WAY-622024(Compound 5j) is a GPCR GPR109b (HM74) agonist, with a pEC50 value of 6.51. GPCR agonist-2 can be used for research of lipid disorders.

Dersimelagon, also known as MT-7117 and WHO 10832, is a novel, orally-administered, small molecule, selective melanocortin-1 receptor (MC1R) agonist that increases skin melanin without sun exposure and is being developed to increase light tolerance in EPP/XLP patients. Dersimelagon significantly boosted sunlight tolerance in patients with erythropoietic protoporphyria in a multicenter, phase 2, randomized trial.

GSK3008348 is an Integrin alphaV inhibitor.

SB-423562 is a short-acting calcium-sensing receptor (CaR) antagonist.

A nontoxic heat shock protein (HSP) coinducer and potentiator of the heat shock response.

Periplocin is a cardiotonic steroid isolated from Periploca forrestii. Periplocin promotes tumor cell apoptosis and inhibits tumor growth. Periplocin has the potential to facilitate wound healing through the activation of Src/ERK and PI3K/Akt pathways mediated by Na/K-ATPase.

ZN-c3 is an orally active, highly potent and selective Wee1 inhibitor (IC50=3.9 nM). ZN-c3 can be used for the research of cancer.

Bufalin inhibits steroid receptor coactivator 1 (SRC-1) and SRC-3 at doses as low as 5 nM, promotes the degradation of SRC-3 protein, and inhibits cancer cell growth both in vitro and in vivo.

(+)-Penbutolol is a β-adrenoceptor antagonist, with an IC50 of 0.74 μM. (+)-Penbutolol is an optical isomer of l-penbutolol with Na+ channel-blocking action.

ALS-22335 is an anti-virus compound.

UDP-GlcNAz disodium is a substrate for UDP-GlcNAc:polypeptidyltransferase. UDP-GlcNAz serves as a sugar donor for the process catalyzed by the OGT enzyme and labels proteins through this process.

AT-527(Bemnifosbuvir hemisulfate), a hemisulfate salt of AT-511, a guanosine nucleotide prodrug, is a potent and orally active HCV viral replication inhibitor. AT-527 is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC90=0.47 μM). Bemnifosbuvir hemisulfate has pangenotypic antiviral activity[1][2][3].Bemnifosbuvir hemisulfate has pan-genotypic antiviral activities that inhibits HCV genotype 1a (HCV GT1a), HCV GT1b, HCV GT2a, HCV GT3a, HCV GT4a, and HCV GT5a replication with EC50 values of 12.8 nM, 12.5 nM, 9.2 nM, 10.3 nM, 14.7 nM, and 28.5 nM, respectively[1]. In normal human airway epithelial cells, the concentration of Bemnifosbuvir hemisulfate required to inhibit replication of SARS-CoV-2 by EC90 is 0.47 μM, very similar to its EC90 against HCoV-229E, HCoV-OC43 and SARS-CoV in Huh-7 cells[2].When given orally to rats (500 mg/kg) and monkeys (30 mg/kg, 100 mg/kg or 300 mg/kg), Bemnifosbuvir hemisulfate preferentially delivers high levels of AT-9010 in the liver in vivo[1].

Misoprostol acid is an active metabolite of Misoprostol. Misoprostol is a synthetic analogue of prostaglandin E1 (PGE1), extensively absorbed, and undergoes rapid de-esterification to Misoprostol acid in the gastrointestinal tract after oral administration. Misoprostol can be used for non-steroidal anti-inflammatory drug-induced (NSAID) gastric ulcers. Misoprostol is an oral agent used to induce labor.

Trabectedin (Ecteinascidin-743 or ET-743) is a novel antitumour agent of marine origin with potent antitumour activity both in vitro and in vivo.

Zuranolone(SAGE-217, CS-2797) is an orally active and potent neuroactive steroid and positive allosteric modulator of the GABAA receptor, with EC50s of 296 nM for α1β2γ2 receptor.

Ritonavir is an inhibitor of HIV protease used to treat HIV infection and AIDS,showed potent activity against COVID-19(SARS-COV-2) .

Luteolin 7-O-glucuronide could inhibit Matrix Metalloproteinases (MMP) activities, with IC50s of 17.63, 7.99, 11.42, 12.85, 0.03 μM for MMP-1, MMP-3, MMP-8, MMP-9, MMP-13, respectively.

VAL-083 is a bi-functional alkylating agent, with potential antineoplastic activity. Upon administration, VAL-083 crosses the blood brain barrier (BBB) and appears to be selective for tumor cells. This agent alkylates and crosslinks DNA which ultimately leads to a reduction in cancer cell proliferation. In addition, VAL-083 does not show cross-resistance to other conventional chemotherapeutic agents and has a long half-life in the brain.

Zanamivir is an influenza viral neuraminidase inhibitor with IC50 values of 0.95 nM and 2.7 nM for influenza A and B, respectively.

Azidamfenicol is a broad-spectrum chloramphenicol-like antibiotic that is active against Gram-negative and Gram-positive bacteria.1 It inhibits ribosomal peptidyltransferase (Ki = 22 µM).2

SR59230A is a potent, selective, and blood-brain barrier penetrating β3-adrenergic receptor antagonist with IC50s of 40, 408, and 648 nM for β3, β1, and β2 receptors, respectively.

Diquafosol tetrasodium is a P2Y2 receptor agonist that stimulates fluid and mucin secretion on the ocular surface, as a topical treatment of dry eye disease.

UDP-GlcNAc Disodium Salt (UDP-α-D-N-Acetylglucosamine Disodium Salt) is a donor substrate of O-GlcNAc transferase (OGT).

MK-8719 is a highly potent and selective OGA inhibitor (EC50 = 52.7 nM) which is a Potential Treatment for Tauopathies. MK-8719 showed excellent CNS penetration that has been advanced to first-in-human phase I clinical trials.

Salidroside, a phenylpropanoid glycoside isolated from Rhodiola rosea, has been reported to have a broad spectrum of pharmacological properties.

Scopine hydrochloride (6,7-Epoxytropine hydrochloride) is the metabolite of anisodine, which is a α1-adrenergic receptor agonist and used in the treatment of acute circulatory shock.

Heparin Lithium salt is an anticoagulant which binds reversibly to antithrombin III (ATIII).

Inecalcitol (TX 522), a unique vitamin D3 analog, is an orally active vitamin D receptor (VDR) agonist. Inecalcitol can induce cell apoptosis and has potent anticancer activities[3.

CHAPS is a zwitterionic surfactant that decreases the sequence specificity of the nucleosome.,nucleosome [1]()

A VHL ligand for PROTAC..