DC22798 |
ADA-07 |
A novel potent TOPK inhibitor that effectively suppresses SUV-induced activation of MAPKs signal transduction resulting in reduced SUV-induced skin carcinogenesis. |
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DC21354 |
MT47-100
Featured
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MT47-100 is a novel compound that exhibits a unique dual functionality as both an allosteric activator and inhibitor of AMP-activated protein kinase (AMPK) complexes, depending on the isoform present. Specifically, MT47-100 acts as a direct activator of AMPK complexes containing the β1 isoform and as a direct inhibitor of AMPK complexes containing the β2 isoform. This isoform-specific modulation of AMPK activity makes MT47-100 a potentially valuable tool for studying the distinct physiological roles of β1- and β2-containing AMPK complexes, as well as a candidate for therapeutic applications targeting AMPK-related pathways. |
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DC23525 |
AAT-008 |
A novel potent, and selective prostaglandin EP4 receptor antagonist with binding IC50 of 2.4 nM. |
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DC22688 |
AZD 3676 |
A novel potent, combined serotonin 5-HT1A and 5-HT1B receptor antagonist with Ki of 0.13 and 2.4 nM in brain homogenates, respectively. |
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DC11986 |
OX03050 |
A novel potent, competitive squalene synthase inhibitor that upregulate the LDLR in mouse and human liver cell lines with EC50 of 26 nM. |
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DC20692 |
ASP 8477 |
A novel potent, highly selective fatty acid amide hydrolase (FAAH) inhibitor with IC50 of 0.99, 1.65 and 57.3 nM for human FAAH-1, FAAH-1 (P129T) and FAAH-2, respectively. |
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DC21507 |
PHA-408 |
A novel potent, highly selective, ATP-competitive IKK-2 inhibitor with IC50 of 40 nM, 350-fold selectivity over IKK-1. |
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DC23309 |
BCL6 inhibitor 8c |
A novel potent, in vivo-active BCL6 inhibitor with IC50 of 0.1 uM in ELISA assays. |
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DC21209 |
KW-2581 |
A novel potent, irreversible and orally active inhibitor of steroid sulfatase (STS) with IC50 of 13 nM in ZR-75-1 cells. |
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DC11769 |
MPO-IN-28
Featured
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A novel potent, irreversible Myeloperoxidase (MPO) inhibitor with IC50 of 44 nM. |
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DC21058 |
GNS-1481 |
A novel potent, irreversible, T790M mutant-selective inhibitor of mutant EGFR with IC50 of 6.2, 3.4 and 4.2 nM for L858R-T790M, T790M and Del19-T790M, respectively. |
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DC21059 |
GNS-1486 |
A novel potent, irreversible, T790M mutant-selective inhibitor of mutant EGFR with IC50 of 8.3, 4.2 and 4.3 nM for L858R-T790M, T790M and Del19-T790M, respectively. |
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DC24024 |
Z-360 |
A novel potent, orally active CCK-2/gastrin receptor antagonist with Ki of 0.47 nM. |
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DC21707 |
STX-681 |
A novel potent, orally active, dual-acting aromatase and steroid sulfatase (STS) inhibitor with ICI0 of 0.82 nM and 39 nM, respectively. |
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DC20806 |
BMS-852927 |
A novel potent, partial LXRβ-selective agonist (EC50=9 nM) with 20% LXRα and 88% LXRβ activity compared to a full pan agonist in transactivation assays. |
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DC22745 |
SLx-4090
Featured
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A novel potent, selective and orally active enterocytic microsomal triglyceride transfer protein (MTP) inhibitor that inhibits only MTP localized to enterocytes with IC50 of 6 nM. |
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DC21667 |
SMM-295 |
A novel potent, selective cannabinoid receptor 2 (CB2) agonist with Ki of 12 nM, >30-fold selectivity over CB1. |
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DC20841 |
BRD6989
Featured
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A novel potent, selective CDK8 inhibitor with IC50 of 0.5 uM against recombinant Cyclin C/CDK8 complex. |
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DC22940 |
SKF-32802 |
A novel potent, selective hERG potassium channel (Kv11.1) activator that induces a leftward shift in the voltage dependence of activation.. |
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DC21703 |
STAT5 inhibitor 17f
Featured
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A novel potent, selective inhibitor of phosphorylation and transcriptional activity of STAT5, but not STAT3, AKT, or Erk1/2 phosphorylation. |
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DC22938 |
ICA-027243
Featured
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A novel potent, selective KCNQ2/Q3 (Kv7.2/Kv7.3) potassium channel opener/activator with EC50 of 0.38 uM.. |
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DC22741 |
RY796 R-form |
A novel potent, selective Kv2 channel inhibitor that potently inhibits Kv2.1 and Kv2.2 with IC50 of 0.14 and 0.09 uM, respectively. |
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DC22744 |
RY796 racemate |
A novel potent, selective Kv2 channel inhibitor that potently inhibits Kv2.1 and Kv2.2 with IC50 of 0.14 and 0.09 uM, respectively. |
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DC22886 |
TASP 0433864 |
A novel potent, selective mGluR2 positive allosteric modulator with EC50 of 199 and 206 nM for human and rat mGlu2, respectively, without exerting agonist activity. |
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DC20441 |
MAO-B inhibitor 8f |
A novel potent, selective monoamine oxidase B (MAO-B) inhibitor with IC50 of 29-56 nM. |
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DC20467 |
mTOR inhibitor 10 |
A novel potent, selective mTOR inhibitor with biochemical IC50 of 21.7 nM for mTORC1, exhibits cellular potency against mTOR with IC50 of 5 nM. |
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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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