| DC73844 |
4A7C-301 |
4A7C-301 is a potent, selective, brain-penetrant agonist of nuclear receptor Nurr1 with EC50 of 6.53 uM, binds to Nurr1 ligand binding domain (LBD) with IC50 of 50 nM. |
|
| DC73845 |
BRF110 |
BRF110 is a potent, selective, brain penetrant and vivo active agonist of Nurr1-RXRα heterodimers with EC50 of 900 nM. |
|
| DC73846 |
SA00025 |
SA00025 is a potent, specific and brain penetrant agonist of Nurr1 (NR4A2) with EC50 of 2.5 nM in HEK293 cells transfected with full length human Nurr1. |
|
| DC73847 |
XCT0135908 |
XCT0135908 (BRF001) is a highly selective activator of Nurr1-RXR heterodimers, stimulates dopamine (DA) neuron survival. |
|
| 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 |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| DC73853 |
AG-205 |
A small molecule inhibitor of progesterone receptor membrane component 1 (PGRMC1) that alters the spectroscopic properties of the PGRMC1-heme complex. |
|
| 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. |
|
| DC73855 |
BPA-B9
Featured
|
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. |
|
| DC73856 |
CD666 |
CD666 is a potent, selective RARgamma (RARγ) agonist. |
|
| 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. |
|
| 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. |
|
| DC73859 |
LG101506 |
LG101506 (LG1506) is a potent, selective and orally active RXR modulator with Ki of 2.6 nM. |
|
| 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. |
|
| 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. |
|
| DC73862 |
BMS-336 |
BMS-336 is a potent, selective, orally active RORγt (RORC2) inverse agonist with EC50 of 39 nM in RORγt reporter assays. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| DC73866 |
CS27109
Featured
|
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. |
|
| DC74561 |
AF-2112 |
AF-2112 is a small molecule inhibitor of TEAD, reduces the expression of CTGF, Cyr61, Axl and NF2, inhibits migration of human MDA-MB-231 breast cancer cells. |
|
| DC74562 |
LM98 |
LM98 (TEAD inhibitor LM98) is a flufenamic acid analogue, shows strong affinity to TEAD, inhibits its autopalmitoylation and reduces the YAP-TEAD transcriptional activity. |
|
| DC74563 |
mCMY020 |
mCMY020 is a potent, specific and covalent inhibitor of TEAD transcriptional activity with IC50 of 91.9-468.6 nM for TEAD1-4. |
|
| DC74564 |
MYF-03-69 |
MYF-03-69 is a selective, covalent, irreversible TEAD inhibitor, binds with TEAD palmitate pocket, disrupts YAP-TEAD association, suppresses TEAD transcriptional activity (IC50=45 nM) and inhibits cell growth of defective Hippo signaling. |
|
| DC74565 |
NSC682769 |
NSC682769 is a specific YAP-TEAD signaling inhibitor, blocks the association of the YAP and TEAD interaction interface, directly binds to YAP with Kd of 738 nM. |
|
| DC74566 |
PDHPS1 |
PDHPS1 is an endogenous stable peptide which is derived from the C-terminal (2090-2110) of NUMA1, inhibits the proliferation of ovarian cancer cells in vitro, regulates ovarian cancer development through targeting YAP1 signaling, binds to and interacts wi |
|
| DC74567 |
SWTX-143 |
SWTX-143 is a potent, irreversible and covalent YAP/TAZ-TEAD inhibitor with IC50 of 12 nM in luciferase reporter assays, binds to the palmitoylation pocket of all four TEAD isoforms, inhibits Hippo pathway-mutant cancer cells. |
|
