GSK3787 is as a potent and selective antagonist of PPARδ with pIC50 of 6.6.

GSK2981278 is a highly potent and selective inverse agonist of retinoic acid receptor-related orphan receptor gamma (ROR gamma).

GSK2033 is a LXR antagonist with pIC50s of 7 and 7.4 for LXRα or LXRβ, respectively.

GSK-0660 is a selective PPARδ antagonist (IC50 values are 0.155, > 10 and ≥ 10 μM at PPARδ, PPARα and PPARγ respectively).

FG-4592 is an HIF αprolyl hydroxylase inhibitor, stabilizes HIF-2 and induces EPO production.

Fenretinide (4-HPR) is a synthetic retinoid deriverative. 4-HBR is shown to exhibit binding to the retinoic acid receptors (RAR) at concentrations necessary to induce cell death.

Ezetimibe (SCH 58235) is a potent cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.

EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ∼6 μM and a selective PPAR-gamma modulator

Desogestrel(Org-2969) is a third-generation 19-nortestosterone derivative progestogen; is contained in many oral contraceptive preparations, both combined (COCs) to ethinyl-estradiol (EE) or alone in a progestin-only pill (POP).

Daprodustat(GSK1278863) isa HIF-prolyl hydroxylase inhibitor.

Cilofexor (GS-9674, GS9674) is novel specific, non-steroidal farnesoid X receptor (FXR) agonist that reduces liver fibrosis and ameliorates portal hypertension in rat NASH models.

CH-223191 is a ligand-selective antagonist of the Ah (Dioxin) receptor.

C-DIM5 is a Nur77 agonist. Activation of the orphan nuclear receptor Nur77 by C-DIM5 is associated with decreased cancer cell survival,

CD437 is a synthetic retinoid that is an RARγ-selective agonist. It displays RARγ-dependent and -independent effects on differentiation and apoptosis.

Calcitriol is the most active metabolite of vitamin D and also a vitamin D receptor (VDR) agonist.

Balaglitazone (DRF-2593; NN-2344) is a novel partial agonist of PPAR-γ.

BMS687453 is a potent and selective peroxisome proliferator activated receptor (PPAR) α agonist, with an EC50 of 10 nM for human PPARα and ∼410-fold selectivity vs human PPARγ in PPAR-GAL4 transactivation assays.

Bazedoxifene is a selective estrogen receptor modulator (SERM) currently in development for osteoporosis prevention and treatment.

Bardoxolone methyl (also known as “RTA 402” and “CDDO-methyl ester”) is an orally-available first-in-class synthetic triterpenoid belonging to the antioxidant inflammation modulator (AIM) class.

AZD9496 is a potent and orally bioavailable selective estrogen receptor downregulator(Ki=0.7 nM) and antagonist.

AR7 is a retinoic acid receptor α (RARα) antagonist.

A PPARα agonist and an irreversible CPT-1 inhibitor.

AI-10-49 selectively binds to CBFβ-SMMHC and disrupts its binding to RUNX1.

A retinoic acid analog and selective RARα agonist

666-15 is a potent and selective CREB inhibitor with an IC50 of 81 nM.

4μ8C is a potent and selective IRE1 Rnase inhibitor with IC50 of 76 nM.

4EGI-1 is a competitive eIF4E/eIF4G interaction inhibitor by binding to eIF4E with KD of 25 μM.

2-methoxyestradiol (2ME2; NSC-659853) is a natural metabolite of estrogen that is known to inhibit HIF-1 alpha with an IC50 of 0.71 ± 0.11 μM for the inhibition of BPAEC migration.

10074-G5 is a c-Myc Max interaction inhibitor.

MeTC7 is a Vitamin-D receptor (VDR) antagonist. MeTC7 has potent VDR inhibition activity with an IC50 value of 2.9 μM. MeTC7 shows good antitumor effects.