|
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. |
|
T9452 |
PW0787
|
|
GPR
|
|
PW0787 is a potent, selective, orally active, and brain-penetrant GPR52 agonist (EC50=135 nM). |
|
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... |
|
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. |
|
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. |
|
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. |
|
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... |
|
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. |
|
T16927 |
SR-3306
|
|
JNK
|
|
SR-3306 is a potent and highly inhibitor of brain penetrant JNK. |
|
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. |
|
T5472 |
PQR620
|
|
mTOR
|
|
PQR620 is a novel potent and selective, brain penetrant inhibitor of mTORC1/2. |
|
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. |
|
T3539 |
Lu AF21934
|
|
GluR
|
|
Lu AF21934 is a brain-penetrant and selective mGlu4 receptor positive allosteric modulator (IC50: 500 nM, human). |
|
T1770 |
GNE-9605
|
|
LRRK2
|
|
GNE-9605 is a highly effective, specifical, and brain-penetrant LRRK2 inhibitor (IC50: 19 nM). |
|
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 |
|
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. |
|
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. |
|
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). |
|
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. |
|
T23508 |
VU 0255035
|
|
AChR
|
|
muscarinic M1 antagonist |
|
T5387 |
LP-211
|
|
Dopamine Receptor
,
5-HT Receptor
|
|
LP-211 is a brain penetrant selective agonist for a 5-HT7 receptor (Ki: 0.58 nM), and >300-fold selectivity over the 5-HT1A receptor. |
|
T14671 |
BMS-193885
|
|
Neuropeptide Y Receptor
|
|
BMS-193885 is a selective, brain-penetrant, and competitive antagonist of the neuropeptide Y1 receptor with a Ki of 3.3 nM, and an IC50 of 5.9 nM for hY1. |
|
T6057 |
URMC-099
|
|
ROCK
,
MLK
,
VEGFR
,
SGK
,
DNA Alkylation
,
Trk receptor
,
c-Met/HGFR
,
LRRK2
,
MEK
,
IGF-1R
,
Syk
,
Bcr-Abl
,
CDK
,
Src
,
Aurora Kinase
,
Autophagy
|
|
URMC-099 is an orally bioavailable, brain penetrant MLK inhibitor (IC50: 19/42/14/150 nM, for MLK1/MLK2/MLK3/DLK), and also inhibits LRRK2 activity (IC50: 11 nM). |
|
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). |
|
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 |
|
T5185 |
PZ-2891
|
|
Others
|
|
PZ-2891 is an orally bioavailable, brain penetrant pantothenate kinase (PANK) modulator(hPANK3,IC50:1.3 nM). |
|
T37806 |
JNJ-55308942
|
|
P2X Receptor
|
|
JNJ-55308942 is a selective and brain-penetrant antagonist of P2X7 functional with IC50s of 10 and 15 nM and Kis of 7.1 and 2.9 nM for hP2X7 and rP2X7, respectively. |
|
T4236 |
AR-M 1000390 hydrochloride
|
ARM390 Hydrochloride,ARM-390 HCl |
Opioid Receptor
|
|
AR-M 1000390 hydrochloride (ARM-390 HCl) , also known as ARM-390, is a low-internalizing nonpeptidic δ-selective opioid receptor agonist; derivative of SNC 80. Does not trigger acute desensitization of the analgesic resp... |
|
T5482 |
TG4-155
|
|
Prostaglandin Receptor
|
|
TG4-155 is a brain penetrant EP2 antagonist (KB = 2.4 nM) that is over 1000-fold less effective at EP4 (KB = 11.4 µM) and a panel of other receptors and channels |
|
T8423 |
ML417
|
|
Dopamine Receptor
,
Arrestin
|
|
ML417 is a selective and brain penetrant agonist of D3 Dopamine (EC50 : 38 nM). |
|
T11599 |
Ibiglustat (L-Malic acid)
|
Ibiglustat L-Malic acid,GZ402671 (L-Malic acid),Venglustat (L-Malic acid),SAR402671 (L-Malic acid) |
Transferase
|
|
Ibiglustat (L-Malic acid) (Ibiglustat L-Malic acid) is a selective, brain-penetrant, and allosteric inhibitor of glucosylceramide synthase. Ibiglustat (L-Malic acid) can be used in studies about PD Parkinson’s disease, S... |
