| DC73377 |
AS408
Featured
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AS408 is a negative allosteric modulator of the β2-adrenergic receptor (β2AR) for both G-protein activation and arrestin recruitment (pKB=6.8, [35S]GTPγS binding assays), binds to a pocket formed by the membrane-facing surface of TM3 and TM5. |
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| DC73409 |
YM-344031
Featured
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YM-344031 is a potent, selective, brain-penetrable CCR3 antagonist with binding IC50 of 3.0 nM, inhibits ligand-induced Ca(2+) flux with IC50 of 5.4 nM. |
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| DC73421 |
ASP4345
Featured
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ASP4345 (ASP-4345) is a potent, selective positive allosteric modulator of the dopamine type 1 (D1) receptor that selectively binds to, and enhances the activity of, D1 receptors. |
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| DC73426 |
F17464
Featured
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F17464 is a dopamine D3 receptor preferential antagonist exhibiting high affinity for human dopamine receptor subtype 3 (hD3) (Ki=0.17 nM) and 5-HT1a (Ki=0.16 nM) and a >50 fold lower affinity for the human dopamine receptor subtype 2 short and long form (hD2s/l) (Ki=8.9 and 12.1 nM, respectively).
F17464 is a D3 receptor antagonist, 5-HT1a receptor partial agonist.
F17464 blocks ketamine induced morphological changes, an effect D3 receptor mediated, in human dopaminergic neurons. F17464 increases dopamine release in the rat prefrontal cortex and mouse lateral forebrain-dorsal striatum and seems to reduce the effect of MK801 on % c-fos mRNA medium expressing neurons in cortical and subcortical regions.
F17464 also rescues valproate induced impairment in a rat social interaction model of autism, with dose range 0.32-2.5 mg/kg i.p. in both rats and mice |
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| DC73453 |
ACT-1016-0707
Featured
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ACT-1016-0707 is a potent, selective, and orally active lysophosphatidic acid receptor subtype 1 receptor (LPA1 receptor, LPAR1) antagonist with IC50 of 3.1 nM, highly selective over LPAR2 or LPAR3. |
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| DC73463 |
CRN04894
Featured
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CRN04894 is a highly potent, selective, orally available melanocortin 2 receptor (MC2R antagonist) antagonist with Ki of 2.1 nM. |
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| DC73469 |
ML353
Featured
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ML353 (VU0478006) is a highly potent, selective, MPEP-site silent allosteric modulator of mGlu5 receptor with with sub-100 nM affinity. |
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| DC73482 |
CVN766
Featured
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CVN766 (CVN 766) is a potent, exquisitely selective orexin 1 receptor (OX1R) antagonist with IC50 of 8 nM, 1000-fold selective over OX2R. |
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| DC73504 |
JR1-157
Featured
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JR1-157 is a potent selective sigma 2 receptor (σ2R) ligand with Ki value of 47 nM, >10-fold selectivity over σ1R. |
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| DC73509 |
S6821
Featured
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S6821 (S 6821) is a potent and selective antagonist of the bitter taste receptor TAS2R8, exhibiting an IC50 value of 21 nM.
It demonstrates high selectivity across a panel of 16 TAS2Rs, effectively reduces the bitterness of coffee, and shows an excellent safety profile. |
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| DC73510 |
Org 274179-0
Featured
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Org 274179-0 is a highly potent, allosteric antagonist of the thyroid-stimulating hormone receptor (TSH receptor), inhibits bTSH-, hTSH- and M22-mediated CRE-luciferase transactivation in the CHO cell line. |
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| DC73526 |
DFV890
Featured
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DFV890 (IFM-2427) is apotent, selective and orally active inhibitor of NLRP3 inflammasome, directly binds to NLRP3 and locks the protein in an inactive conformation,prevents NLRP3 inflammasome assembly in response to sterile danger signals. |
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| DC73561 |
E104
Featured
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E014 is a potent, selective TLR7 agonist with EC50 of 69 nM in Ramos Blue reporter assays, >500-fold selective for TLR7 over TLR8. |
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| DC73563 |
E6742
Featured
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E6742 (E6742) is a potent, selective, dual TLR7/8 inhibitor with binding Kd of 1.7 uM/37 nM in ITC assays, respectively, inhibits TLR7/8 agonist CL097 induced reporter activation with IC50 values of 22, 68, and 3.0 nM for hTLR7, mTLR7, and hTLR8, respecti |
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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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| 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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| 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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| DC73624 |
FP802
Featured
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FP802 is a novel small molecule with significant neuroprotective properties, specifically designed to target and disrupt the TwinF interface within the NMDAR/TRPM4 death signaling complex. This unique mechanism allows FP802 to selectively eliminate extrasynaptic NMDAR (eNMDAR)-mediated toxicity, which is implicated in various neurodegenerative diseases, while preserving the essential physiological functions of synaptic NMDARs. This selectivity makes FP802 a promising therapeutic candidate for conditions involving excitotoxicity and neuronal cell death. |
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| DC73665 |
KCNQ2 activator Ebio1
Featured
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Ebio1 is a selective voltage-gated potassium channel KCNQ2 activator. Ebio1 activates KCNQ2 by generating an extended channel gate with greater conductance at a saturation voltage (+50 mV). |
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| DC73675 |
VU0546110
Featured
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VU0546110 (VU 0546110) is a potent, selective inhibitor of the sperm-specific potassium channel SLO3 with IC50 of 1.29 uM, impairs sperm function. |
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| DC73683 |
LTGO-33
Featured
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LTGO-33 is a potent, selective inhibitor of voltage-gated sodium channel NaV1.8 with IC50 of 44 nM (hNaV1.8), 600-fold selectivity against NaV1.1-NaV1.7 and NaV1.9. |
|
| DC73704 |
AD-5591
Featured
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AD-5591 (AD5591) is a potent, selective, new generation small molecule ALDH2 activator, has the improved biological activities and pharmacological properties compared to Alda-1.
AD-5591 (100 μM) significantly increases the enzymatic activity of recombinant WT and mutant human ALDH2 proteins.
AD-5591 is the active form of AD-9308. |
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| DC73705 |
AD-9308
Featured
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AD-9308 is a water-soluble, orally bioavailable, potent, and highly selective ALDH2 activator, AD-9308 is a valine ester prodrug of a potent and selective small molecule ALDH2 activator AD-5591. |
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| DC73741 |
MZ-101
Featured
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MZ-101 is a potent, selective inhibitor of glycogen synthase 1 (GYS1) with IC50 of 41 nM (human GYS1), with no inhibition against GYS2. |
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| DC73744 |
ADAM9i
Featured
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ADAM9i is a specific small molecule inhibitor of ADAM9 protein with binding KD of 5.9 uM and enzyme IC50 of 5.2 uM, promotes the selective degradation of KRAS and sensitizes pancreatic cancers to chemotherapy. |
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| DC73746 |
BAY-9835
Featured
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BAY-9835 is the first orally bioavailable ADAMTS7 inhibitor with IC50 of 6 nM, which is selective against a range of off-targets and metalloproteases except for ADAMTS12. |
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| DC73761 |
NAMPT activator (NAT)
Featured
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NAMPT activator (NAT) is a potent, small molecule activator of nicotinamide phosphoribosyltransferase (NAMPT) with ITC KD of 500 nM. |
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| DC73763 |
CC-11050
Featured
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Dovramilast (CC-11050) is a potent and orally active phosphodiesterase 4 (PDE4) inhibitor, CC-11050 is a promising candidate for host directed therapy of patients with pulmonary TB. |
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