ZLN005 is a novel transcriptional regulator of peroxisome proliferator-activated receptor-γ coactivator-1α (PGC-1α).

RTA-408 is a synthetic triterpenoid that potently activates the antioxidative transcription factor Nrf2 and inhibits the proinflammatory transcription factor NF-κB.

SYP-5 is a novel HIF-1 inhibitor, suppresses tumor cells invasion and angiogenesis.

AZD9977 is a first-in-class, potent, selective, mineralocorticoid receptor (MR) modulator with IC50 of 0.37. 0.08 and 0.08 uM for human, mouse and rat MR, respectively.

Desidustat is an inhibitor of HIF hydroxylase.

Bigelovin, a sesquiterpene lactone isolated from Inula helianthus-aquatica, is a selective retinoid X receptor α agonist. Bigelovin suppresses tumor growth through inducing apoptosis and autophagy via the inhibition of mTOR pathway regulated by ROS generation.

Endoxifen (E-isomer hydrochloride) is a tamoxifen metabolite and potent Selective Estrogen Response Modifier (SERM).

FG-2216 is a potent HIF-prolyl hydroxylase inhibitor with IC50 of 3.9 uM for PDH2 enzyme; orally bioavailable and induced significant and reversible Epo induction in vivo.

GW 7647 is a potent PPARα agonist with 200-fold selectivity over PPARγ and PPARδ.

TMP778 (TMP-778) is a potent, selective RORγt inhibitor with IC50 of 7 nM in FRET assays and 63 nM in IL-17 promoter assays, with no inverse agonist activity.

IOX4 is a potent inhibitor of PHD2 (IC50 = 1.6 nM).

Endoxifen is a Estrogen receptor α (ERα) ligand; potent antiestrogen,an active metabolite of the cancer drug tamoxifen.

Doxercalciferol is a synthetic vitamin D2 analog, suppressing parathyroid synthesis and secretion, used to treat secondary hyperparathyroidism and metabolic bone disease.

JNJ-42041935 is a potent (pKi = 7.3-7.9), 2-oxoglutarate competitive, reversible, and selective inhibitor of PHD enzymes.

KG-501 is a small molecule inhibitor of Aldolase, Histochemical substrate for alkaline phosphatases.

KHS101 is a selective inducer of neuronal differentiation; induces neuronal differentiation in cultured hippocampal neural progenitor cells (NPCs) by interacting with TACC3 (EC50 ~1 μM).

L-165041 is a potent PPARδ agonist (Ki = 6 nM).

(rac)-PF-998425 is a potent, selective, nonsteroidal androgen receptor (AR) antagonist. (rac)-PF-998425 has IC50 values of 26 and 90 nM in the AR binding and cellular assays, respectively. (rac)-PF-998425 has the potential for the research of the androgenetic alopecia.

DS20362725 is an estrogen-related receptor α (ERRα) agonist. DS20362725 inhibits the binding between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM) with an IC50 value of 0.6 μM. DS20362725 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM).

DS45500853 is an estrogen-related receptor α (ERRα) agonist. DS45500853 inhibits the binding between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM) with an IC50 value of 0.80 μM. DS45500853 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM).

Enzalutamide D3 is a deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells.

FXR/TGR5 agonist 1 has agonist action on FXR and TGR5, and can be used for the treatment of fatty liver disease.

hFSH-β-(33-53) TFA, a thiol-containing peptide which corresponds to a second FSH receptor-binding domain, is a FSHR (follicle-stimulating hormone receptor) antagonist. hFSH-β-(33-53) TFA inhibits binding of FSH to receptor and is a partial agonist of estradiol synthesis in Sertoli cells.

SHR168442 is a modulator of retinoid-related orphan receptor gamma (RORγ) with an IC50 value of 0.035 μM.

LXR-623 is a novel Liver X Receptor modulator

15-Deoxy-Δ-12,14-prostaglandin J2 (15d-PGJ2) is a cyclopentenone prostaglandin and a metabolite of PGD2. 15-Deoxy-Δ-12,14-prostaglandin J2 is a selective PPARγ (EC50 of 2 µM) and a covalent PPARδ agonist. 15-Deoxy-Δ-12,14-prostaglandin J2 promotes efficient differentiation of C3H10T1/2 fibroblasts to adipocytes with an EC50 of 7 μM.

LY2955303 is a potent and selective RAR-gamma antagonist for the treatment of osteoarthritis pain.

MA-0204 is a potent, selective PPARδ modulator with good pharmacokinetic properties.

RORγt Inverse agonist 6 (compound 43) is a RORγt inverse agonist for the study of Th17-driven autoimmune diseases. RORγt Inverse agonist 6 (compound 43) suppresses IL-17A gene expression by IL-23 stimulation in vivo.

Keap1-Nrf2-IN-3 is a KEAP1:NRF2 protein−protein interaction inhibitor, and with a Kd value of 2.5 nM for KEAP1 protein.