| DC73604 |
TMEM16A blocker 1PBC
Featured
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1PBC is a small molecule blocker of calcium-activated chloride channel TMEM16A, blocks TMEM16A completely with an IC50 of 4 uM at zero mV and saturating Ca2+ concentration (2 uM). |
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| DC73605 |
TMinh-23
Featured
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TMinh-23 is (Compound 10bm) is a potent, selective inhibitor of transmembrane protein 16A (TMEM16A or ANO1, DOG1, ORAOV2, TAOS-2) with IC50 of 30 nM in short-circuit current assays, weakly inhibits TMEM16B (IC50=400 nM, 13 -fold selectivity). |
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| DC73606 |
VI-116 |
VI-116 is a potent and selective volume-regulated anion channel (VRAC) inhibitor, fully inhibits VRAC-mediated I- quenching with an IC50 of 1.27 uM in LN215 cells. |
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| DC73607 |
ART26.12 |
ART26.12 is a third generation, selective fatty acid-binding protein 5 (FABP5) inhibitor with Ki value of 0.77 uM, >25-fold selective over FABP3, FABP4 and FABP7. |
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| DC73609 |
ASP8062 |
ASP8062 is a potent, selective GABA B receptor positive allosteric modulator (PAM), positive allosteric modulating activity for human and rat GABAB receptors, exerts analgesic effects in rat model of fibromyalgia. |
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| DC73610 |
DS-II-73 |
DS-II-73 is a selective α2/3/5-containing GABAA receptor (GABAAR) potentiator with IC50 of 320 nM, 381 nM and 435 nM for α2β3γ2 α3β3γ2 α5β3γ2. |
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| DC73611 |
SGS742 |
CGP 36742 (SGS-742) is a BBB-penetrant GABAB receptor antagonist, discretely up-regulates GABAB receptor binding sites. |
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| DC73612 |
Glutipyran |
Glutipyran is a small-molecule glucose transporter inhibitor, inhibits glycolytic activity and cell growth in human pancreatic cancer cells. |
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| DC73613 |
(R)-AS-1 |
(R)-AS-1 is an orally bioavailable, selective positive allosteric modulator (PAM) of the glutamate transporter EAAT2 with EC50 of 11 nM and Emax of 251%, shows potent antiseizure activity in vivo. |
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| DC73614 |
GT951 |
GT951 (GT-951) is a potent, selective activator (positive allosteric modulator) of EAAT2 with EC50 of 0.8 nM in vitro glutamate uptake assays in COS cells overexpressing EAAT2. |
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| DC73615 |
GTS467 |
GTS476 (GTS-476) is a potent, selective, orally active activator of EAAT2 with EC50 of 35.1 nM in vitro glutamate uptake assays in COS cells overexpressing EAAT2. |
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| DC73616 |
GTS511 |
GTS511 (GTS-511) is a potent, selective, brain-permeable activator of EAAT2 with EC50 of 3.8 nM in vitro glutamate uptake assays in COS cells overexpressing EAAT2. |
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| DC73617 |
NV-6297
Featured
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NV-6297 (NV6297) is a potent, selective mTORC1 pathway signaling inhibitor without inhibition on mTORC2, inhibits S6K1 phosphorylation (pS6K1 T389) in MCF7 cells with IC50 of 120 nM, directly and selectively targets GLUT-1. |
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| DC73618 |
NUCC-0200590 |
NUCC-0200590 is a small-molecule inhibitor of the TRIP8b-HCN interaction with IC50 of 7.0 uM in AlphaScreen assays, effectively disrupts the TRIP8b-HCN interaction in vitro and in vivo. |
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| DC73619 |
Org 34167
Featured
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Org 34167 HCl salt is a broad-spectrum inhibitor of HCN channels with IC50 of 23.4, 8.2 and 9.2 uM for HCN1, HCN2 and HCN4 channels, respectively, slowing activation and causing a hyperpolarising shift in voltage-dependence of activation. |
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| DC73620 |
RO-275 |
RO-275 is a potent, selective HCN1 ion channel inhibitor with IC50 of 46 nM, displays 311/100/302-fold selectivity over HCN2/HCN3/HCN4. |
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| DC73621 |
(R)-OF-NB1 |
(R)-OF-NB1 is a small molecule splice variant GluN2B-selective NMDAR antagonist with IC50 of 675 nM and 97 nM for F-NB1 for splice variant containing exon 5 and GluN1-1a in X. laevis oocytes. |
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| DC73622 |
(S)-(-)-DQP-997-74 |
(S)-(-)-DQP-997-74 is a potent, selective GluN2C- and GluN2D-containing NMDARs negative allosteric modulator with IC50 of 69 and 35 nM, respectively, exhibits >100- and >300-fold over GluN2A- and GluN2B-containing receptors. |
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| DC73623 |
DQP-997-74 |
DQP-997-74 is a potent, selective GluN2C- and GluN2D-containing NMDARs negative allosteric modulator with IC50 of 0.35 and 0.13 uM, respectively, exhibits >100-fold over GluN2A- and GluN2B-containing receptors. |
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| DC73624 |
FP802 |
FP802 is a potent neuroprotectant and small molecule inhibitor of TwinF interface, shows selective elimination of eNMDAR-mediated toxicity via disruption of the NMDAR/TRPM4 death signaling complex, while sparing the vital physiological functions of synapt |
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| DC73625 |
GluN2A PAM (R)-9 |
GluN2A PAM (R)-9 is a potent, brain penetrant, GluN2A-selective positive allosteric modulator with EC50 of 0.51 uM, Emax 350%. |
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| DC73626 |
Org 26576 |
Org 26576 (MK 8777. |
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| DC73627 |
PTC-174 |
PTC-174 is a selective, positive allosteric modulator of NMDA receptors containing GluN2C or GluN2D subunits with EC50 of 4.1 uM (GluN1/2C) and 5.7 uM (GluN1/2D). |
|
| DC73628 |
UBP1700 |
UBP1700 is a subtype-selective competitive antagonist of GluN2C/2D-containing NMDA receptors with Ki of 7-9 nM, 50-fold selectivity over GluN2A and GluN2B. |
|
| DC73629 |
UBP791 |
UBP791 is a subtype-selective competitive antagonist of GluN2C/2D-containing NMDA receptors with Ki of 80-90 nM, 50-fold selectivity over GluN2A and GluN2B. |
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| DC73630 |
UBP792 |
UBP792 is a novel negative allosteric modulator (antagonist) of NMDA receptors, displays partial subtype-selectivity by having a varied maximal inhibition of GluN2A-, GluN2B-, GluN2C-, and GluN2D-containing receptors (52%, 70%, 87%, 89%, respectively) wit |
|
| DC73631 |
ZCAN155 |
ZCAN155 is a small molecule that prevents AMPA-mediated excitotoxicity (IC50=35 nM) by targeting an allosteric binding site of AMPA glutamate receptor 2 (GluA2), restores neurological function and myelination. |
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| DC73632 |
ZCAN262 |
ZCAN262 is a small molecule that prevents AMPA-mediated excitotoxicity (IC50=8.5 nM) by targeting an allosteric binding site of AMPA glutamate receptor 2 (GluA2). |
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| DC73633 |
(S)-CE-123 |
(S)-CE-123 is a specific small molecule dopamine transporter (DAT) inhibitor, improves memory acquisition and memory retrieval. |
|
| DC73634 |
CDTP-32476 |
CDTP-32476 is a potent slow-onset dopamine reuptake blocker with an affinity of 8.6 nM, CDTP-32476 is moderately selective (14-fold) versus NE reuptake blockade with little effect on the SERT. |
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