
CO23 is a blood-brain barrier penetrant and selective TRα agonist and can be used in studies about the regulation of growth and development. |
