FT113 is a potent and orally active fatty acid synthase (FASN) inhibitor, with an IC50 of 213 nM for full-length recombinant human FASN enzyme.

Fulacimstat(BAY 1142524) is a small molecule chymase inhibitor.

Fumalic acid (Ferulic acid)

G-15 is a cell-permeable non-steroidal antagonist of GPER (Ki = 20 nM).

G1T28(Trilaciclib) is a potential first-in-class, short-acting IV CDK4/6 inhibitor being developed to preserve hematopoietic stem cells and enhance immune system function during chemotherapy.

G-36 is a cell-permeable non-steroidal antagonist of GPER, inhibiting activation by either 17β-estradiol or the GPER-selective agonist G-1(IC50 = 112 and 165 nM, respectively).

Gambogic Acid activates caspases with EC50 of 0.78-1.64 μM and competitively inhibits Bcl-xl, Bcl-2, Bcl-w, Bcl-B, Bfl-1 and Mcl-1 with IC50 of 1.47 μM, 1.21 μM, 2.02 μM, 0.66 μM, 1.06 μM and 0.79 μM, respectively.

GCN2-IN-1 is a potent general control nonderepressible 2 kinase (GCN2) inhibitor with IC50s of <0.3 μM in the enzyme and cell assay.

GDC0575（ARRY-575，RG7441）is a small molecule inhibitor of cell cycle checkpoint kinase 1 (Chk1), with potential chemosensitization activity.

GDP366, a dual inhibitor of survivin and Op18, induces cell growth inhibition, cellular senescence and mitotic catastrophe in human cancer cells.

Genistein is a highly specific inhibitor of protein tyrosine kinase (PTK).

Genz-123346 free base is an inhibitor of GL1 synthase that blocks the conversion of ceramide to GL1; IC50 for GM1 inhibition is 14 nM.

GIBH-130 is a novel inhibitor of neuroinflammation effective in Alzheimer’s disease models.

GJ103 is an active analog of the read-through compound GJ072.

GLPG0634 (analog) is a pan JAK inhibitor with IC50s of 50-200 nM for JAK1/JAK2/JAK3; more information can be found in the reference patents.

GLPG-1837(ABBV-974) is a novel cystic fibrosis transmembrane conductance regulator CFTR potentiator.

glucagon receptor antagonists-4 is a highly potent glucagon receptor antagonist.

GLX351322 is an inhibitor of NADPH oxidase 4, and inhibits hydrogen peroxide production from NOX4-overexpressing cells with an IC50 of 5 μ M.

SNX-2112 selectively binds to the ATP pocket of HSP90α and HSP90β with Ka of 30 nM and 30 nM, uniformly more potent than 17-AAG.

AF38469 is a potent, selective, orally bioavailable Sortilin inhibitor with IC50 of 330 nM, shows no activity against the NTR1 receptor as well as a panel of targets known to bind acidic molecules (δ-Opioid, GPR40, PPARδ, EP1, Angiotensin AT1, Endothelin

PNU-159682 is a major bioactive metabolite of Nemorubicin in human liver microsomes; > 3,000-fold cytotoxic than its parent compound(MMDX and doxorubicin).

Lumateperone (ITI-007) is a potent 5-HT2A antagonist (Ki=0.54 nM), postsynaptic D2 antagonist(Ki=32 nM), and SERT blocker (Ki= 61 nM).

Masitinib is a broad coronavirus 3CL inhibitor that effectively blocks replication of SARS-CoV-2. Science 20 Jul 2021: eabg5827 DOI: 10.1126/science.abg5827

LY2584702 is a potent, selective, ATP-competitive inhibitor of P70 S6 kinase-1 (p70S6K1) with IC50 of 4 nM.

Fasentin is a novel inhibitor of glucose uptake (GLUT) that sensitizes cancer cells to FAS-induced cell death, preferentially inhibits GLUT4 (IC50=68 uM) over GLUT1.

DDO-5936 is a potent PPI inhibitor targeting Hsp90-Cdc37 protein-protein interaction (PPI) as Orally Active Inhibitors for the Treatment of Colorectal Cancer. DDO-5936 disrupted the Hsp90-Cdc37 PPI both in vitro and in vivo via binding to a previously unknown site on Hsp90 involving Glu47, one of the binding determinants for the Hsp90-Cdc37 PPI, leading to selective down-regulation of Hsp90 kinase clients in HCT116 cells. In addition, inhibition of Hsp90-Cdc37 complex formation by DDO-5936 resulted in a remarkable cyclin-dependent kinase 4 decrease and consequent inhibition of cell proliferation through Cdc37-dependent cell cycle arrest.

Ombrabulin (AVE8062) hydrochloride is a synthetic derivative of CA-4-P, which inhibits growth in a large number of drug-resistant animal tumors and carcinogen-induced tumors.

Nalfurafine (TRK-820, TRK820) is potent, selective agonist of kappa-opioid receptor with Ki of 3.5 nM, 15-fold less potent for μOR and little affinity for δOR (Ki=53 and 1,200 nM, respectively).

Avatrombopag (AKR-501) hydrochloride is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag hydrochloride mimics the biological activities of TPO. Avatrombopag hydrochloride increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag hydrochloride is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A.

Avatrombopag, also known as AKR-501, YM477, AS 1670542 or E5501, is a novel orally-active thrombopoietin (TPO) receptor agonist. AKR-501 specifically targeted the TPO receptor and stimulated megakaryocytopoiesis throughout the development and maturation of megakaryocytes just as rhTPO did. AKR-501 may be useful in the treatment of patients with thrombocytopenia.