DC23862 |
MET inhibitor Compound 1 |
A novel potent, selective orally bioavailable MET tyrosine kinase inhibitor with IC50 of <1 nM and 12 nM for unphosphorylated and phosphorylaed MET, respectively. |
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DC22977 |
Lu AF-58027 |
A novel potent, selective PDE1 inhibitor with IC50 of 13/45/1.4 nM for PDE1A/B/C, respectively. |
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DC21458 |
(S)-PBMC |
A novel potent, selective TRPM8 antagonist with IC50 of 15.6 nM (hTRPM8). |
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DC20951 |
DFL 23448 |
A novel potent, selective TRPM8 channel antagonist with IC50 of 10 and 21 nM in hTRPM8 HEK293 cells activated by Cooling Agent 10 or cold. |
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DC21747 |
tBPC |
A novel potent, selective Y4R positive allosteric modulator (EC50=5.1 uM) that potentiates Y4R activation in G-protein signaling and arrestin3 recruitment experiments. |
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DC22700 |
DETQ |
A novel potent, selective, allosteric and orally active dopamine D1 receptor potentiator with Kb of 26 nM. |
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DC22857 |
Pyr-1 |
A novel potent, selective, cell permeable and ATP competitive LIMK inhibitor. |
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DC23672 |
Gemigliptin
Featured
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A novel potent, selective, competitive and orally active DPP4 inhibitor with potential for the treatment of type 2 diabetes. |
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DC20685 |
AS2795440 |
A novel potent, selective, oral PIKfyve inhibitor that selectively decreases c-Rel binding to gene promoters of IL-12p40 and IL-1β, regulates cytokine production through PIKfyve-c-Rel pathway ( IL-12p40 IC50=2 nM). |
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DC20782 |
BI 689648 |
A novel potent, selective, orally active aldosterone synthase inhibitor with IC50 of 2 nM, displays 150-fold selectivity over related cortisol synthase. |
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DC22673 |
SCH 486757 |
A novel potent, selective, orally active nociceptin/orphanin FQ peptide (NOP, ORL1) receptor agonist with Ki of 4.6 nM, with high selectiivity over classical opioid receptors. |
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DC21441 |
ONO-2952 |
A novel potent, selective, orally active translocator protein 18 kDa (TSPO/PBR) antagonist with Ki of 0.33-9.3 nM for both rat and human TSPO. |
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DC22740 |
RO 5126946 |
A novel potent, selective, orally bioavailable and brain-penetran α7nAChR positive allosteric modulator with EC50 of 60 nM. |
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DC20690 |
ASP 2905
Featured
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A novel potent, selective, orally bioavailable inhibitor of voltage-gated potassium channel KCNH3 with IC50 of 9.0 nM. |
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DC21522 |
Balixafortide(POL6326)
Featured
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Balixafortide(POL 6326) is a novel potent, selective, peptidic CXCR4 antagonist that interferes with the tumor-protective microenvironment and sensitizes tumor cells to chemotherapy. |
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DC22600 |
HI-TOPK-032
Featured
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A novel potent, specific TOPK inhibitor that has no effect on ERK1, JNK1, or p38 kinase activity. |
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DC23487 |
AS2575959 |
A novel potent, specific, orally available GPR40 agonist that influences glucose-dependent insulin secretion both in vitro pancreas β-cell-derived cells and in vivo. |
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DC23450 |
SAS-1121 |
A novel potent, subtype-selective sigma 2 receptor/PGRMC1 ligand with Ki of 16.2 nM, 574-fold selectivity over sigma 1 receptors.. |
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DC23465 |
DKR-1051 |
A novel potent, subtype-selective sigma 2 receptor/PGRMC1 ligand with Ki of 61 nM, 9-fold selectivity over sigma 1 receptors (Ki=556 nM). |
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DC22370 |
Meptyldinocap |
A novel powdery mildew (Erysiphe necator) fungicide that shows protectant and post-infective activities. . |
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DC22592 |
Amiselimod hydrochloride (MT-1303 hydrochloride)
Featured
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A novel prodrug S1P receptor modulator lacking S1P3 receptor agonism to avoid bradycardia associated with fingolimod and other S1P receptor modulators. |
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DC26112 |
SLMP53-1
Featured
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SLMP53-1 is a novel reactivator of wild-type and mutant p53, shows a p53-dependent anti-proliferative activity in human wt and mut p53R280K-expressing tumor cells. |
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DC25071 |
PDE6δ inhibitor 8 |
A novel selective small molecule inhibitor of PDE6δ/KRas interaction with Kd of 358 pM.. |
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DC23742 |
Rac1-IN-6 |
A novel selective small molecule Rac1 inhibitor that blocks Rac1-PAK1 complex formation with IC50 of 88±48 nM. |
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DC23749 |
Rac1-IN-1 |
A novel selective small molecule Rac1 inhibitor that blocks Rac1-PAK1 complex formation with IC50 of 95±21 nM. |
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DC21702 |
SC-99
Featured
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A novel selective STAT3 inhibitor that inhibits JAK2-STAT3 activation but has no effects on other transcription factors such as NF-κB, and kinases such as AKT, ERK, and c-Src. |
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DC22660 |
Tenovin-D3 |
A novel selective, small-molecule inhibitor of sirtuin SITR2 with IC50 of 21.8 uM. |
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DC22961 |
ITP-2 |
A novel small molecule activator of Kv 11.1 (hERG) channel (216% over control at 3 uM for hERG1a activation). |
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DC22982 |
Aldi-6 |
A novel small molecule ALDH inhibitor with IC50 of 600 nM, 800 nM and 1000 nM for ALDH1A1, ALDH2, and ALDH3A1, respectively. |
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DC20650 |
AKI603
Featured
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AKI-603 is a novel small molecule Aurora A kinase inhibitor with IC50 of 12.3 nM, also inhibits Aurora B kinase activity to a less extent; disrupts normal spindle structure, and induces cell-cycle arrest; t; suppresses stem cell properties in breast cancer cells, and also suppresses the expression of self-renewal genes (β-catenin, c-Myc, Sox2, and Oct4); reduces xenograft tumor growth after intragastric administration. |
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