Rasarfin is a novel dual Ras and ARF6 inhibitor. Rasarfin blocks agonist-mediated internalization of AT1R and other GPCRs. Rasarfin also potently inhibits agonist-induced ERK1/2 signaling by GPCRs, and MAPK and Akt signaling by EGFR, as well as prevents cancer cell proliferation. In silico modeling and in vitro studies reveal a unique binding modality of Rasarfin within the SOS-binding domain of Ras. Rasarfin is a novel dual Ras and ARF6 inhibitor. Rasarfin blocks agonist-mediated internalization of AT1R and other GPCRs. Rasarfin also potently inhibits agonist-induced ERK1/2 signaling by GPCRs, and MAPK and Akt signaling by EGFR, as well as prevents cancer cell proliferation. In silico modeling and in vitro studies reveal a unique binding modality of Rasarfin within the SOS-binding domain of Ras.

Supinoxin, also known as RX-5902, is orally bioavailable small molecule inhibitor of phosphorylated-p68 RNA helicase (P-p68), with potential anti-proliferative and antineoplastic activity. Upon oral administration, P-p68 inhibitor RX-5902 may both inhibit the activity of the anti-apoptotic B-cell lymphoma 2 (Bcl-2) protein and facilitate the induction of cyclin-dependent kinase inhibitor 1 (p21). This may prevent G2/M cell cycle progression and lead to growth inhibition in tumor cells. P-p68 is overexpressed in various types of solid tumors but absent in normal tissues, and plays a role in tumor progression and metastasis.

MKT-077 (FJ-776) is a highly water-soluble (>200 mg/ml) rhodacyanine dye that exhibits significant antitumor activity, binds to Hsp70 family member, mortalin (mot-2), and abrogates its interactions with p53.

GPR52-IN-43(CAY10786) is a novel GPR52 antagonist, reducing mHTT levels by targeting GPR52 and promoting survival of mouse primary striatal neurons, and also reducing HD-related phenotypes in HdhQ140.

Compound 101 (GRK2 inhibitor 101, Takeda compound 101, Cmpd101) is a novel membrane-permeable, small-molecule inhibitor of GRK2 and GRK3.

D-Luciferin sodium is heterocyclic light-emitting compound and natural ligand for luciferase used to detect cell activity. It requires ATP for its reaction, emitting a greenish-yellow luminescence at a peak wavelength of approximately 530 nm. The salt form of luciferin dissolves in water or other typical buffers.

M1001 is a novel allosteric agonist of hypoxia-inducible factor-2α subunit (hif-2α), significantly displacing pocket residue y281

ZZW-115 (ZZW115, ZZW 115) is a potent inhibitor of NUPR1 (Kd=2.1 uM), an intrinsically disordered protein (IDP) with an entirely disordered conformation.

Cell-permeable, irreversible inhibitor of caspase-3/CPP32; inhibits tumor cell apoptosis. Neuroprotective in rat hippocampus following seizures in vivo.

Z-IETD-FMK is a specific Caspase-8 inhibitor.

ICG amine, as a near-infrared fluorescent probe, binds to amino acid residues without condensing agents. ICG is a tricarbocyanine dye.

Ganaplacide (KAF156, GNF-156) is a novel antimalarial clinical candidate that shows blood schizonticidal activity with IC50 of 6-17.4 nM against P falciparum drug-sensitive and drug-resistant strains.

SKA-31 (Naphtho[1,2-d]thiazol-2-ylamine) is a potent activator of potassium channel with EC50 of 260 nM, 1.9 μM, 2.9 μM, and 2.9 μM for KCa3.1, KCa2.2, KCa2.1 and KCa2.3, respectively.

Alexamorelin is a synthetic growth hormone (GH) secretagogue.

GSK2837808A is a potent, selective lactate dehydrogenase A (LDHA) inhibitor (IC50 values are 1.9 and 14 nM for LDHA and LDHB respectively).

BI 671800 is a potent, oral prostaglandin D2 receptor (CRTH2) antagonist for treatment of asthma..

HCV-IN-30 (compound 48) is a HCV NS5A replication complex inhibitor, with IC50s of 901 and 102 nM for genotypes 1a and 1b replicons, respectively.

SPDB is a disulfide chemical linker for antibody-drug conjugates (ADCs)..

Opicapone(BIA 9-1067) is a long-acting, peripherally selective inhibitor of catechol-O-methyltransferase.

RTICBM-189 is a Urea derivative and a CB1 allosteric modulator. RTICBM-189 showed no activity at >50 protein targets and excellent brain permeation but relatively low metabolic stability in rat liver microsomes. Pharmacokinetic studies in rats confirmed the excellent brain exposure of 31 with a brain/plasma ratio Kp of 2.0. Importantly, intraperitoneal administration of RTICBM-189 significantly and selectively attenuated the reinstatement of the cocaine-seeking behavior in rats without affecting locomotion.

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.

GT 949 is a selective excitatory amino acid transporter-2 (EAAT2) positive allosteric modulator with an EC50 of 0.26 nM.

TAS4464 is a highly potent and selective inhibitor of NEDD8 (IC50 of 0.955 nM). TAS4464 selectively inhibited NAE relative to the other E1s UAE and SAE. TAS4464 treatment inhibited cullin neddylation and subsequently induced the accumulation of CRL substrates such as CDT1, p27, and phosphorylated IκBα in human cancer cell lines. TAS4464 showed greater inhibitory effects than those of the known NAE inhibitor MLN4924 both in enzyme assay and in cells.

Flibanserin is a novel multifunctional serotonin agonist and antagonist (MSAA) that improves sexual functioning in premenopausal women who suffer from reduced sexual interest and desire.

Etoricoxib is a new COX-2 selective inhibitor with anti-inflammatory, antipyretic, analgesic, and potential antineoplastic properties.

Dizocilpine, a potent anticonvulsant, is a selective and non-competitive NMDA receptor antagonist, with a Kd of 37.2 nM in rat brain membranes. Dizocilpine acts by binding to a site located within the NMDA associated ion channel and thus prevents Ca2+ flux.

M2N12 is a potent and highly selective cell division cycle 25C protein phosphatase (Cdc25C) inhibitor with an IC50 value of 0.09  μM. M2N12 also has promising activity against Cdc25A and Cdc25B with IC50 values of  0.53  μM and 1.39 μM, respectively. M2N12 has anti-tumor activity and can be used for cancer research.

Bifluranol (brand name Prostarex; former developmental code name BX-341) is a synthetic nonsteroidal estrogen of the stilbestrol group related to diethylstilbestrol that has been used as an antiandrogen in the United Kingdom in the treatment of benign prostatic hyperplasia. It exerts functional antiandrogen effects by binding to and activating the estrogen receptor in the pituitary gland, consequently suppressing the secretion of luteinizing hormone (and hence acting as an antigonadotropin) and thereby reducing gonadal androgen production and systemic androgen levels.