DC22758 |
SI-113 |
A potent, specific inhibitor of the SGK1 kinase activity, induces autophagy, apoptosis and ER stress in cancer cells. |
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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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DC20998 |
ES 936 |
A potent, specific mechanism-based human NAD(P)H: quinone oxidoreductase 1 (NQO1) inhibitor that demonstrates efficient inactivation of NQO1 at 100 nM in in cellular systems. |
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DC22823 |
Tariquidar methanesulfonate hydrate |
A potent, specific P-gp inhibitor with Kd of 5.1 nM. |
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DC21849 |
YU-101 |
A potent, specific proteasome β5 subunit inhibitor with IC50 of 0.26 uM, 7.3 and 17.3-fold selectivity over β2i and β1i subunit, respecitvely.. |
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DC26068 |
BMS-753 |
A potent, specific RARα agonist with Ki of 2 nM, displays no significant effects on RARγ in reporter based assays.. |
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DC22661 |
AB1 |
A potent, specific S1P2 receptor (Edg-5) antagonist with IC50 of 3 nM, with no agonistic or antagonistic activities on other S1PRs. |
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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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DC22864 |
KSP-IA |
A potent, specific, allosteric and cell-active inhibitor of KSP with IC50 of 11 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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DC21318 |
ML 171 |
A potent, specific, cell-active NADPH oxidase1 (Nox1) inhibitor that strongly blocks ROS generation in HT29 cells with IC50 of 0.129 uM. |
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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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DC21110 |
HCI-2389 |
A potent, specific, irreversible NIMA-related Kinase 2 (NEK2) inhibitor with IC50 of 16.65 nM. |
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DC11977 |
SX-517 |
A potent, specific, noncompetitive dual CXCR1 and CXCR2 antagonist with IC50 of 38 nM (vs. CXCL1) and 36 nM (vs. CXCL8), respectively. |
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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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DC11716 |
XL-844 |
A potent, specific, orally available, ATP‑competitive inhibitor of Chk1 and Chk2 with Ki of 2.2 nM and 0.07 nM, respectively. |
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DC11766 |
UbcH5c-IN-6d |
A potent, specific, orally bioactive small-molecule inhibitor of ubiquitin-conjugating enzyme UbcH5c with Kd of 283 nM. |
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DC22550 |
TAK-220 |
A potent, specific, orally bioavailable CCR5 antagonist that blocks the binding of MIP-1α to CCR5 with IC50 of 1.4 nM. |
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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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DC22539 |
Pasireotide L-aspartate salt |
A potent, stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (pKi=8.2/9.0/9.1/<7.0/9.9 for sst1/2/3/4/5, respectively). |
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DC22746 |
TROX-1 |
A potent, state-dependent blocker of Cav2 channels that preferentially inhibits potassium-triggered calcium influx through recombinant Cav2.2 under depolarized conditions with IC50 of 0.27 uM, compared with hyperpolarized conditions (IC50>20 uM). |
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DC23782 |
4-Br-BnIm |
A potent, subtype-selective Grp94 inhibitor with Kd of 0.96 uM, 13-fold selectivity over Hsp90α. |
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DC23519 |
PF-06462894 |
A potent, subtype-selective mGluR5 negative allosteric modulator with Ki of 6.1 nM. |
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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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DC11621 |
eIF4A3-IN-1q |
A potent, subtype-selective, orally available eIF4A3 inhibitor with IC50 of 0.14 uM. |
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DC11972 |
PNU 96415E |
A potential antipsychotic agent that binds selectively to D4 and 5-HT2A receptors with Ki of 3.0 and 5.8 nM, respectively. |
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DC22923 |
HXJ 42 |
A PP1 analog that has greater selectivity and potency for Zap-70(AS) over wild-type Zap-70, as assessed by Erk and Lat phosphorylation, as well as by proliferative responses of mature CD4+ cells. |
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DC22471 |
Pantoprazole sodium hydrate |
A proton pump inhibitor that inhibits gastric acid secretion. |
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DC23928 |
Esomeprazole magnesium salt |
A proton pump inhibitor that reduces stomach acid secretion by inhibition of the H+/K+-ATPase in the parietal cells. |
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