WS-898 is a highly effective ABCB1 inhibitor capable of reversing paclitaxel (PTX) resistance in drug-resistant SW620/Ad300, KB-C2, and HEK293/ABCB1 cells (IC50 = 5.0, 3.67, and 3.68 nM, respectively).

Posenacaftor (PTI-801) is a cystic fibrosis transmembrane regulator (CFTR) protein modulator that corrects the folding and trafficking of CFTR protein. Posenacaftor is used for the research of cystic fibrosis (CF).

NMDA receptor antagonist-3, a NMDA receptor antagonist, stands out with a remarkable percentage of recovery (40.0%, at 100 μM) and safe toxicological profile in SH-SY5Y and human adipose mesenchymal stem cells.

nAChR agonist 2 (compound 8) is a selective alpha4beta2 (α4β2) nAChR agonist (Kd=26 nM).

P2X receptor-1 is a potential inhibitor of P2X receptor for the treatment of pain and inflammation.

TC-N 1752 is a potent and orally active inhibitor of Nav1.7, with IC50s of 0.17 μM, 0.3 μM, 0.4 μM, 1.1 μM and 2.2 μM at hNav1.7, hNav1.3, hNav1.4, hNaV1.5 and rNav1.8, respectively. TC-N 1752 also inhibits tetrodotoxin-sensitive sodium channels. TC-N 1752 shows analgesic efficacy in the Formalin model of pain.

TRPA1 Antagonist 3 is a photoswitchable TRPA1 agonist that enables optical control of the TRPA1 channel.

CGP 35348 is a selective, brain penetrant, centrally active GABAB receptor antagonist with an EC50 of 34 μM. CGP 35348 shows affinity for the GABAB receptor only. CGP 35348 has a potential to improve neuromuscular coordination and spatial learning in albino mouse following neonatal brain damage.

CP-601932 ((1S,5R)-CP-601927) is a high-affinity partial agonist at α3β4 nAChR (EC50=~ 3 μM). CP-601932 has the same high-binding affinity at α3β4 (Ki=21 nM) as at α4β2 nAChRs (Ki=21 nM) and an order of magnitude lower affinity for α6 and α7 nAChR subtypes. CP-601932 selectively decreases ethanol but not sucrose consumption and operant self-administration following long-term exposure. CP-601932 readily penetrates the CNS.

Guangxitoxin 1E is a potent and selective blocker of KV2.1 and KV2.2 channels. Guangxitoxin 1E inhibits KV2 with an IC50 of 1-3 nM. KV2 channels underlie delayed-rectifier potassium currents in various neurons.

(-)-Denudatin B is an antiplatelet agent. (-)-Denudatin B relaxed vascular smooth muscle by inhibiting the Ca2+ influx through voltage-gated and receptor-operated Ca2+ channels. And (-)-Denudatin B has nonspecific antiplatelet action

3-Aminopropylphosphinic acid (3-APPA), a phosphonic analog of GABA, is a GABAB receptor agonist.

Anabaseine, an alkaloid, stimulates a wide variety of animal nicotinic acetylcholine receptors (AChRs), especially the neuromuscular receptors and α7 AChRs.

4-(Phenyldiazenyl)benzoic acid is a photosensitive and photoswitchable TRPA1 agonist that can be used as pharmacological tools for study of pain signaling.

Co 101244 (PD 174494) hydrochloride is a NR2B-containing NMDA receptor antagonist.

SB 452533 is a potent and selective TRPV1 antagonist with the pKb of 7.8.

Iptakalim hydrochloride, a lipophilic para-amino compound, is a novel ATP-sensitive potassium channel (KATP) opener, as well as an α4β2-containing nicotinic acetylcholine receptor (nAChR) antagonist.

CGP 39551 is a potent, orally active, competitive N-methyl-D-aspartate (NMDA) receptor antagonist with potent anticonvulsant activity. CGP 39551 shows measurable inhibitory activity at both L-[3H]-glutamate (Ki=8.4 μM).

Ruzinurad is a highly selective URATl inhibitor (WO2020088641, compound I). Ruzinurad can be used in the study of hyperuricemia.

Idrevloride, an epithelial sodium channel (ENaC) inhibitor (WO2016133967), can be used for the research of skin disorders.

Zelquistinel is a N-methyl-D-aspartate (NMDA) receptor partial agonist used for the research of depression, anxiety and other related psychiatric disorders.

Pregabalin arenacarbil is a prodrug of Pregabalin.Pregabalin is an analog of gamma-aminobutyric acid (GABA) for the research of post herpetic neuralgia, peripheral diabetic neuropathy,fibromyalgia and epilepsy.

Simpinicline (OC-02), a highly selective nicotinic acetylcholine receptor (nAChR) agonist, shows potent antiviral activity against the SARS-CoV-2 variants in cell culture with an IC50 of 0.04 µM.

Ropanicant (SUVN-911 free base) is a novel, potent, selective, and orally active neuronal nicotinic acetylcholine α4β2 receptor antagonist for the research of depression.

Plazinemdor is a N-methyl-D-aspartate(NMDA) receptor positive allosteric modulator. Plazinemdor can be uses in the research of psychiatric, neurological, and neurodevelopmental disorders, as well as diseases of the nervous system..

Alogabat (example 8) is a GABAA α5 receptor positive allosteric modulators (PAMs) (extracted from patent WO2018104419A1).

Gitoxin, a Na+/K+-ATPase inhibitor, usually appears as a result of metabolic degradation of Digitoxin, is just the hydroxyl (ZOH) group close to the C-17β position, which changes the pharmacokinetics and pharmacodynamics of these substances considerably.

NHE3-IN-2 is a Na+/H+ exchanger-3 (NHE3) inhibitor ( patent WO2001079186A1, example 6-Chlor-4-phenyl-2-chinazolinyl-guanidin).

Ziconotide acetate (SNX-111 acetate), a peptide, is a potent and selective block of N-type calcium channels antagonist. Ziconotide acetate reduces synaptic transmission, and can be used for chronic pain research.

A small molecule corrector of ΔF508-CFTR with IC50 of 6.0 uM..