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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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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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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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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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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DC21271 |
Volinanserin (MDL100907)
Featured
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A potent, selective 5-HT2A receptor antagonist with Ki of 0.36 nM, > 80-fold selectivity for 5-HT2A over other serotonergic receptors. |
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DC20851 |
BW-723C86
Featured
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A potent, selective 5-HT2B receptor agonist with pKi of 7.1, >10-fold selectivity over 5-HT2A, 5-HT2C, and other 5-HT subtypes. |
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DC23941 |
RU-24969
Featured
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A potent, selective agonist of 5-HT1A and 5-HT1B receptors, with preference for 5-HT1B. |
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DC20564 |
TBBz
Featured
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A potent, selective and ATP-competitive CK2 inhibitor with Ki of 0.5-1 uM. |
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DC20309 |
ANTISAUVAGINE-30
Featured
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A potent, selective and competitive corticotropin-releasing factor CRF2 receptor antagonist with Ki of 1.4 nM, 100-fold selectiivity over CRF1. |
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DC11755 |
L-732138
Featured
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A potent, selective and competitive NK1 receptor antagonist with IC50 of 2.3 nM. |
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DC21827 |
XE 991 dihydrochloride
Featured
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A potent, selective and orally active blocker of voltage-gated potassium channels Kv7 (KCNQ) that blocks KCNQ1, KCNQ2 and KCNQ2+KCNQ3 with Kd of 0.78, 0.7 and 0.6 uM, respectively. |
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DC23371 |
NI-42
Featured
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NI-42 is a potent, selective and orally active BRPF1 bromodomain inhibitor with IC50 of 7.9 nM, with excellent selectivity over nonclass IV BRDs; weakly inhibits BRPF2 (BRD1), BRPF3, BRD9 and BRD4 (BD1) with IC50 of 48, 260, 310 and 4500 nM respectively, and no activity for ATAD2A/2B (IC50>100 uM); shows a modest (GI50=1-10 uM) and selective inhibition of proliferation of certain cancer lines, particularly those lines exhibiting monocytic lineage differentiation; a novel, structurally orthogonal chemical probe for the BRPFs suitable for cellular and in vivo studies. |
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DC21689 |
SR 142948A
Featured
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A potent, selective and orally active neurotensin receptor antagonist with IC50 of 1.19 nM. |
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DC23207 |
JNJ-17203212
Featured
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A potent, selective and orally bioavailable TRPV1 receptor antagonist with IC50 of 65 nM and 102 nM for hTRPV1 and rTRPV1, respectively. |
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DC11511 |
A-485
Featured
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A potent, selective and, cell and in vivo active p300/CBP catalytic inhibitor with IC50 of 9.8/2.6 nM. |
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DC20602 |
5F 203
Featured
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A potent, selective antitumour agent through activation the aryl hydrocarbon receptor (AhR) pathway. |
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DC20658 |
AM1241
Featured
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A potent, selective cannabinoid receptor CB2 agonist with Ki of 7.1 nM, >80-fold selectivity over CB1 receptors in radioligand binding assay. |
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DC22917 |
SCH 79797 dihydrochloride
Featured
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A potent, selective competitive and nonpeptide PAR-1 antagonist with IC50 of 70 nM. |
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DC11866 |
AZD 3147
Featured
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A potent, selective dual mTORC1 and mTORC2 inhibitor with enzyme IC50 of 1.5 nM. |
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DC22747 |
AICP
Featured
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AICP is a highly potent and selective GluN2C-containing NMDA receptor agonist that specifically targets the glycine-binding site of these receptors. It exhibits an EC50 of 1.7 nM at GluN1/GluN2C NMDA receptors, making it a powerful tool for studying the functional roles of GluN2C-containing NMDA receptors in the central nervous system. |
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DC11617 |
PU-H54
Featured
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PU-H54 is potent, selective Grp94 inhibitor. |
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DC22946 |
ML-T531
Featured
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ML-T531 is a potent, selective hERG potassium channel (Kv11.1) activator with EC50 of 3.13 uM. |
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DC22966 |
ABH hydrochloride
Featured
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A potent, selective human Arginase inhibitor with Ki of 0.25 uM (pH=7.5), 8.5 nM (pH=9.5) for type II arginase. |
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DC11857 |
BAY-8040 (R)
Featured
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Bay-8040 is a potent, selective human neutrophil elastase (HNE) inhibitor with IC50 of 28 nM; displays no significant inhibition toward 68 other pharmacologically relevant targets (>10 uM), and a panel of related serine proteases; shows in vivo efficacy with regard to decreasing cardiac remodeling and amelioration of cardiac function in monocrotaline-induced rat model for pulmonary arterial hypertension. |
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DC11706 |
R-10015
Featured
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A potent, selective inhibitor of human LIMK1 with IC50 of 38 nM . |
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DC23189 |
CL-82198
Featured
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CL-82198 is a selective inhibitor of MMP-13. CL-82198 binds to the entire S1’ pocket of MMP-13, which is the basis for its selectivity towards MMP-13 and the lack of inhibitory activities against other MMPs. CL-82198 is a pharmacologic treatment for preventing osteoarthritis (OA) progression. |
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DC22625 |
Rolipram
Featured
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A potent, selective inhibitor of phosphodiesterases PDE4 with IC50 of 3 nM, 130 nM and 240 nM for PDE4A, PDE4B, and PDE4D, respectively. |
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DC11507 |
CLP257
Featured
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CLP257 (CLP-257) is a potent, selective K+-Cl- cotransporter KCC2 activator with EC50 of 616 nM; displays selectivity for KCC2 over other KCC family members, NKCC1 and GABAA receptors, and a panel of 55 other receptors; restores impaired Cl(-) transport i |
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DC11503 |
KDOAM-25
Featured
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A potent, selective KDM5 sub-family(JARID1) inhibitor with biochemical IC50 of 71/19/69/69 nM for KDM5A/B/C/D, respectively. |
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