DC21288 |
MK-8617
Featured
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A potent, orally active pan-inhibitor of HIF prolyl hydroxylase (HIF-PHD) with IC50 of 1.0,1.0, and 14 nM for HIF-PHD1, 2, and 3, respectively. |
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DC22849 |
DSM 74 |
A potent, orally active PfDHODH inhibitor (IC50=0.3 uM) with antimalarial activity. |
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DC22704 |
SN79 |
A potent, orally active sigma receptor antaognist with Ki of 27 and 7 nM for σ1 and σ2, respectively. |
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DC22601 |
BMS-433796 |
A potent, orally active γ-secretase inhibitor with cell IC50 of 0.3 nM. |
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DC22853 |
IDN-7314 |
A potent, orally active, and irreversible pan-Caspase protease inhibitor with IC50 of <0.08 to 7 nM for inhibition of activated caspase 3, 6 and 8. |
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DC11893 |
Firibastat |
A potent, orally active, centrally acting aminopeptidase inhibitor, the prodrug of the specific and selective aminopeptidase A inhibitor EC33. |
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DC11629 |
NK1-IN-9 |
A potent, orally active, dual NK1 receptor antagonist (IC50=0.5 nM) and SERT inhibitor (IC50=5.2 nM). |
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DC11855 |
CHR 2863 |
A potent, orally available hydrophobic aminopeptidase inhibitor that structurally mimics the aminopeptidase inhibitor Tostedostat.. |
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DC20807 |
Gemopatrilat |
A potent, orally available, dual ACE-neutral endopeptidase (vasopeptidase) inhibitor with IC50 of 12 and 63 nM, respectively. |
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DC21396 |
Marizomib
Featured
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A potent, orally bioactive 20S proteasome inhibitor with IC50 of 1.3 nM (inhibition of proteasomal chymotrypsin-like proteolytic activity). |
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DC22598 |
Rislenemdaz |
A potent, orally bioavailable brain‐penetrant, NR2B-selective NMDA receptor (GluN2B) antagonist with Ki and IC 50 of 8.1 nM and 3.6 nM respectively, with no off-target activity. |
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DC23970 |
SCH-563705 |
A potent, orally bioavailable dual CXCR2/CXCR1 receptor antagonist with IC50 of 1.3 nM and 7.3 nM, respectively. |
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DC11518 |
Cavosonstat
Featured
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Cavosonstat is a potent, orally bioavailable inhibitor of S-nitrosoglutathione reductase (GSNOR) and CFTR modulator. |
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DC21541 |
PSI-421 |
A potent, orally bioavailable P-selectin inhibitor with improved pharmacokinetic properties and oral efficacy in models of vascular injury.. |
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DC24192 |
Dasatinib hydrochloride |
A potent, orally bioavailable, dual Src/Abl kinase inhibitor with IC50 of 0.5, 0.4, 0.5 and <1 nM for Src, Lck, Yes and Bcr-Abl, respectively. |
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DC11695 |
AT-IAP |
A potent, orally bioavailable, dual XIAP/cIAP1 inhibitor with EC50 of 5.1/0.32 nM, respectively. |
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DC11697 |
AM-1638 |
A potent, orally bioavailable, full agonist of GPR40/FFA1 with EC50 of 0.16 uM. |
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DC11860 |
FV-162 |
A potent, orally bioavailable, irreversible proteasome inhibitor with potent antimyeloma activity (IC50<60 nM). |
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DC21631 |
MK-8242 |
A potent, orally bioavailable, small-molecule inhibitor of HDM2/p53 protein-protein interaction. |
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DC11959 |
PD 184161
Featured
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A potent, orally-active MEK1/2 inhibitor with IC50 of 10-100 nM. |
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DC11731 |
Ruzasvir |
A potent, pan-genotype HCV NS5A inhibitor with replicon EC90 of 0.003, 0.016, 0.067, 0.036, 0.007, and 0.007 nM for GT1a, GT1a L31V, GT1a Y93H, GT2b, GT3a, and Gt4a, respectively.. |
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DC21560 |
RC-3095
Featured
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RC-3095 is a gastrin-releasing peptide receptor antagonist, synergizes with gemcitabine to inhibit the growth of human pancreatic cancer CFPAC-1 in vitro and in vivo. RC-3095 inhibit the growth of human glioblastomas in vitro and in vivo. RC3095 inhibits tumor growth and decrease the levels and mRNA expression of epidermal growth factor receptors in H-69 small cell lung carcinoma.R,BRS-1) antagonist. |
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DC23935 |
CH-5450 |
A potent, peptide-inhibitor of human chymase with Ki of 1 nM. |
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DC22580 |
SCH-1473759 hydrochloride |
A potent, picomolar, dual inhibitor of Aurora A and B with IC50 of 0.02 and 0.03 nM, respectively. |
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DC22581 |
SCH-1473759 |
A potent, picomolar, dual inhibitor of Aurora A and B with IC50 of 0.02 and 0.03 nM, respectively. |
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DC11794 |
GNF-351
Featured
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GNF-351 is a potent, pure aryl hydrocarbon receptor (AHR) antagonist (IC50=62 nM) devoid of partial agonist potential; antagonizes agonist and SAhRM-mediated suppression of SAA1, inhibit both DRE-dependent and -independent activity; decreases migration and invasion of HNSCC cells and prevents benzo[a]pyrene-mediated induction of the chemotherapy efflux protein ABCG2. |
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DC21334 |
MN-25 |
A potent, reasonably selective agonist of peripheral cannabinoid receptor with Ki of 11 nM for CB2, 22-fold selectivity over the psychoactive CB1 receptors (Ki=245 nM).. |
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DC21377 |
NESS-040C5 |
A potent, reasonably selective cannabinoid CB2 agonist with Ki of 0.4 nM, 25-fold selectivity over CB1 receptor.. |
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DC11717 |
PD-321852 |
A potent, reasonably selective Chk1 inhibitor with cell IC50 of 5 nM. |
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DC12016 |
NB 001 |
A potent, relatively selective and orally active adenylyl cyclase 1 (AC1) inhibitor with IC50 of 10 uM (cAMP production inhibition). |
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