| DC72788 |
AZD0095
Featured
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AZD0095 is a selective and orally active MCT4 inhibitor (IC50: 1.3 nM). AZD0095 effectively inhibits the tumor growth in NCI-H358 xenograft in combination with Cediranib. |
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| DC72806 |
Camlipixant
Featured
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Camlipixant (BLU-5937) a potent, selective, non-competitive and orally active P2X3 homotrimeric receptor antagonist with an IC50 of 25 nM against hP2X3 homotrimeric. Camlipixant shows potent anti-tussive effect and no taste alteration. Camlipixant can be used for the research of unexplained, refractory chronic cough. |
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| DC72829 |
Zuranolone
Featured
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Zuranolone(SAGE-217, CS-2797) is an orally active and potent neuroactive steroid and positive allosteric modulator of the GABAA receptor, with EC50s of 296 nM for α1β2γ2 receptor. |
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| DC72837 |
FM04 |
FM04 is a potent P-glycoprotein (P-gp) inhibitor (EC50=83 nM). FM04 inhibits P-gp in 2 mechanism: (1)FM04 binds to Q1193, followed by interacting with the functionally critical residues H1195 and T1226; or (2)FM04 binds to I1115 (a functionally critical residue itself), disrupting the R262-Q1081-Q1118 interaction pocket and uncoupling ICL2-NBD2 interaction and thereby inhibiting P-gp. |
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| DC72866 |
ML-213 |
ML213 is a novel potent, selective KCNQ2 (Kv7.2) and KCNQ4 (Kv7.4) activator with EC50 of 230 and 510 nM, respectively.
ML213 displays >80-fold selectivity over other related potassium channels (KCNQ1/3/5).
ML213 causes significant hyperpolarization in mesenteric artery smooth muscle cells, shows potent vasorelaxant effects in different blood vessels. |
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| DC72875 |
GLPG2451 |
GLPG2451 (GLPG 2451) is a potent potentiator of cystic fibrosis transmembrane conductance regulator (CFTR) with EC50 of 11 nM for F508del CFTR in the YHA assay and EC50 of 18 nM in TECC assay using HBE cells from patients carrying the F508del mutation.
GLPG2451 improves the gating function of the CFTR channel. |
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| DC73592 |
A3907 |
A3907 is an apical sodium-dependent bile acid transporter (ASBT) inhibitor. |
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| DC73593 |
ML753286 |
ML753286 is a potent, selective BCRP inhibitor with IC50 of 0.6 uM (BCRP efflux transporter), shows no activity against P-glycoprotein (P-gp), organic anion-transporting polypeptide (OATP), or major cytochrome P450s (CYPs). |
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| DC73594 |
2E151 |
2E151 is a small molecule calcium channel activator, increases murine antigen-specific antibody responses when used as a co-adjuvant with LPS. |
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| DC73595 |
2D216 |
2D216 is a small molecule calcium channel activator, increases murine antigen-specific antibody responses when used as a co-adjuvant with LPS. |
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| DC73596 |
Efonidipine hydrochloride |
Efonidipine (NZ-105) is a potent, dual T-type and L-type calcium channel blocker, exhibits antihypertensive effect through vasodilatation. |
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| DC73597 |
Extracellular vesicle enhancer 634 |
Extracellular vesicle enhancer 634 (Compound 634) is a small molecule enhancer of extracellular vesicle (EV) release with immunostimulatory potency via induction of Ca2+ influx, which is mediated by store-operated Ca2+ entry (SOCE). |
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| DC73598 |
IPPQ |
IPPQ is a small molecule that selectively target the interface between the N-type calcium (CaV2.2) channel and CaVβ, specifically binds to CaVβ2a and inhibits CaVβ2's interaction with CaV.2-AID (alpha interacting domain). |
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| DC73599 |
PST3093 |
PST3093 (PST 3093) is the main Istaroxime metabolite and a selective SERCA2a activator, reduces the SERCA2a KdCa value by about 20% at 100 nM. |
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| DC73600 |
TMDJ-035 |
TMDJ-035 is the first highly potent and selective ryanodine receptor 2 (RyR2) inhibitor with EC50 of 13 nM, shows no effect on RyR1 and RyR3. |
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| DC73601 |
TTA-Q6 |
TTA-Q6 is a potent, selective T-type Ca2+ channel antagonist with IC50 of 14 nM and 590 nM in FLIPR depolarized assaay and FLIPR hyperpolarized assay, respectively. |
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| DC73602 |
DRAinh-A270 |
DRAinh-A270 is a small-molecule, selective inhibitor of intestinal anion exchanger SLC26A3 (DRA), inhibits SLC26A3-mediated chloride/bicarbonate exchange with IC50 of 35 nM and oxalate/chloride exchange with IC50 of 60 nM. |
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| DC73603 |
OV350
Featured
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OV350 (OV-350) is a potent, selective and direct K+-Cl- cotransporter KCC2 agonist with EC50 of 261.4 nM, with no effect on KCC2 plasma membrane accumulation and phosphorylation. |
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| 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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