| DC57090 |
MIPS-521
Featured
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MIPS521 is a positive allosteric modulator of the adenosine A1 receptor. |
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| DC60119 |
YQ128
Featured
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YQ128 is a potent and selective second-generation NLRP3 (NOD-like receptor P3) inflammasome inhibitor with an IC50 of 0.30 ± 0.01 μM. Further studies from in vitro and in vivo models confirmed its selective inhibition on the NLRP3 inflammasome and its brain penetration. Furthermore, pharmacokinetic studies in rats at 20 mg/kg indicated extensive systemic clearance and tissue distribution, leading to a half-life of 6.6 h. |
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| DC60120 |
QQN05022(Dot1L-IN-4)
Featured
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QQN05022, also known as Dot1L-IN-4 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor. This molecule was first reported in ACS Medicinal Chemistry Letters (2019), 10(12), 1655-1660. This product has no formal name at the moment. For the convenience of communication, a temporal code name was therefore proposed according to MedKoo Chemical Nomenclature. |
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| DC60121 |
NVP-BHG712 isomer
Featured
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NVP-BHG712 isomer is a regioisomer of NVP-BHG712, which shows conserved non-bonded binding to EPHA2 and EPHB4. BHG-712, is a EphB4 kinase inhibitor and BCR-ABL inhibitor. NVP-BHG712 inhibits EphB4 kinase activity in the low nanomolar range in cellular assays showed high selectivity for targeting the EphB4 kinase when profiled against other kinases in biochemical as well as in cell based assays. |
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| DC60122 |
SC-10914
Featured
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SC10914 is a highly potent PARP inhibitor (PARP1 IC50 = 7.87 nM) with potent anti-proliferative activity against human BRCA deficient tumor cells (MDA-MB-436, BRCA1 deficient, IC50 = 4.03 nM, Capan-1 BRCA2 deficient, IC50 = 11.66 nM) and PTEN deficient tumor cells (HGC-27,PTEN deficient, IC50 = 0.35 μM). SC10914 showed potent anti-tumor activity in BRCA1/2 mutant tumor models and better pharmacokinetics profile has the potential to be selected as the clinical candidate for the treatment of treatment of BRCA1/2 deficient cancers. |
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| DC60123 |
N-desethyl Amodiaquine HCl
Featured
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N-desethyl Amodiaquine is a primary metabolite of the antimalarial compound aminodiaquine, produced by the action of cytochrome P450 isoform 2C8. N-desethyl Amodiaquine is highly active against P. falciparum and can synergize with amodiaquine. |
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| DC57082 |
MC-MMAE
Featured
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Mc-MMAE is a protective group (maleimidocaproyl)-conjugated monomethyl auristatin E (MMAE), which is a potent tubulin inhibitor. Mc-MMAE is a drug-linker conjugate for ADC. |
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| DC57088 |
SU0268
Featured
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SU0268 is a potent and selective OGG1 inhibitor. DNA glycosylases involved in the first step of the DNA base excision repair pathway are promising targets in cancer therapy. There is evidence that reduction of their activities may enhance cell killing in malignant tumors. |
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| DC57110 |
MAT2A inhibitor-2
Featured
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MAT2A inhibitor 2 is a methionine adenosyltransferase 2A (MAT2A) inhibitor. |
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| DC60124 |
nor-NOHA HCl
Featured
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nor-NOHA, also known as N-Hydroxy-nor-L-Arginine, is an Arginase inhibitor. nor-NOHA induces apoptosis in leukemic cells specifically under hypoxic conditions but CRISPR/Cas9 excludes arginase 2 (ARG2) as the functional target. Nor-NOHA can induce cell apoptosis and inhibit the ability of invasion and migration of HepG2 cells by inhibiting Arg1, which is related with the increase of iNOS expression and the high concentration of NO. |
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| DC46818 |
ACT-451840
Featured
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ACT-451840 is an orally active, potent and low-toxicity compound, showing activity against sensitive and resistant plasmodium falciparum strains. ACT-451840 targets all asexual blood stages of the parasite, has a rapid onset of action. ACT-451840 behaves in a way similar to artemisinin derivatives, with very rapid onset of action and elimination of parasite. ACT-451840 can be used for the research of malarial. |
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| DC46833 |
Pulrodemstat
Featured
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Pulrodemstat (CC-90011) is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. Pulrodemstat is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. Pulrodemstat induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity. |
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| DC46834 |
Menin-MLL inhibitor 20,MRN73473
Featured
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Menin-MLL inhibitor 20 is an irreversible menin-MLL interaction inhibitor with antitumor activities (WO2020142557A1, compound 6). |
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| DC46835 |
Ziftomenib
Featured
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Ziftomenib is a menin-MLL interaction inhibitor with antitumor activities (WO2017161028A1, compound 151). |
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| DC46840 |
Mesdopetam
Featured
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Mesdopetam (IRL790) is an orally active and low toxicity dopamine D3 receptor antagonist. Mesdopetam can be used for the research of Parkinson's disease (PD). |
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| DC46844 |
Emraclidine
Featured
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Emraclidine is a muscarinic M4 receptor positive allosteric modulator (WO2018002760, compound 11). Emraclidine can be used for the research of neurological diseases. |
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| DC46850 |
SB 218795
Featured
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SB 218795 is a potent and selective non-peptide NK3 receptor antagonist, with a Ki 13 nM for hNK3. SB 218795 shows about 90-fold and 7000-fold selectivity for hNK3 over hNK2 and hNK1, respectively. SB 218795 can inhibit NK3 receptor-mediated pupillary constriction of the rabbit. |
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| DC46854 |
BMY-14802 hydrochloride
Featured
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BMY-14802 hydrochloride (BMY-14802-1) is a selective and orally active sigma receptor antagonist with an IC50 of 112 nM. BMY-14802 hydrochloride is also a 5-HT1A and adrenergic α1 receptors agonist. BMY-14802 hydrochloride has antipsychotic effects. |
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| DC46864 |
Sivopixant
Featured
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Sivopixant (S-600918) is a potent and selective P2X3 receptor antagonist (P2X3 IC50=4.2 nM; P2X2/3 IC50=1100 nM). Sivopixant shows strong analgesic effect. |
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| DC46870 |
Enavogliflozin
Featured
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Enavogliflozin (DWP-16001), an antidiabetic agent, is an orally active, best-in-class and selective sodium-glucose cotransporter-2 (SGLT-2) inhibitor. |
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| DC46871 |
Vocacapsaicin
Featured
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Vocacapsaicin (CA-008), a prodrug of Capsaicin, is a first-in-class non-opioid TRPV1 agonist. Vocacapsaicin can provide meaningful and long-lasting pain relief. |
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| DC46872 |
Evifacotrep
Featured
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Evifacotrep, a short transient receptor potential channel 5 (TRPC5) antagonist (WO2020061162, compound 100), can be used for the research of neurological diseases. |
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| DC46877 |
Y134
Featured
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Y134 is a selective and orally active oestrogen receptor (ER) modulator (SERM), exhibits potent antagonist activity at ERα and ERβ. Y134 shows 121.1-fold selectivity for ERα (Ki=0.09 nM) over ERβ (Ki=11.31 nM). |
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| DC46880 |
Cedirogant
Featured
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Cedirogant (ABBV-157) is an orally active RORγt inverse agonist. Cedirogant can be used for psoriasis research. |
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| DC46883 |
Tinlarebant
Featured
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Tinlarebant (LBS-008) is an orally active non-retinoid RBP4 (retinol-binding protein 4) antagonist. Tinlarebant can be used for the research of the Stargardt disease. |
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| DC46887 |
CID1231538
Featured
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CID1231538, a benzothiazole analogue, is a potent GPR35 antagonist (IC50=0.55 μM). GPR35 is a G protein-coupled receptor (GPCR). |
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| DC46900 |
Utreloxastat
Featured
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Utreloxastat is a compound used for the research of the disorders including α-synucleinopathies, tauopathies, Amyotrophic lateral sclerosis (ALS), traumatic brain injury, and ischemic-reperfusion related injuries (patent WO2020081879A2, example A1). |
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| DC46910 |
Sebetralstat
Featured
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Sebetralstat is a plasma kallikrein inhibitor (WO2016083820). Sebetralstat can be used for the research of metabolic diseases. |
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| DC46916 |
2-bromo-Hexadecanoic acid
Featured
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2-Bromohexadecanoic acid (2-BP, 2-bromopalmitate) is a nonmetabolisable analogue of palmitate and acts as a palmitoylation inhibitor. 2-Bromohexadecanoic acid can directly and irreversibly inhibit the palmitoyltransferase activity of all DHHC (Asp-His-His-Cys) proteins. |
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| DC46917 |
[SER140]-PLP(139-151)
Featured
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[SER140]-PLP(139-151) is a polypeptide fragment of the lipid protein of myelin. |
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