|
T5447 |
Anle138b
|
|
Beta Amyloid
,
Others
|
|
Anle138b: a novel oligomer modulator for disease-modifying therapy of neurodegenerative diseases such as prion and Parkinson's disease |
|
T60003 |
AC1-IN-1
|
|
Adenylyl cyclase
|
|
AC1-IN-1 is a selective inhibitor of adenylyl cyclase type 1 (AC1, IC50 = 0.54 µM). |
|
T5513 |
RO-3
|
|
P2X Receptor
|
|
RO3 is a selective antagonist of homomeric P2X3 and heteromeric P2X2/3 receptor |
|
T2354 |
UNC 0631
|
UNC0631 |
Histone Methyltransferase
|
|
UNC 0631 is a effectvie histone methyltransferase G9a inhibitor (IC50=4 nM). |
|
TQ0232 |
UNC0646
|
UNC 0646 |
Histone Methyltransferase
|
|
UNC0646 is a potent and selective inhibitor of the homologous protein lysine methyltransferases, G9a and GLP (IC50s: 6 nM/15 nM for G9a/GLP). UNC0646(UNC 0646) potently blocks G9a/GLP methyltransferase activity in cells ... |
|
T11799 |
L-745870 hydrochloride
|
|
Dopamine Receptor
|
|
L-745870 hydrochloride has excellent brain penetration. L-745870 hydrochloride is a high-affinity, selective and orally active human dopamine D4 receptor antagonist with a Ki of 0.43 nM, and considerably weaker D2 recept... |
|
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. |
|
T2344 |
LY 344864
|
LY344864 |
5-HT Receptor
|
|
LY 344864, a specifc receptor agonist, is an affinity of 6 nM (Ki) at the recently cloned 5-HT1F receptor. |
|
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. |
|
T6920 |
ON123300
|
|
FGFR
,
c-RET
,
JAK
,
CDK
,
PDGFR
,
Src
,
AMPK
|
|
ON123300 is a potent and multi-targeted kinase inhibitor for CDK4/Ark5/PDGFRβ/FGFR1/RET/Fyn (IC50: 3.9/5/26/26/9.2/11 nM). |
|
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. |
|
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). |
|
T10905 |
CXCR2-IN-1
|
|
CXCR
|
|
CXCR2-IN-1 has a pIC50 of 9.3 and is a CXCR2 antagonist of the central nervous system penetration agent. |
|
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. |
|
T14345 |
Atropine methyl bromide
|
Methylatropine bromide |
AChR
|
|
Atropine methyl bromide (Methylatropine bromide) is a quaternary ammonium salt of atropine, characterized as a muscarinic receptor (mAChR) antagonist. It functions as a mydriatic to dilate the pupil during ophthalmic exa... |
|
TP2501 |
Difelikefalin acetate
|
Difelikefalin acetate(1024828-77-0 free base),CR 845 acetate,FE 202845 acetate |
Opioid Receptor
|
|
Difelikefalin acetate (CR 845 acetate) is a peripherally restricted kappa opioid receptor agonist. CR845 exhibit low P450 CYP inhibition and low penetration into the brain. |
|
T35914 |
Epitinib succinate
|
HMPL-813 succinate |
EGFR
|
|
Epitinib succinate (HMPL-813 succinate) is an orally active and brain penetration EGFR tyrosine kinase inhibitor and can be used in studies about cancer. |
|
T33604 |
Z-Glycine
|
Carbobenzoxyglycine,N-Carbobenzoxyglycine |
Others
|
|
Z-Glycine (Carbobenzoxyglycine) is a drug-lipid conjugates designed to promote brain penetration based on its lipophilicity and resemblance to lipids in biological membranes[1]. |
|
T10335 |
Antihistamine-1
|
|
P450
|
|
Antihistamine-1 is an H1-antihistamine (Ki: 6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel (IC50s: 5.4 and 0.8 μM). |
|
T61383 |
Diaziquone
|
NSC 182986 |
|
|
Diaziquone (NSC-182986) is a water-soluble synthetic azacyclic benzoquinone that enhances penetration of the blood-brain barrier, has antitumor activity, and is used in the treatment of extreme renal failure. |
|
T61148 |
Flutrimazole
|
|
Antifungal
|
|
Flutrimazole is a dual-action imidazole antifungal compound, exhibiting both anti-inflammatory and antifungal properties. Notably, flutrimazole demonstrates limited transdermal penetration, making it particularly advanta... |
|
T10630 |
BuChE-IN-TM-10
|
TM-10 |
AChR
|
|
BuChE-IN-TM-10 (TM-10) is a potent inhibitor of butyrylcholinesterase (BuChE), exhibiting an IC50 of 8.9 nM. It effectively inhibits and disaggregates self-induced Aβ aggregation, displays significant antioxidant activit... |
|
T20870 |
IR-820
|
IR 820,IR820,New Indocyanine Green |
|
|
IR-820 (New Indocyanine Green) is a near-infrared dye with better stability, good color rendering, and excellent fluorescence penetration. IR-820 is an infrared blood pool contrast agent used to detect and quantify disea... |
|
TP2505L |
LAH4 acetate
|
KKALLALALHHLAHLALHLALALKKA acetate,LAH4 acetate(184776-51-0 Free base) |
Antibacterial
|
|
LAH4 acetate is the α-helical structure of the designed amphoteric peptide antibiotic, which is capable of complexing DNA, associating with the cell surface membrane and wrapped in the endosome, which is destroyed with t... |
|
T1101 |
Minocycline hydrochloride
|
Minocycline HCl |
HIF/HIF Prolyl-Hydroxylase
,
Antibacterial
,
Antibiotic
|
|
Minocycline hydrochloride (Minocycline HCl) is a tetracycline antibiotic with excellent absorption and tissue penetration that is used for several bacterial infections as well as treatment of acne. Minocycline hydrochlor... |
|
T25124 |
AZ599
|
AZ-599,AZ 599 |
|
|
AZ599 is a full agonist of CB1 with good solubility and low CNS penetration. |
|
T12179 |
Nav1.1 activator 1
|
|
Others
|
|
Nav1.1 activator 1 is a highly potent activator of Nav1.1 with BBB penetration. |
|
T12416 |
PF-03654746 Tosylate
|
|
Histamine Receptor
|
|
PF-03654746 Tosylate is selective antagonist of histamine H3 receptor with high brain penetration. |
|
T29016 |
Trolamine salicylate ester
|
Trolamine salicylate (ester) |
|
|
Trolamine salicylate (ester) is a salicylate ester with Trolamine. Trolamine salicylate ester may have better skin 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. |
|
T29359 |
2-n-Nonyl-1,3-dioxolane
|
AI3-22560,Decanal ethylene acetal,2-Nonyldioxolane |
|
|
2-n-Nonyl-1,3-dioxolane is a biochemical. It is used as an absorption and penetration enhanceron transdermal. |
|
T26722 |
AZD7268
|
AZD-7268,AZD 7268 |
|
|
AZD7268 is a potent, selective, reversible, and orally bioavailable agonist of δ-opioid receptor with CNS penetration. |
|
T27437 |
GS-462808
|
GS462808,GS 462808 |
|
|
GS-462808 is a late sodium current inhibitor of the cardiac Nav1.5 channel. GS-462808 had lower brain penetration and serendipitously lower activity at the brain isoforms. |
|
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. |
|
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. |
|
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. |
|
T11799L |
L-745870
|
|
Dopamine Receptor
|
|
L-745870 is a high-affinity and selective human dopamine D4 receptor antagonist (Ki: 0.43 nM). L-745870 has excellent brain penetration. It considerably weaker D2 (Ki: 960 nM) and D3 (Ki: 2300 nM) receptors affinity. |
|
T11797 |
L-690488
|
|
Others
|
|
L-690488 has more effective cell penetration than L-690330. L-690488 is a prodrug of L-690330 and is a selective inositol monophosphatase (IMPase) inhibitor. |
|
T39102 |
MLK-IN-1
|
|
|
|
MLK-IN-1 (US20140256733A1, compound 68) is a highly potent and selective inhibitor of mixed lineage kinase 3 (MLK-3). It exhibits excellent brain penetration and specifically targets MLK-3. |
|
T82175 |
HR2-18
|
|
|
|
HR2-18 is a bioactive peptide that inhibits SARS-CoV penetration into cells. |
|
T40438 |
PEG-8 laurate
|
|
|
|
PEG-8 laurate is a monofunctional surfactant and skin penetration enhancer. It disrupts the skin barrier and facilitates the formation of elastic vesicles when synthesized. |
|
T38586 |
Grepafloxacin
|
dl-Grepafloxacin,OPC-17116 |
|
|
Grepafloxacin (OPC-17116) is a fluoroquinolone antibiotic that is administered orally. It possesses strong efficacy against community-acquired respiratory pathogens, notably Streptococcus pneumonia. Grepafloxacin exhibit... |
|
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). |
|
T71037 |
BAY-438
|
|
|
|
BAY-438 is an allosteric MEK inhibitor with long half-lives, high bioavailabilities, low brain penetration potential and high efficacy in a K-Ras-mutated A549 xenograft model. |
|
T70133 |
BAY-846
|
|
|
|
BAY-846 is an allosteric MEK inhibitor with long half-lives, high bioavailabilities, low brain penetration potential and high efficacy in a K-Ras-mutated A549 xenograft model. |
|
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... |
|
T16772 |
Ro 64-6198
|
|
Others
|
|
Ro 64-6198 is a nonpeptide, high-affinity, and brain penetration N/OFQ receptor (NOP) agonist (EC50: 25.6 nM). Ro 64-6198 is at least 100 times more selective for the NOP receptor over the classic opioid receptors. |
|
T33441 |
MK789
|
MK 789,MK-789 |
|
|
MK-789 is an inhibitor of dehydropeptidase I. MK-789 and MK-791 alter the renal excretion of N-formimidoyl thienamycin from glomerular filtration plus tubular secretion to glomerular filtration only, possibly by competit... |
|
T60533 |
Nln activator 1
|
|
|
|
Nln activator 1 is a first-in-class activator of peptidomimetic neurolysin with enhanced brain penetration and stability. |
