DC73848 |
MBX-102 acid |
MBX-102 acid is the active form of JNJ39659100 (MBX-102), a selective partial PPAR-γ agonist with EC50 of 23.34 uM (hPPAR-γ), enhances insulin sensitivity in vitro in 3T3-L1 adipocytes, binds to the PPAR-γ LBD in a manner that is distinct from but overla |
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DC73849 |
MMT-160 |
MMT-160 is a novel selective peroxisome proliferator-activated receptor γ (PPARγ) antagonist with IC50 of 0.17 uM, covalently binds to the PPARγ ligand binding domain (LBD) via Cys285. |
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DC73850 |
SR10221 |
SR10221 is a potent, selective PPARγ inverse agonist with IC50 of 13 nM in biochemical peptide recruitment assays, represses downstream PPARγ target genes leading to growth inhibition in bladder cancer cell lines. |
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DC73851 |
FKK6 |
FKK6 (Felix Kopp Kortagere 6) is a specific human pregnane X receptor (hPXR) agonist with IC50 of 1.56 uM in a cell-free competitive hPXR TR-FRET-binding assays. |
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DC73852 |
SJPYT-318 |
SJPYT-318 is a highly selective pregnane X receptor (PXR) agonist, targets PXR ligand-binding domain (LBD), exhibits selectivity for PXR LBD over LXR LBDs for recruiting SRC-1. |
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DC73853 |
AG-205 |
A small molecule inhibitor of progesterone receptor membrane component 1 (PGRMC1) that alters the spectroscopic properties of the PGRMC1-heme complex. |
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DC73854 |
AGN196996 |
AGN 196996 (IRX6696) is a potent selective RARα antagonist with Ki of 2 nM, shows little to no activity against RARβ and RARγ. |
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DC73855 |
BPA-B9
Featured
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BPA-B9 (Bipyridine amide B9) is a small molecule RXRα-targeted anti-mitotic agent, binds to RXRα (Kd=39 nM) and selectively inhibits the p-RXRα/PLK1 interaction to induce mitotic arrest and catastrophe in cancer cells. |
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DC73856 |
CD666 |
CD666 is a potent, selective RARgamma (RARγ) agonist. |
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DC73857 |
E6060 |
E6060 is a potent, selective retinoic acid receptor subtype α (RAR-α) agonist with Ki of 0.2 nM, IC50 of 0.2 nM for RAR-α-mediated reporter transactivation assays. |
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DC73858 |
IRX4647 |
IRX4647 is a selective RARγ agonist, regulates T cell biology and reduces syngeneic tumor growth of immune checkpoint-resistant lung cancer cell line (344SQ) when combined with anti-PD-L1. |
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DC73859 |
LG101506 |
LG101506 (LG1506) is a potent, selective and orally active RXR modulator with Ki of 2.6 nM. |
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DC73860 |
XS-060 |
XS-060 is a small molecule RXRα-targeted anti-mitotic agent, binds to RXRα (Kd=1.3 uM) and selectively inhibits the p-RXRα/PLK1 interaction to induce mitotic arrest and catastrophe in cancer cells. |
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DC73861 |
STL1267 |
STL1267 is a specific, high affinity synthetic agonist of nuclear receptor REV-ERB with EC50 of 0.13 uM and Ki of 0.16 uM, binds directly to the ligand binding domain (LBD) of REV-ERB. |
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DC73862 |
BMS-336 |
BMS-336 is a potent, selective, orally active RORγt (RORC2) inverse agonist with EC50 of 39 nM in RORγt reporter assays. |
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DC73863 |
ODH-08 |
ODH-08 is a novel specific small molecule ligand and agonist of RORα with KD value of 8.4 um, shows potent antifibrotic effect. |
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DC73864 |
PCCR-1 |
PCCR-1 is a potent, specific RORγ inhibitor with binding IC50 of 34.45 nM and 778.1 nM for human and mouse RORγ, respectively, > 300-fold selectivity over other isoforms of ROR. |
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DC73865 |
W6134 |
W6134 (RORγ covalent inhibitor 29) is a first-in-class, potent and selective RORγ covalent inhibitor with IC50 of 0.21 uM, targets the Cys320 of RORγ. |
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DC73866 |
CS27109
Featured
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CS27109 is a potent, selective thyroid hormone receptor-β (THR-β) agonist with AC50 value of 1.98 uM, 12.6-fold selectivity over THR-α. |
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DC73867 |
EN171
Featured
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EN171 covalently targets both C38 and C96 on 14−3−3 to enhance 14−3−3 interactions with ERα, YAP, and TAZ, leading to impaired estrogen receptor and Hippo pathway transcriptional activity. |
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DC73868 |
CNB-001 |
CNB-001 is a pyrazole derivative of curcumin with neuroprotective properties, inhibits extracellular Aβ toxicity in hippocampal neurons with EC50 of 400 nM. |
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DC73869 |
DDQ |
DDQ is a small molecule inhibitor of binding sites of Amyloid beta (Aβ) and Drp1, reduces interaction between Aβ and Drp1, shows anti-aging effects. |
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DC73870 |
MeSC-04 |
MeSC-04 is a potent α-Syn amyloid formation inhibitor, reduces the number and size of amyloid fibrils in vitro. |
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DC73871 |
NPT200-11 |
NPT200-11 is an orally bioavailable and brain penetrating alpha-synuclein (ASYN) misfolding and aggregation inhibitor. |
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DC73872 |
SRI-42667 |
SRI-42667 is a selective small-molecule Tau-SH3 interaction inhibitor with IC50 of 0.91 uM (Tau-FynSH3 interaction), prevents amyloid-β toxicity and network hyperexcitability. |
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DC73873 |
CC-8977 |
CC-8977 is a hgihly potent, selective inhibitor of calcium/calmodulin-dependent kinase kinase II (CaMKK2) with binding IC50 of 7 nM. |
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DC73874 |
SMP-114 |
SMP-114 (Rimacalib) is a potent, specific and orally available CaMKII inhibitor with potential for treatment of rheumatoid arthritis. |
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DC73875 |
BMS-332 |
BMS-332 (BMS332) is a potent, selective dual DGKα/ζ inhibitor with IC50 of 9/8 nM respectively. |
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DC73876 |
BMS-684 |
BMS-684 (BMS684) is a potent, selective inhibitor of diacylglycerol kinase α(DGKα) with IC50 of 15 nM, weakly inhibist DGKβ and DGKγ, does not inhibit other DGK lipid kinases. |
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DC73877 |
JNJ-3790339 |
JNJ-3790339 is a potent and selective inhibitor of diacylglycerol kinase α (DGKα), demonstrates similar cytotoxicity in GBM and melanoma cells as ritanserin. |
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