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T9833 |
Opiranserin hydrochloride
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|
P2X Receptor
,
GlyT
,
5-HT Receptor
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|
Opiranserin (VVZ-149) hydrochloride is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. It shows antagonistic activity on rP2X3 (IC50... |
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T11908 |
LY2365109 hydrochloride
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GlyT
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LY2365109 hydrochloride is a potent and selective GlyT1 inhibitor, with an IC50 of 15.8 nM for glycine uptake in cells over-expressing hGlyT1a. |
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T6788 |
Bitopertin
|
Paliflutine,RO4917838,RG1678 |
GlyT
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Bitopertin (Paliflutine) (RG1678, RO-4917838) is a potent inhibitor of glycine transporter 1 (GlyT1), with Ki of 8.1 nM for human hGlyT1b and IC50 of 22-25 nM in Chinese hamster ovary cells. |
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T6541 |
Ibutilide Fumarate
|
Corvert Fumarate,U70226E |
Calcium Channel
,
Sodium Channel
|
|
Ibutilide Fumarate (U70226E) is the fumarate salt form of ibutilide, a class III antiarrhythmic agent. Ibutilide exerts its effect by activating a slow, inward, predominately sodium current rather than by blocking outwar... |
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T6352 |
(-)-Dizocilpine maleate
|
C13737,(-)-MK 801 (Maleate),(-)-MK 801 Maleate |
NMDAR
,
iGluR
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(-)-Dizocilpine maleate ((-)-MK 801 (Maleate)) is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes. |
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T1050 |
Prazosin hydrochloride
|
Prazosin hydrochloride,Prazosin HCl,cp-12299-1,Peripress,Vasoflex,Minipress |
Potassium Channel
,
MRP
,
Adrenergic Receptor
,
ABC
,
Autophagy
|
|
Prazosin hydrochloride (Vasoflex) reduces peripheral resistance and relaxes vascular smooth muscles as a selective adrenergic alpha-1 antagonist by a mechanism not completely known. Prazosin hydrochloride is a synthetic ... |
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T16399 |
Opiranserin
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|
P2X Receptor
,
GlyT
,
5-HT Receptor
|
|
Opiranserin is a development as an injectable agent for the treatment of postoperative pain. Opiranserin is a non-opioid and non-NSAID analgesic candidate and is a dual antagonist of glycine transporter type 2 (GlyT2) an... |
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T21102 |
L-4FPG
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L4FPG,L 4FPG |
Others
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L-4FPG is a Glycine (HY-Y0966) derivative, inhibits the neutral amino acid transporters ASCT1 and ASCT2. |
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T3215 |
JNJ-42165279
|
JNJ42165279 |
FAAH
,
Autophagy
|
|
JNJ-42165279 covalently inactivates the FAAH enzyme but is highly selective with regard to other enzymes, ion channels, transporters, and receptors. JNJ-42165279 (10 μM) exhibits high selectivity against a panel of 50 re... |
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T3526 |
Dasotraline hydrochloride
|
SEP-225289 hydrochloride |
Dopamine Receptor
,
5-HT Receptor
,
Serotonin Transporter
,
Norepinephrine
|
|
Dasotraline hydrochloride (SEP-225289 hydrochloride) (SEP-225289 hydrochloride) is a triple reuptake inhibitor that inhibits dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respe... |
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T7941 |
Imipramine hydrochloride
|
Imipramine (hydrochloride),Tofranil,G 22355,Imipramine HCl,Melipramine |
Serotonin Transporter
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|
Imipramine hydrochloride (Imipramine HCl) is a first generation tricyclic antidepressant that acts primarily as an inhibitor of serotonin and norepinephrine transporters (Kds = 1.4 and 37 nM, respectively).Imipramine hyd... |
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T9146 |
Ms48107
|
Benzenemethanol, 2-[4-amino-6-[[(4-phenoxyphenyl)methyl]amino]-1,3,5-triazin-2-yl]-3-fluoro- |
Others
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|
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... |
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T19649 |
PF-06273340
|
PF 6273340,PF 06273340,PF6273340,PF-6273340 |
Trk receptor
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|
PF-06273340 is an effective, Selective, and Peripherally Restricted Pan-Trk inhibitor (IC50: Trk-A = 6 nM; Trk-B = 4 nM; Trk-C = 3 nM). PF-06273340 has low metabolic turnover in HLM and hHep is a good substrate for efflu... |
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T11689 |
ITI-214
|
ITI214 |
PDE
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ITI-214 is a picomolar PDE1 inhibitor with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters, and ion channels, exhibits potent PDE1 inhibitory activity (Ki = ... |
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T4664 |
ML 297
|
ML297 |
Potassium Channel
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ML 297 is a selective Kir3.1/3.2 (GIRK1/2) channel activator (IC50 values are 160, 887 and 914 nM for GIRK1/2, GIRK1/4 and GIRK1/3 respectively). ML 297 exhibits no effect on GIRK2, GIRK2/3, Kir2.1 and Kv7.4 channels, an... |
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T4410 |
LM10
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|
Others
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Selective tryptophan 2, 3-dioxygenase (TDO) inhibitor (IC50 values are 0.62 and 2 μM for human and mouse TDO, respectively). Exhibits selectivity for TDO over IDO, MAO-A, MAO-B, and a panel of receptors and transporters.... |
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T17243 |
VU0463271
|
N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide |
Potassium Channel
|
|
VU0463271 (N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide) is a potent and selective antagonist of the neuronal-specific potassium-chloride cotransporter 2 (KCC2), with an IC50 of 61 nM ... |
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T2194 |
Direct Blue 1
|
Pontamine sky blue,Chicago Sky Blue 6B |
GluR
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Direct Blue 1 (Pontamine sky blue), a counterstain for background autofluorescence in immunofluorescence histochemistry, structurally resembles glutamate and operates as a potent, competitive VGLUT inhibitor, not impacti... |
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T15773 |
Lofepramine
|
Gamanil,Amplit,Leo 640,Lopramine |
5-HT Receptor
,
Norepinephrine
|
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Lofepramine (Leo 640) is a potent tricyclic antidepressant that is extensively metabolized to desipramine. It inhibits the serotonin and norepinephrine transporters by inhibiting neurons with Kd values of 70 and 5.4 nM, ... |
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T3625 |
Bempedoic acid
|
ETC1002,ESP-55016,ETC 1002,ETC-1002 |
ATP Citrate Lyase
,
AMPK
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Bempedoic acid (ETC1002) is an orally available, once-daily LDL-C lowering small molecule designed to lower elevated levels of LDL-C and to avoid side effects associated with existing LDL-C lowering therapies. Bempedoic ... |
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T8720 |
PRX-07034 hydrochloride
|
PRX-07034 |
5-HT Receptor
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PRX-07034 hydrochloride is a selective antagonist of 5-HT6 receptor. It has cognition and memory-enhancing properties and potently decreases food intake and body weight in rodents. PRX-07034 hydrochloride is both a poten... |
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T15411 |
GPNA hydrochloride
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Apoptosis
,
Others
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GPNA hydrochloride is specific glutamine (Gln) transporter ASCT2(SLC1A5) inhibitor. GPNA reversibly induces apoptosis in A549 cells. GPNA hydrochloride is a well-known substrate of the enzyme γ-glutamyltransferase (GGT).... |
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T41194 |
FFN 102 mesylate
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Others
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FFN 102 mesylate is a pH responsive fluorescent false neurotransmitter (FFN), a selective dopamine transporter (DAT) and VMAT2 substrate. Exhibits no significant binding to a panel of 38 CNS receptors, including dopamine... |
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T32873 |
Maralixibat Chloride
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SHP-625,SHP625,Livmarli,LUM001 chloride,Lopixibat chloride,Lopixibat,SHP625 chloride,SHP 625 |
Potassium Channel
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Maralixibat Chloride (LUM001 chloride), an apical, sodium-dependent, bile acid transport inhibitor, prevents enterohepatic bile acid recirculation. |
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T23752 |
AR-C141990
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ARC-141990,AR C141990,ARC141990,ARC 141990 |
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AR-C141990 is a lactate transporters inhibitor. |
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T70341 |
D-473
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|
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D-473 is a novel orally active triple reuptake inhibitor targeting dopamine, serotonin and norepinephrine transporters. |
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T22867 |
Indatraline hydrochloride
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Others
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Inhibits transporters for 5-HT (SERT), dopamine (DAT) and noradrenalin (NET) |
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T39767 |
AR-C141990 hydrochloride
|
AR-C141990 hydrochloride |
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AR-C141990 hydrochloride is a potent inhibitor of lactate transporters known as monocarboxylate transporters (MCTs). It has pK i values of 7.6 and 6.6 for MCT-1 and MCT-2, respectively. Additionally, this compound exhibi... |
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T21451 |
Nefazodone
|
Nefadar,Dutonin,Serzone |
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Nefazodone is an antidepressant. It has low affinity for the serotonin (200 nM), dopamine (360 nM), and norepinephrine (360 nM) transporters, and therefore acts as a weak serotonin-norepinephrine-dopamine reuptake inhibi... |
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T69767 |
NV-5440
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|
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NV-5440 is a novel cell penetrant, potent and selective class I glucose transporters (GLUT1) inhibitor, selectively inhibiting mTORC1 |
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T69889 |
JBP485
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|
|
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JBP485 is an inhibitor of renal transporters OAT1 and OAT3. JBP485 is an antihepatitis agent as a substrate for intestinal PEPT1. |
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T70315 |
AGI-16903
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|
|
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AGI-16903 is a metabolite of enasidenib -- an isocitrate dehydrogenase-2 inhibitor that has been shown to inhibit human nucleoside transporters and uptake of azacitidine in oocytes. |
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T26363 |
Napitane Mesylate
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ABT-200,A-75200 |
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Napitane Mesylate is a potent alpha 2-adrenoceptor antagonist. Napitane Mesylate blocks norepinephrine uptake by inhibiting the norepinephrine transporter. Napitane Mesylate also binds to CA transporters in the central n... |
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T25292 |
DCCCyb
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|
|
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DCCCyb is an orally bioavailable and selective GlyT1 Inhibitor. DCCCyb demonstrated excellent in vivo occupancy of GlyT1 transporters in rhesus monkeys as determined by the displacement of a PET tracer ligand. |
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T11688 |
ITI-214 free base
|
ITI214 free base |
Others
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ITI-214 free base is a picomolar PDE1 inhibitor with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters, and ion channels, exhibits potent PDE1 inhibitory activ... |
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T70615 |
TAS-303
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|
|
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TAS-303 is a selective norepinephrine reuptake inhibitor which displays significant norepinephrine transporter (NET) inhibitory activity toward serotonin or dopamine transporters. Radioligand-binding studies showed that ... |
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T70760 |
NVP018
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|
|
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NVP018, also known as BC 556, is a potent inhibitor of hepatitis B virus, hepatitis C virus (HCV), and HIV-1 replication, shows minimal inhibition of major drug transporters, and has a high barrier to generation of both... |
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T70469 |
AK-42
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|
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AK-42 is a novel potent and specific inhibitor of CLC-2, displaying unprecedented selectivity over CLC-1, the closest CLC-2 homolog, and exhibiting no off-target engagement against a panel of 61 common channels, receptor... |
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T39878 |
FFN270 hydrochloride
|
FFN270 hydrochloride |
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FFN270 hydrochloride, a fluorescent tracer for norepinephrine and vesicular monoamine transporters, features dual resolved absorption/excitation peaks that vary with solvent pH (FFN270 ex: 320 nm or 365 nm, em: 475 nm). ... |
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T68326 |
Annamycin
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|
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Annamycin is a semi-synthetic doxorubicin analogue annamycin with antineoplastic activity. Annamycin intercalates into DNA and inhibits topoisomerase II, resulting in the inhibition of DNA replication and repair and RNA ... |
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T39976 |
MS67
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|
|
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MS67 is a potent and selective degrader of the WD40 repeat domain protein 5 (WDR5) with a dissociation constant (Kd) of 63 nM. It exhibits no activity against protein methyltransferases, kinases, G-protein-coupled recept... |
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T28648 |
S39625
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S-39625,S 39625 |
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S39625, an E-ring camptothecin keto analogue, is a stable, potent, and selective topoisomerase I inhibitor without being substrates of drug efflux transporters. Nanomolar concentrations of S39625 induces intense and pers... |
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T74582 |
Trimipramine N-oxide
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|
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Trimipramine N-oxide, an active metabolite of the tricyclic antidepressant trimipramine, effectively inhibits human monoamine transporters for noradrenaline (hNAT), serotonin (hSERT), dopamine (hDAT), and the human organ... |
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T37453 |
Butyryl-L-carnitine (chloride)
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|
|
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Butyryl-L-carnitine is a butyrate ester of carnitine. It is an inhibitor of intestinal transporters, blocking carnitine uptake by the carnitine transporter and glycine transport by the amino acid transporter in human ret... |
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T28183 |
NNC052090
|
NNC-052090,NNC-05-2090,NNC05-2090,NNC 052090,NNC 05-2090 |
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NNC052090 is a GABA uptake inhibitor that displays moderate selectivity for BGT-1 transporters with Ki values are 1.4, 15, 19 and 41 μM for hBGT-1, hGAT-3, hGAT-1 and hGAT-2 respectively. NNC052090 also displays affinity... |
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T37699 |
Org 24598
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|
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Potent and selective inhibitor of the glial glycine transporter GlyT1b (IC50 = 6.9 nM). Displays negligible activity at GlyT-2, adrenoreceptors, dopamine, 5HT receptors and noradrenaline, dopamine, 5HT and GABA transport... |
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T16393 |
ONO-2952
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Others
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ONO-2952 is more selective for TSPO than other receptors, transporters, ion channels, and enzymes. ONO-2952 is a potent and selective translocator protein 18 kDa (TSPO) antagonist (Ki: 0.33-9.30 nM for rat and human TSPO... |
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T39397 |
S-MGB-234
|
|
|
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S-MGB-234 is a minor groove binder utilized for the treatment of Animal African Trypanosomiasis (AAT). It exhibits exceptional in vitro efficacy against the primary causative agents of AAT, namely Trypanosoma congolense ... |
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T71764 |
YM 298198 Hydrochloride
|
|
|
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YM 298198 Hydrochloride is a non-competitive antagonist with high affinity and selectivity for mGlu1 receptors (Ki = 19 nM). YM 298198 Hydrochloride is inactive at other mGlu receptor subtypes (mGlu2-7), ionotropic recep... |
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T78201 |
PU-48
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|
|
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PU-48 is a potent inhibitor of urea transporters A (UT-A) with an IC50 value of 0.32 μM, exhibiting a significant diuretic effect in mouse models without notable cytotoxicity. This compound has the potential for further ... |
