DC7991 |
8-Chloro-11-(4-methyl-1-piperazinyl)-5H-dibenzo[b,e](1,4)diazepine N-oxide
Featured
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Clozapine N-oxide is a major metabolite of Clozapine noted to decrease SR-2A (5-HT2 serotonin receptor) density in vitro. |
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DC12714 |
CLP-290
Featured
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CLP290 (CLP-290) is an orally acirtve small molecule K+-Cl- cotransporter isotype 2 (KCC2) activator, the carbamate prodrug of CLP257; In vivo co-treatment with morphine and oral CLP290 prevented membrane KCC2 downregulation in SDH neurons. Concurrently, co-treatment with CLP290 significantly mitigated MIH and acute administration of CLP257 in established MIH restored normal nociceptive behavior. |
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DC9797 |
18-[4-(2,2-Difluoro-3-aza-1-azonia-2-boranuidatricyclo[7.3.0.03,7]dodeca-1(12),4,6,8,10-pentaen-8-yl)phenyl]octadecyl-[2-(trimethylazaniumyl)ethoxy]phosphinate
Featured
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CLR1501 is a synthetic analogs of the tumor-targeting agent alkylphosphocholine (APC), which is specifically attracted to cancer cells. |
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DC10795 |
CM-272
Featured
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CM-272 is a first-in-class reversible dual small molecule inhibitor against G9a and DNMTs in hematological malignancies. |
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DC7605 |
CM346(Afobazole)
Featured
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CM-346 increased the power of the low-frequency θ-rhythm (4.8–5.8 Hz) and the dominant activity peak (6.0–7.2 Hz) and decreased the spectral power in the 19–20 Hz band. |
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DC21530 |
CMP-5
Featured
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CMP-5 (PRMT5-IN-5) is a first-in-class, small-molecule inhibitor that specifically targets protein arginine methyltransferase 5 (PRMT5), an enzyme involved in epigenetic regulation and cellular signaling. PRMT5 catalyzes the symmetric dimethylation of arginine residues on histones and other proteins, playing a critical role in gene expression, cell proliferation, and survival. CMP-5 has shown remarkable specificity in blocking Epstein-Barr virus (EBV)-driven B-lymphocyte transformation and survival, while sparing normal B cells, making it a promising therapeutic candidate for EBV-associated cancers and other PRMT5-dependent diseases. |
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DC9803 |
CMP8
Featured
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CMP8 is a high-affinity ligand that binds only to mutant ERLBD. |
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DC22512 |
CMPDA
Featured
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CMPDA is a potent positive allosteric modulator of GluR2 receptors with EC50 of 45.4 and 63.4 nM at GluR2i and GluR2o respectively, in a calcium influx screening assays. |
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DC7761 |
Brincidofovir (CMX-001)
Featured
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CMX001 (Brincidofovir; HDP-CDV) was developed as an orally active, lipophilic form of cidofovir (CDV); has enhanced activity in vitro and in vivo compared to CDV against certain herpesviruses, adenoviruses and orthopoxviruses.IC50 Value: 5.5 nM (EC50, in PDA at 7 dpi) [3]Target: anti-CMVCMX001 is currently in Phase II clinical studies for development as a therapeutic agent for human CMV, adenovirus and BK virus infections, as well as, for adverse events following smallpox vaccinations.in vitro: In PDA at 7 dpi, the CMX001 50% effective concentration (EC50) was 5.55 nM, the 50% cytotoxic concentration (CC50) was 184.6 nM, and the 50% selectivity index (SI50) was 33.3. The EC90 was 19.7 nM, the CC90 was 5,054 nM, and the SI90 was 256.1. In COS-7 cells, JCV replication was faster and the EC50 and EC90 were 18- and 37-fold higher than those in PDA, i.e., 0.1 μM and 0.74 μM (CC50, 0.67 μM; SI50, 6.7; CC90, 12.2 μM; SI90, 16.5) at 5 dpi [3].in vivo: CMX001 and CDV are equally efficacious at protecting mice from mortality following high ectromelia virus doses (10,000 x LD(50)) introduced by the intra-nasal route or small particle aerosol. Using CMX001 at a 10mg/kg dose followed by 2.5mg/kg doses every other-day for 14 days provided solid protection against mortality and weight loss following an intra-nasal challenge of (100-200) x LD(50) of ectromelia virus [1]. When CMX001 was administered orally to mice infected with HSV-1, mortality was reduced significantly (p≤0.001) with all three dose levels when treatments were initiated 24 h post viral inoculation. When treatments were started 48 h post viral inoculation, 5 and 2.5 mg/kg significantly reduced mortality (p≤ 0.001). If treatments were delayed until 72 h post viral inoculation, CMX001 did not reduce mortality or increase the mean day to death. When mice were infected intranasally with HSV-1 and treatments initiated 24 h post viral inoculation using CMX001 at 5 mg/kg or ACV at 100 mg/kg, virus replication in target organs was reduced by both CMX001 and ACV when compared to vehicle treated mice [2]. Toxicity: Diarrhea was the most common adverse event in patients receiving CMX001 at doses of 200 mg weekly or higher and was dose-limiting at 200 mg twice weekly. Myelosuppression and nephrotoxicity were not observed [4]. |
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DC12476 |
CN427
Featured
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CN427 (CN-427) is novel BRD4 (BD1, 2) inhibitor with IC50 of 66 nM, MV4-11 viability IC50 of 1.1 uM.. |
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DC10752 |
CNDAC HCl
Featured
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CNDAC (DFP-10917; TAS-109) is an orally available deoxycytosine nucleoside analog with potential antineoplastic activity. |
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DC9799 |
CNDAC
Featured
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CNDAC is the active component of sapacitabine. |
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DC10671 |
CNQX disodium salt
Featured
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CNQX is a potent AMPA/kainate receptor antagonist. Also antagonist at glycine modulatory site on NMDA receptor complex. |
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DC10670 |
CNQX
Featured
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CNQX is a potent AMPA/kainate receptor antagonist. Also antagonist at glycine modulatory site on NMDA receptor complex. |
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DC23180 |
CNV1014802(Raxatrigine)
Featured
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CNV1014802 (GSK-1014802, Raxatrigine, Vixotrigine, BIIB074) is a potent, selective Nav1.7 sodium channel blocker, shows analgesic effects and potential in the treatment of cognitive symptoms of schizophrenia in vivo. |
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DC8095 |
Raxatrigine hydrochloride
Featured
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CNV1014802(GSK-1014802) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor. |
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DC7105 |
CNX-2006
Featured
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CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR. |
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DC7161 |
CNX-774
Featured
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CNX-774 is a potent, selective, and orally available small molecule inhibitor of Btk (IC50< 1 nM) that forms a ligand-directed covalent bond with Cys-481, a non-conserved amino acid within the active site of the enzyme. |
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DC8651 |
CO-1686 hydrobromide
Featured
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CO-1686 hydrobromide is a novel, irreversible and orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M (IC50=21 nM). |
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DC7106 |
Rociletinib (CO-1686)
Featured
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CO-1686 is a novel, irreversible and orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M(IC50=21 nM). |
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DC2046 |
Cobicistat (GS-9350)
Featured
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Cobicistat (GS-9350) is a potent and selective inhibitor of CYP3A with IC50 of 30-285 nM. |
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DC8863 |
Coelenterazine
Featured
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Coelenterazine is a luminescent enzyme substrate, used for monitoring reporter genes in BRET, ELISA and HTS techniques. |
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DC10336 |
Coenzyme Q9
Featured
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Coenzyme Q9, a nine isoprenyl group-containing member of the ubiquinone family, is a normal constituent of human plasma. |
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DC11955 |
Takeda compound 101
Featured
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Compound 101 (GRK2 inhibitor 101, Takeda compound 101, Cmpd101) is a novel membrane-permeable, small-molecule inhibitor of GRK2 and GRK3. |
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DC2085 |
Compound 401
Featured
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Compound 401 is a cell-permeable pyrimido-isoquinolinone compound that acts as a potent, reversible, and ATP-competitive inhibitor of DNA-PK (IC50 = 280 nM) with ~19-fold selectivity over FRAP (mTOR) (IC50 = 5.3 µM). |
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DC8340 |
myo-Inositol,1,2-anhydro-
Featured
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Conduritol B Epoxide (CBE) is a specific covalent inhibitor of β-glucosidase which results in the accumulation of glucocerebroside. |
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DCAPI1091 |
Conivaptan hydrochloride
Featured
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Conivaptan(YM 087) is a non-peptide inhibitor of antidiuretic hormone (vasopressin receptor antagonist) with Ki values of 0.48 and 3.04 nM for rat liver V1A receptor and rat kidney V2 receptor respectively. |
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DC8477 |
VER-49009
Featured
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Consistent with inhibition of Hsp90, VER-49009 induces the expression of Hsp27 and Hsp72 while reducing the client proteins C-RAF, B-RAF, survivin, and PRMT5, causing cell cycle arrest and apoptosis. |
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DC10776 |
Cordycepin
Featured
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Cordycepin is an adenosine analogue, which is readily phosphorylated to its mono-, di-, and triphosphate intracellularly. It has a very potent anti-cancer, anti-oxidant and anti-inflammatory activities. |
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DC12098 |
Corin
Featured
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Corin is a dual inhibitor of histone lysine specific demethylase (LSD1) and histone deacetylase (HDAC), with a Ki(inact) of 110 nM for LSD1 and an IC50 of 147 nM for HDAC1. |
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