DC21177 |
JNJ 39758979
Featured
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JNJ-39758979 is a selective, orally active, and high-affinity histamine H4 receptor antagonist with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 shows good anti-inflammatory and antipruritic activity. |
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DC24048 |
NVP-BKM120 hydrochloride
Featured
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A potent, selective, orally bioavailable inhibitor of class I PI3K isoforms with IC50 of 52 nM/166 nM/116 nM/262 nM for p110α/β/δ/γ, respectively. |
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DC23552 |
AS-2444697 HCl
Featured
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A potent, selective, orally bioavailable IRAK-4 inhibitor that potently inhibits human and rat IRAK-4 activity with subnanomolar order, >30-fold selectivity over IRAK-1. |
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DC21607 |
SB-649868
Featured
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SB-649868 is a potent and selective orally active orexin (OX) 1 and OX2 receptor antagonist (pKi =9.4 and 9.5 at the OX1 and OX2 receptor, respectively). |
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DC11748 |
LY2033298
Featured
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LY2033298 is a robust allosteric potentiator that is highly selective for the human M4 muscarinic acetylcholine receptor subtype. LY2033298 enhances inhibition by oxotremorine of light-induced phase shifts in hamster circadian activity rhythms. |
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DC11691 |
NSC95397
Featured
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A potent, selective, reversible Cdc25 dual specificity phosphatase inhibitor with Ki of 32/96/40 nM for Cdc25A/B/C, respectively. |
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DC11978 |
SB 265610
Featured
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SB-265610 is a selective, competitive, nonpeptide and allosteric CXCR2 antagonist. |
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DC21321 |
ML349
Featured
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A potent, specific acyl protein thioesterase 2 (APT-2, LYPLA2) inhibitor with IC50 of 144 nM and Ki of 120 nM, >20-fold selectivity over APT-1 and serine hydrolase enzyme family. |
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DC23074 |
Sivelestat
Featured
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A potent, specific and competitive inhibitor of human neutrophil elastase with IC50 of 44 nM. |
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DC23494 |
GRI 977143
Featured
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A potent, specific and nonlipid agonist of LPA2 receptor with EC50 of 3.3 uM, does not activate any of the other LPA GPCRs (>10 uM). |
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DC24105 |
MK-0591(Quiflapon )
Featured
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A potent, specific and orally active 5-Lipoxygenase-activating protein (FLAP) inhibitor with IC50 of 1.6 nM in FLAP binding assay. |
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DC21807 |
VU 0465350
Featured
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VU 0465350 is a potent, specific BMP receptor activin receptor-like kinase 3 (ALK3) antaognist with Ki of 92.3 nM; shows no activity for ALK2/4/5, also shows affinity for TGFBR2, VEGFR2 and AMPK; blocks SMAD phosphorylation in vitro and in vivo, and enhances liver regeneration after partial hepatectomy. |
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DC21794 |
VH 298
Featured
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A potent, specific cell-active VHL E3 ubiquitin ligase inhibitor that inhibits VHL/HIF-α interaction with Kd of 90 nM in ITC assays. |
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DC23985 |
Laduviglusib trihydrochloride
Featured
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Laduviglusib (CHIR-99021) trihydrochloride is a well-characterized small molecule inhibitor that specifically targets glycogen synthase kinase-3 alpha and beta (GSK-3α/β). It exhibits potent inhibitory activity with IC50 values of 10 nM for GSK-3α and 6.7 nM for GSK-3β. Importantly, it demonstrates high selectivity, being over 500-fold more selective for GSK-3 compared to other kinases such as CDC2 and ERK2, as well as a broad range of other protein kinases. |
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DC24007 |
R-1479
Featured
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A potent, specific inhibitor of HCV NS5B polymerase and HCV replication (IC50=1.28 uM, replicon assay). |
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DC11871 |
MMV019313
Featured
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MMV019313 (MMV 019313, MMV-019313) is a potent, specific malaria bifunctional farnesyl/geranylgeranyl diphosphate synthase (FPPS/GGPPS) inhibitor with IC50 of 330 nM; shows no activity against human FPPS or GGPPS (>200 uM); exhibits distinct modes of inhibition compared with bisphosphonates, inhibits P. falciparum growth with EC50 of 268 nM, overexpression and an S228T variant of PfFPPS/GGPPS confer resistance to MMV 019313. |
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DC24060 |
YM-155 hydrochloride
Featured
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A potent, specific survivin inhibitor that inhibits survivin promoter activity with IC50 of 0.54 nM. |
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DC22865 |
CK-0106023
Featured
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A potent, specific, allosteric inhibitor of KSP motor domain ATPase with Ki of 12 nM. |
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DC20890 |
ChoK-α inhibitor CK37
Featured
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A potent, specific, competitive inhibitor of choline kinase-α (Chok-α) by targeting the choline binding site; significantly increases LC3II expression in MCF-7 and MCF-7/TAM cells, increases the size and number of autophagosome, causes MCF-7 and MCF-7/TAM |
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DC26079 |
GW 803430
Featured
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A potent, specific, orally active melanin concentrating hormone receptor 1 (MCHR1) inhibitor with kI of 3.8 nM, >100-fold selectivity over a battery of GPCRs, ion channels and enzymes. |
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DC20928 |
CRT0066101
Featured
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A potent, specific, orally active pan-PKD (protein kinase D) inhibitor with biochemical IC50 of 1, 2.5 and 2 nM for PKD1, 2, and 3 respectively. |
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DC22540 |
Pasireotide
Featured
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Pasireotide (SOM230), a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide also exhibits antisecretory, antiproliferative, and proapoptotic activity.
At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Pasireotide acetate) usually boasts enhanced water solubility and stability. |
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DC22939 |
NS3861 fumarate
Featured
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NS3861 fumarate is an agonist of nicotinic acetylcholine receptors (nAChRs) and binds with high affinity to heteromeric α3β4 nAChR. The binding Ki values of 0.62, 25, 7.8, 55 nM for α3β4, α3β2, α4β4, α4β2, respectively. |
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DC23938 |
Esomeprazole sodium
Featured
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A proton pump inhibitor that reduces stomach acid secretion by inhibition of the H+/K+-ATPase in the parietal cells. |
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DC11545 |
IPAG
Featured
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IPAG is a prototypic selective inhibitor of sigma1 receptor that engages the unfolded protein response and induces autophagy in cancer cells. |
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DC23004 |
PSMA-ligand-1
Featured
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PSMA ligand-tubulysin compounds represent a cutting-edge approach to targeted cancer therapy, combining the precision of PSMA targeting with the potent cytotoxicity of tubulysin. This strategy holds significant promise for improving outcomes in prostate cancer and other PSMA-expressing malignancies, offering a highly specific and effective treatment option with reduced systemic toxicity. As research progresses, these compounds could play a transformative role in the field of oncology. |
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DC22348 |
Zalcitabine
Featured
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A pyrimidine analog reverse transcriptase inhibitor (NRTI) for the treatment of HIV/AIDS. |
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DC7054 |
AM580
Featured
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A retinoic acid analog and selective RARα agonist |
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DC23944 |
K-7174
Featured
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A selctive small molecule inhibitor of the transcription factor GATA-binding protein 2 (GATA2). |
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DC23943 |
K-7174 dihydrochloride
Featured
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K-7174 dihydrochloride is a selctive small molecule inhibitor of the transcription factor GATA-binding protein 2 (GATA2). |
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