| DC65238 |
compound 53
Featured
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”Compound 53” (University of Texas Southwestern Medical Center) is a stimulator of interferon (IFN) genes (STING) agonist. |
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| DC65239 |
TXA6101
Featured
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TXA6101 is an FtsZ inhibitor that is associated with potent activity against clinical isolates of methicillin-resistant Staphylococcus aureus (MRSA) that are resistant to current standard-of-care antibiotics. |
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| DC65240 |
Compound 4e
Featured
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“compound 4e” (Chiesi Farmaceutici) is an inhaled p38α/β mitogen-activated protein kinase (MAPK) inhibitor being developed for lung inflammatory diseases. |
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| DC65241 |
MAGLi 432
Featured
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MAGLi 432 is a novel, reversible monoacylglycerol lipase (MAGL) inhibitor. |
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| DC60456 |
HHS-166
Featured
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HHS-166 shows dose-dependent inhibition of arsenite-induced stress granule (SG) formation, and liganded G3BP1 Y40 in the NTF2 dimerization domain of this essential nucleating protein for SG regulation. |
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| DC60457 |
AHL-030
Featured
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AHL-030 is a potent and selective EDC3-targeted ligands. AHL-030 is also an stress granules (SGs) enhancer and results in a 2-fold increase in SGs per arsenite-treated cell. |
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| DC65242 |
MK-0159
Featured
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MK-0159 is a CD38 enzymatic inhibitor. Mice treated with MK-0159 show strong protection from myocardial damage upon cardiac I/R injury compared to those treated with NAD+ precursors (nicotinamide riboside) or another CD38 inhibitor. |
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| DC65243 |
lunresertib（RP-6306）
Featured
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RP-6306 is a selective inhibitor of PKMYT1 (Protein Kinase Membrane-Associated Tyrosine/Threonine 1), a key regulator of cell cycle progression. It was identified from patent WO2021195781A1 as compound 182. PKMYT1 is part of the DNA damage response pathway and plays a role in controlling the G2/M checkpoint, particularly in cells with disrupted cell cycle regulation, such as cancer cells. By inhibiting PKMYT1, RP-6306 can induce mitotic catastrophe and cell death in cancer cells, especially those with CCNE1 amplification or other dependencies on the G2/M checkpoint. |
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| DC65244 |
Dalzanemdor
Featured
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Dalzanemdor (SAGE-718) is a N-methyl-D-aspartate (NMDA) receptor positive allosteric modulator. |
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| DC65245 |
BI-4142
Featured
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BI-4142 is a potent, highly selective and orally active HER2 inhibitor with an IC50= 5 nM. BI-4142 showed efficacy against HER2 exon 20 insertion-driven tumors, while preserving EGFR wt signaling. |
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| DC65246 |
GST-HG131
Featured
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GST-HG131 is a specific inbihitor of hepatitis B virus (HBV) surface antigen, belongs to dihydrobenzopyridooxazepine (DBP) series. GST-HG131 exhibits excellent and specific HBV antigens inhibition with EC50 of 28.2 nM (HBsAg) and 16.0 nM (HBeAg), respectively, but also it is safety for animal. |
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| DC65247 |
AZD-1656
Featured
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AZD-1656 is a glucokinase (GK) activator potentially for the treatment of type 2 diabetes and obesity. |
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| DC65248 |
JNJ-64264681
Featured
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JNJ-64264681 is a covalent, irreversible BTK inhibitor with potent whole blood activity and exceptional kinome selectivity. JNJ-64264681 demonstrated excellent oral efficacy in both cancer and autoimmune models with sustained in vivo target coverage amenable to once daily dosing and has advanced into human clinical studies to investigate safety and pharmacokinetics. |
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| DC65249 |
AN15368
Featured
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AN15368 (AN 15368) is a small molecule prodrug activated by parasite carboxypeptidases to yield a compound that targets the messenger RNA processing pathway in Trypanosoma cruzi (T. cruzi), exhibits potent in vitro activity against T. |
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| DC60334 |
Sirpiglenastat (Synonyms: DRP-104)
Featured
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Sirpiglenastat (DRP-104) is a broad acting glutamine antagonist. Sirpiglenastat has anticancer effects by directly targeting tumor metabolism and simultaneously inducing a potent antitumor immune response. |
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| DC65251 |
ENT-01
Featured
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ENT-01 shows promise in the treatment of constipation in those with Parkinson's disease (PD) by preventing or reducing the formation of αS aggregates that form in enteric neurons. ENT-01 has undergone Phase 2b clinical trials to evaluate the safety and efficacy of the orally administered drug for the alleviation of constipation in those with PD. |
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| DC65252 |
compound 27
Featured
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compound 27, is a potent (13 nM) CNS-penetrant compound that reduces very long chain fatty acid (VLCFA) levels in the CNS, which are believed to be pathological in the rare disease adrenoleukodystrophy (ALD). The starting point came from an HTS on compounds from an internal collection. |
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| DC65253 |
compound 14d
Featured
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“Compound 14d” (Shionogi & Co.) is a highly potent, dose-dependent adenosine monophosphate activated protein kinase (AMPK) activator being investigated for its blood-glucose-lowering effects. |
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| DC65254 |
BI685509
Featured
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BI685509 is a soluble guanylate cyclase (sGC) activator taken orally, with potential to treat diabetic and kidney diseases. In both rat and human platelets, BI685509 was found to restore/enhance cGMP, but had no effect on the functionality of nitric oxide pathways. BI685509 is currently undergoing phase 2 trials for the treatment of diabetic nephropathy, with the aim of improving kidney function. |
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| DC65255 |
DN-1289
Featured
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DN-1289 is a potent and selective dual DLK/LZK inhibitor. DN1289 demonstrated excellent in vivo plasma half-life across species and is anticipated to freely penetrate the central nervous system with no brain impairment based on in vivo rodent pharmacokinetic studies and human in vitro transporter data. Proximal target engagement and disease relevant pathway biomarkers were also favorably regulated in an in vivo model of amyotrophic lateral sclerosis. |
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| DC65256 |
compound 6
Featured
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“Compound 6” (Novartis) is a first-in-class YAP-TEAD protein-protein inhibitor. The TEAD transcription factor and its coactivator YAP and WWTR1/TAZ of the Hippo pathway are responsible for directly regulating the expression of genes involved in cell proliferation and organ size. |
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| DC65257 |
compound 29
Featured
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Overcoming FGFR mutation resistance and FGFR1-mediated hyperphosphatemia toxicity through isoform-selective FGFR2/3 inhibition. “Compound 29” is an ATP-competitive fibroblast growth factor receptor (FGFR) 2/3 inhibitor with subnanomolar potency. |
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| DC60458 |
BI-3231
Featured
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BI-3231 is a novel potent and selective HSD17B13 inhibitor with IC50 of 1 nM and Ki of 0.7 nM, respectively. BI-3231 is a valuable chemical probe to further elucidate the biological function of HSD17B13. |
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| DC60459 |
OICR-8268
Featured
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OICR-8268 is a small molecule ligands that target DCAF1 and shows the highest affinity for binding to the DCAF1 WDR domain with SPR KD of 38 nM. OICR-8268 is an excellent tool compound to enable the development of next-generation DCAF1 ligands toward cancer therapeutics. |
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| DC65258 |
PUM00199
Featured
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PUM00199, also known as PARP10-IN-3, is a selective mono‐ADP‐ribosyltransferase PARP10 inhibitor with an IC50 of 480 nM for human PARP10. |
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| DC65259 |
KR-32568
Featured
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KR-32568 is an inhibitor of the sodium-hydrogen exchanger isoform-1 (NHE-1; IC50 = 230 nM). It restores cardiac contractile function ex vivo in an isolated ischemic rat heart model when used at a concentration of 10 μM. |
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| DC65260 |
TCS-46b
Featured
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TCS 46b is an orally active, subtype-selective GluN1A/GluN2B NMDA receptor antagonist |
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| DC65261 |
SBS probe
Featured
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SBS is a useful probe and tool molecule for detecting amyloid deposits in systemic amyloidosis in vitro and in vivo. SBS can be used for detecting amyloid fibrils in autopsy and biopsy samples from patients with localized amyloidosis, such as familial prion disease, and systemic amyloidosis, such as familial amyloidotic polyneuropathy, amyloid A (AA) amyloidosis, light chain (AL) amyloidosis, and dialysis-related amyloidosis. |
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| DC60460 |
SJ3149
Featured
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SJ3149 is a uniquely potent and selective CK1α degrader with DC50 of 3.7 nM. SJ3149 shows high activity across a range of acute leukemia (AL) cell lines derived from different hematologic neoplasms, such as B-cell and T-cell acute lymphoblastic leukemia. SJ3149 activity shows a strong correlation with wild-type TP53 expression.SJ3149 (SJ-3149) is uniquely potent and selective CK1α degrader with DC50 of 3.7 nM and Dmax 95% in MOLM-13 cells, potently inhibits the viability of MOLM-13 cells with IC50 of 13 nM.
SJ 3149 shows a broad antiproliferative profile on a panel of AML and ALL cell lines with IC50 values in a single digit nanomolar range, and even sub-nanomolar activity.
SJ-3149 also potently inhibited the viability of multiple cell lines derived from solid tumors, including breast, soft tissue, and tumors of the male and female reproductive system, with several cell lines being inhibited more potently than MOLM-13.
SJ3149 also inhibits several TP53-altered cell lines, such as BT-20 and KU812. |
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| DC60461 |
UCL-TRO-1938
Featured
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UCL-TRO-1938 is a small-molecule activator of the PI3Kα isoform with EC50 of 60 μM. UCL-TRO-1938 activats PI3Kα but not PI3Kβ or PI3Kδ and effectively boosts endogenous protective and regenerative signalling. |
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