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. |
|
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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DC11612 |
KBP-7018 hydrochloride |
A novel potent, multikinase inhibitor with IC50 of 10, 7.6 and 25 nM for c-Kit, RET and PDGFRβ, respectively. |
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DC11611 |
KBP-7018 |
A novel potent, multikinase inhibitor with IC50 of 10, 7.6 and 25 nM for c-Kit, RET and PDGFRβ, respectively. |
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DC11751 |
UHC1 |
A novel potent, non-agonist PPARγ ligand that blocks CDK5-mediated PPARγ phosphorylation, without the classical agonism. |
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DC11750 |
SR-1664
Featured
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SR-1664 is a novel potent, non-agonist PPARγ ligand that blocks the Cdk5-mediated phosphorylation in vitro (IC50=80 nM) and in vivo, without the classical agonism. |
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DC11968 |
OSU-03013 |
A novel potent, orally active 3-phosphoinositide-dependent kinase-1 (PDK-1) with IC50 of 2 uM. |
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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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DC11607 |
JTZ-951(Enarodustat)
Featured
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A novel potent, orally active HIF prolyl hydroxylase (PHD) inhibitor with IC50 of 0.22 uM for PHD2. |
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DC11608 |
JTZ-951 hydrochloride |
A novel potent, orally active HIF prolyl hydroxylase (PHD) inhibitor with IC50 of 0.22 uM for PHD2. |
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DC11546 |
Azeloprazole sodium |
A novel potent, orally active proton pump inhibitor that irreversibly inhibits H+,K+-ATPase activity with IC50 of 0.28 uM. |
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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. |
|
DC11599 |
PF-739 |
A novel potent, pan-AMPK activator with similar potency for all AMPK heterotrimers. |
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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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DC11610 |
AKS1-IN-19 |
A novel potent, selective and orally active ASK1 (MAP3K5) inhibitor with pIC50 of 8.3. |
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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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DC11696 |
CM-579 |
A novel potent, selective and reversible dual inhibitor of G9a/DNMTs with IC50 of 16 nM and 32 nM for G9a and DNMT1, respectively. |
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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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DC11953 |
MU 380 |
A novel potent, selective CHK1 inhibitor 2 nM, >80-fold selectivity over CHK2. |
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DC11982 |
CX815 |
A novel potent, selective CXCR2 inhibitor with IC50 of 0.4 nM. |
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DC11981 |
CX4152 |
A novel potent, selective CXCR2 inhibitor with IC50 of 7.6 nM. |
|
DC11827 |
9-ING-41
Featured
|
9-ING-41 is a potent glycogen synthase kinase-3 (GSK-3) inhibitor[1]. 9-ING-41 induces apoptosis and cell cycle arrest at prophase by targeting centrosomes and microtubule-bound GSK-3β. 9-ING-41 has anticancer activity[2]. |
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