WAY-641966 is a anti-prion agent.

WAY-320461 is a FAK inhibitor.

ELOVL1-IN-2 is an elongation of very long chain fatty acid 1 (ELOVL1) enzyme inhibitor, ELOVL1-IN-2 shows weak ELOVL1 inhibition (IC50=21 μM) and moderate potency in a primary cellular assay (HEK293 C26 IC50=6.7 μM) .

ESI-08 is a potent and selective EPAC antagonist, which can completely inhibit both EPAC1 and EPAC2.

5-HT3 antagonist 5 is a quinoxalin-2-carboxamide compound, a 5-HT3 receptor antagonist. 5-HT3 antagonist 5 exerts antagonism on 5-HT3 agonist and 2-methyl-5-HT, and shows anti-depressant effect in mice[1].

PKCiota-IN-2 is a potent PKCiota (PKC-ι) inhibitor with an IC50 of 2.8 nM. PKCiota-IN-2 also inhibits PKC-α and PKC-ε with IC50s of 71 nM and 350 nM, respectively.

RET agonist BT44 is a novel, specific RET agonist, promotes RET phosphorylation and selectively activates downstream cascades in the cells expressing GFL receptors.BT44 has no effect on TrkA and TrkB receptors; In GFRα1/RET expressing cells, 10–50 µM of BT44 increased the activity of luciferase reporter by approximately two fold (P<0.0001).BT44 dose-dependently stimulated neurite outgrowth from DRG sensory neurons and its efficacy was comparable to that of ARTN.BT44 alleviated mechanical hypersensitivity in surgery- and diabetes-induced rat models of neuropathic pain.

NPT200-11 is an orally bioavailable and brain penetrating alpha-synuclein (ASYN) misfolding and aggregation inhibitor.

MMV030084 (MMV-030084) is a potent, specific P. falciparum cGMP-dependent protein kinase (PKG) inhibitor (Kdapp=9-16 nM), inhibits invasion of P. berghei ANKA parasites into HepG2 liver cells with IC50 of 199 nM.MMV030084 potently inhibits hepatocyte invasion by Plasmodium sporozoites, merozoite egress from asexual blood stage schizonts, and male gamete exflagellation, shows potent activity against liver, asexual, and sexual blood stage development.MMV030084 showed an IC50 of 109 nM against the drug-sensitive 3D7-A10 line, and an IC50 of 120 nM against multidrug-resistant Dd2-B2 parasites in a 72-h growth inhibition assay against Pf ABS parasites.MMV030084 inhibited male gamete exflagellation at an IC50 of 141 nM when gametocytes were stimulated to develop into male gametes.MMV030084 is a promising Plasmodium PKG-targeting chemotype.

TRPM4-IN-2 (NBA) is a potent transient receptor potential melastatin 4 (TRPM4) inhibitor with an IC50 value of 0.16 μM. TRPM4-IN-2 can be used for researching prostate cancer and colorectal cancer[1][2].

BAY-4931 is a potent covalent PPARγ inverse-agonist with IC50 of 0.17 nM and could be a novel tool for probing the in vitro biology of PPARγ inverse-agonism.

BAY-0069 is a potent covalent PPARγ inverse-agonist with IC50 of 0.22 nM and could be a novel tool for probing the in vitro biology of PPARγ inverse-agonism.

BAY-069 is a potent dual BCAT1/BCAT2 inhibitor with IC50 of 31 nM/153 nM. BAY-069 displays high cellular activity in U-87 MG and MDA-MB-231 cell lines.

JDQ443 (example 1a) is a covalent KRAS G12C inhibitor (extracted from patent WO2021120890A1).

Adaptaquin is an inhibitor of hypoxia-inducible factor prolyl hydroxylase 2 (HIF-PHD2), with an IC50 of 2 μM. Adaptaquin can inhibit lipid peroxidation and maintain mitochondrial function[1][2].

Vibozilimod (example 33) is a S1p1 receptor agonist (extracted from patent WO2012140020A1).

.Valemetostat is an antineoplastic agent.

Dopamine D2 receptor agonist-2 (compound 36) is a potent dopamine D2 receptor biased agonism ligand with an Ki value of 11.2 nM. Dopamine D2 receptor agonist-2 can be used to research antipsychosis[1].

c-Fms-IN-13 (compound 14) is a potent FMS kinase inhibitor with an IC50 value of 17 nM. c-Fms-IN-13 can be used as an anti-inflammatory agent[1].

RLX-33 is a potent, selective and blood-brain barrier (BBB) penetrant relaxin family peptide 3 (RXFP3) antagonist, also blocks relaxin-3-induced ERK1/2 phosphorylation, with IC50 values of 2.36 μM for RXFP3, 7.82 and 13.86 μM for ERK1 and ERK2 phosphorylation, respectively. RLX-33 can block the stimulation of food intake induced by the RXFP3-selective agonist R3/I5 in rats. RLX-33 can be used for the research of metabolic syndrome[1].

Lepidiline C shows cytotoxic activity against HL-60 cells with an IC50 of 27.7 μM.

ISR-IN-1 (Compound 48) is an inhibitor of the integrated stress response.

ISR-IN-2 (Compound 47) is an inhibitor of the integrated stress response .

UCM05 (G28UCM) is a potent inhibitor of fatty acid synthase (FASN) shows activity against HER2+ breast cancer xenografts and is active in anti-HER2 drug-resistant cell lines[1]. UCM05 is a Filamentous temperature-sensitive protein Z (FtsZ) inhibitor and inhibits the growth of the Gram-positive bacterium B. subtilis with MIC values of 100 μM but lack activity on the Gram-negative bacterium E. coli[2].

BSP16 is a potent, orally active stimulator of interferon genes (STING) agonist. BSP16 can selectively stimulate the STING pathway. BSP16 can be used for the research of cancer.

α-Lapachone shows trypanocidal activity[1].

GSK 3186899 (GSK-3186899, DDD853651) is a novel specific inhibitor of parasite cdc-2-related kinase 12 (CRK12), shows activity against L. donovani in intra-macrophage assay with EC50 value of 1.4 uM, and shows good selectivity against mammalian THP-1 host cells (EC50> 50 uM).