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Fluzoparib chemical structureDC22228

Fluzoparib

Fluzoparib (SHR-3162) is a novel, potent and orally available inhibitor of PARP; potently inhibited PARP1 enzyme activity and induced DNA double-strand breaks, G2/M arrest and apoptosis in homologous recombination…

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PF-670462 chemical structureDC2086

PF-670462

PF-670462 is a potent and selective inhibitor of casein kinase (CK1ε and CK1δ), with IC50s of 7.7 nM and 14 nM, respectively.

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PBIT chemical structureDC7550

PBIT

PBIT is a specific inhibitor of the Jumonji AT-rich Interactive Domain 1(JARID1) enzymes. PBIT inhibits JARID1B (KDM5B or PLU1 ) histone demethylase an IC50 of about 3 μM . PBIT also inhibits JARID1A and JARID1C with…

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Fenoldopam (mesylate) chemical structureDC9424

Fenoldopam (mesylate)

Fenoldopam(SKF 82526) mesylate is a drug and synthetic benzazepine derivative which acts as a selective D1 receptor partial agonist.Target: D1 ReceptorFenoldopam is a selective dopamine-1 (DA1) agonist with…

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PKG drug G1 chemical structureDC10821

PKG drug G1

PKG drug G1 targets C42 of PKG Iα. PKG drug G1 can couple to vasodilation and blood pressure lowering by a C42 PKG Iα-independent mechanism.

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CID-2011756 chemical structureDC7253

CID-2011756

CID 2011756 is an ATP competitive PKD inhibitor, with an IC50 of 3.2 µM for PKD1 in cell free assay, and also shows cellular pan-PKD inhibitory activity against PKD2 and PKD3 (IC50, 0.6 and 0.7 µM, respectively). CID…

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VGX-1027(GIT 27) chemical structureDC7528

VGX-1027(GIT 27)

VGX-1027(GIT27) is an isoxazole compound that exhibits various immunomodulatory properties; reduce the secretion of IL-1beta, TNF-alpha and IL-10 from purified murine macrophages.Administration of VGX-1027 to NOD mice…

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AMG-510(Sotorasib) chemical structureDC22298

AMG-510(Sotorasib)

AMG-510 is a specific covalent inhibitor of K-RAS(G12C) with potential antineoplastic activity. Upon oral administration, KRAS mutant-targeting AMG-510 selectively targets the KRAS p.G12C mutant, at either the DNA, RNA…

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R1530 chemical structureDC7206

R1530

R1530 is the multikinase inhibitor with potential antiangiogenesis and antineoplastic activities.R1530 is also a mitosis-angiogenesis inhibitor (MAI) that inhibits multiple receptor tyrosine kinases involved in…

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ATB-346 chemical structureDC7365

ATB-346

ATB-346 is a novel hydrogen sulphide-releasing derivative of naproxen with markedly reduced toxicity. IC50 value: Target: COX-2 ATB-346 suppressed gastric prostaglandin E(2) synthesis as effectively as naproxen, but…

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Bromosporine chemical structureDC7543

Bromosporine

Bromosporine is a broad spectrum inhibitor for bromodomains with IC50 of 0.41 μM, 0.29 μM, 0.122 μM and 0.017 μM for BRD2, BRD4, BRD9 and CECR2, respectively.IC50 value: 0.41/0.29/0.122/0.017 uM (BRD2/BRD4/BRD9/CECR2)…

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ALG1001 (Risuteganib) chemical structureDC22211

ALG1001 (Risuteganib)

ALG1001 (Risuteganib, ALG-1001) is a first-in-class, RGD class oligopeptide that inhibits integrin receptors (αvβ3, αvβ5, and α5β1) associated with angiogenesis; ALG1001 inhibits an integrin-mediated pathway of the…

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GSK2636771 chemical structureDC6315

GSK2636771

GSK2636771 is a potent, selective and oral inhibitor of PI3Kβ with a Ki of 0.89 nM and an IC50 of 5.2 nM, showing 900-fold selectivity over p110α and p110γ, and 10-fold selectivity over p110δ isoforms.

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Y-320 chemical structureDC7535

Y-320

Y-320 is a new phenylpyrazoleanilide immunomodulator; inhibits IL-17 production by CD4 T cells stimulated with IL-15 with IC50 values of 20 to 60 nM.Y-320 inhibited IL-17 production by CD4 T cells stimulated with IL-15…

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PR-619 chemical structureDC7252

PR-619

PR-619 is a broad-range DUB inhibitor with EC50 of 3.93, 4.9, 6.86, 7.2, and 8.61 μM for USP4, USP8, USP7, USP2, and USP5, respectively.

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SSR-240612 HCl chemical structureDC10799

SSR-240612 HCl

SSR240612 is a potent, and orally active specific non-peptide bradykinin B1 receptor antagonist, with Kis of 0.48 nM and 0.73 nM for B1 kinin receptors of human fibroblast MRC5 and HEK cells expressing human B1…

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TAK-960 chemical structureDC7309

TAK-960

TAK-960 is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM at 10 μM ATP; TAK-960 also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM,…

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Emapunil(AC-5216) chemical structureDC7731

Emapunil(AC-5216)

Emapunil(AC-5216;XBD-173) is a translocator protein[TSPO (18 kDa)] ligand.IC50 value:Target: TSPO ligandXBD173 enhanced gamma-aminobutyric acid-mediated neurotransmission and counteracted induced panic attacks in…

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Rbin-1 chemical structureDC11468

Rbin-1

Rbin-1 is a potent, reversible, and specific chemical inhibitor of eukaryotic ribosome biogenesis. Rbin-1 inhibits the ATPase with GI50 of 136±7 nM.

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Lorcaserin Hydrochloride chemical structureDC8644

Lorcaserin Hydrochloride

Lorcaserin (APD-356, trade name upon approval Belviq,expected trade name during development, Lorqess is a weight-loss drug developed by Arena Pharmaceuticals. It has serotonergic properties and acts as an anorectic.…

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AC 55541 chemical structureDC7698

AC 55541

AC-55541 is a novel small-molecule protease-activated receptor 2(PAR2) agonist; activated PAR2 signaling in cellular proliferation assays, phosphatidylinositol hydrolysis assays, and Ca(2+) mobilization assays, with…

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MS436 chemical structureDC7620

MS436

MS436 is a new class of bromodomain inhibitor, exhibits potent affinity of an estimated Ki=30-50 nM for the BRD4 BrD1 and a 10-fold selectivity over the BrD2.

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(S)-PFI-2 HCl chemical structureDC8290

(S)-PFI-2 HCl

Negative control of (R)-PFI 2 hydrochloride. Exhibits 500-fold lower activity in a SETD7 enzymatic assay (IC50 = 1 μM) compared to the active enantiomer.

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SP-420 chemical structureDC8039

SP-420

SP-420 is a desferrithiocin analogue with iron-clearing efficiency with ICE value of 26.7; more potent than desferrithiocin.

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Fexinidazole chemical structureDC7811

Fexinidazole

Fexinidazole is an antiparasitic agent. It has activity against Trypanosoma cruzi, Tritrichomonas foetus, Trichomonas vaginalis, Entamoeba histolytica, Trypanosoma brucei, and Leishmania donovani. The biologically…

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kobe2602 chemical structureDC7444

kobe2602

kobe2602 is a novel and effective small-molecule compound inhibiting Ras–Raf interaction by SBDD; exhibits potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 149 ± 55…

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LY364947 chemical structureDC6305

LY364947

LY-364947 is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM, and exhibits 7-fold selectivity over TGFβR-II.

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GNF-5 chemical structureDC7420

GNF-5

GNF-5, an analogue of GNF-2 with improved pharmacokinetic properties, is a selective non-ATP competitive inhibitor of Bcr-Abl with an IC50 value of 0.22±0.1 uM (Wild type Abl).IC50 Value: 0.22±0.1 uM (Wild type Abl)…

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Lcl-161 chemical structureDC7184

Lcl-161

LCL161 is a IAP inhibitor which inhibits XIAP in HEK293 cell and cIAP1 in MDA-MB-231 cell with IC50s of 35 and 0.4 nM, respectively.

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Dapivirine chemical structureDC7395

Dapivirine

apivirine(TMC 120, TMC 120 R147681) is a NNRTI for HIV reverse transcriptase with IC50 of 24 nM, inhibits a broad panel of HIV-1 isolates from different classes, inclucing a wide range of NNRTI-resistant isolates.

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