4BPPNit is a small molecule significantly augmented glycosylation of α-dystroglycan, in part through upregulation of LARGE1 glycosyltransferase gene expression.

SKF-34288 (3-Mercaptopicolinic acid) hydrochloride is an orally active phosphoenolpyruvate carboxykinase (PEPCK, PCK) inhibitor with Ki of 2-9 uM, an inhibitor of gluconeogenesis.

2-TCPA is a potent, specific inhibitor of carbamoyl-phosphate synthetase, aspartate transcarbamoylase, and dihydroorotase (CAD), suppresses SARS-CoV-2 replication in Caco-2 cells with IC50 of 2.36 uM.

2,5-pyridinedicarboxylic acid is a highly selective D-dopachrome tautomerase (D-DT, MIF2) inhibitor with Ki of 17.2 uM, 79-fold selectivity over MIF, effectively blocks the D-DT-induced activation of CD74.

(S)-IBD3540 is a potent, gut-restricted and orally active small molecule glutamate carboxypeptidase II (GCPII) inhibitor with IC50 of 4 nM, demonstrates anti-colitis activity in both acute and chronic mouse colitis models.

(R)-HTS-3 is a small-molecule inhibitor of LPCAT3, an integral membrane acyltransferase in the Lands cycle responsible for generating C20:4 phospholipids.

GRL018-21 is a highly selective, potent, and non-covalent GRK5 inhibitor with IC50 of 10 nM, >100,000-fold selectivity over GRK2.

JNJ-3790339 is a potent and selective inhibitor of diacylglycerol kinase α (DGKα), demonstrates similar cytotoxicity in GBM and melanoma cells as ritanserin.

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.

BMS-332 (BMS332) is a potent, selective dual DGKα/ζ inhibitor with IC50 of 9/8 nM respectively.

SMP-114 (Rimacalib) is a potent, specific and orally available CaMKII inhibitor with potential for treatment of rheumatoid arthritis.

CC-8977 is a hgihly potent, selective inhibitor of calcium/calmodulin-dependent kinase kinase II (CaMKK2) with binding IC50 of 7 nM.

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.

NPT200-11 is an orally bioavailable and brain penetrating alpha-synuclein (ASYN) misfolding and aggregation inhibitor.

MeSC-04 is a potent α-Syn amyloid formation inhibitor, reduces the number and size of amyloid fibrils in vitro.

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.

CNB-001 is a pyrazole derivative of curcumin with neuroprotective properties, inhibits extracellular Aβ toxicity in hippocampal neurons with EC50 of 400 nM.

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.

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.

BMS-336 is a potent, selective, orally active RORγt (RORC2) inverse agonist with EC50 of 39 nM in RORγt reporter assays.

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.

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.

LG101506 (LG1506) is a potent, selective and orally active RXR modulator with Ki of 2.6 nM.

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.

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.

CD666 is a potent, selective RARgamma (RARγ) agonist.

AGN 196996 (IRX6696) is a potent selective RARα antagonist with Ki of 2 nM, shows little to no activity against RARβ and RARγ.

A small molecule inhibitor of progesterone receptor membrane component 1 (PGRMC1) that alters the spectroscopic properties of the PGRMC1-heme complex.

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.

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.