α,β-Methylene ATP dilithium, a phosphonic analog of ATP, is a P2X3 and P2X7 receptor ligand. α,β-Methylene ATP dilithium is a highly selective agonist for P2X1 and P2X3, with practically no activity at P2X2,4-7.

Epiboxidine is a potent and selective neural nAChR agonist with Kis of 0.46 nM and 1.2 nM for rat and human α4β2 nAChRs, respectively. Epiboxidine is a methylisoxazole analog of the alkaloid Epibatidine, and is also an analog of another nAChR agonist, ABT 418.

D-AP4 (D-APB; D-2-Amino-4-phosphonobutyric acid), a phosphono analogue of glutamate, is an NMDA broad spectrum excitatory amino acid receptor antagonist. D-AP4 also is an agonist for a quisqualate-sensitized AP6 site in hippocampus. D-AP4 inhibits AMPA receptor-stimulated 57Co2+ influx in cultured cerebellar granule cells (IC50 ≥ 100 μM).

Navocaftor, as a cystic fibrosis transmembrane regulator (CFTR), is a protein modulator (US 20200377491 Al, example 1).

Dirocaftor (PTI-808) is a CFTR potentiator that enhances the function of CFTR protein by opening chloride channels. Dirocaftor can be used for cystic fibrosis (CF) research.

Bamocaftor (VX-659) is a cystic fibrosis transmembrane conductance regulator (CFTR) corrector designed to restore F508del-CFTR protein function. Bamocaftor can be used combine with Tezacaftor and Ivacaftor in cystic fibrosis research.

Norverapamil D7 ((±)-Norverapamil D7) hydrochloride is a deuterium labeled Norverapamil. Norverapamil ((±)-Norverapamil), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.

Nezulcitinib (TD-0903) is an inhaled and lung-selective pan-Janus kinase (JAK) inhibitor. Nezulcitinib can be used for the research of COVID-19 associated acute lung injury and impaired oxygenation.

JAK2/FLT3-IN-1 (TFA) is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 (TFA) has anti-cancer activity.

Deuruxolitinib (CTP-543), a deuterated Ruxolitinib, modulates the activity of JAK1/JAK2. Deuruxolitinib can be used for the research hair loss disorders (from patent WO2017192905A1, compound I).

BGC-20-1531 (PGN 1531) free base is a potent and selective prostanoid EP4 receptor antagonist, with a pKb of 7.6. BGC-20-1531 free base has the potential for the research of migraine headache.

2-Methylthio-AMP (2-MeSAMP) diTEA is a selective and direct P2Y12 antagonist. 2-Methylthio-AMP diTEA is an inhibitor of ADP-dependent platelet aggregation.

Imnopitant is a NK1 receptor antagonist (WO2020132716, compound 1) .

L-AP3, metabotropic glutamate receptor (mGluR) antagonist, inhibits D-phosphoserine and L-phosphoserine with IC50s of 368 μM and 2087 μM, respectively.

UPF-523 (AIDA), a rigid (carboxyphenyl) glycine derivative, is a relatively potent and selective antagonist of group I metabotropic glutamate receptors (mGlu1a) with an IC50 of 214 μM. But UPF-523 has no effect on group II (mGlu2), group III (mGlu4) receptors or ionotropic glutamate receptors. UPF-523 has the potential for the research of the acute arthritis.

DH97 is a potent and selective antagonist of MT2 melatonin receptor, with a pKi of 8.03 for human MT2. DH97 shows 89- and 229-fold selectivity for human MT2 over human mt1 and Xenopus mel1c receptor subtypes. DH97 can inhibit melatonin-induced enhancement of electrically-evoked responses.

UCM 608 is a high affinity melatonin (MT) membrane receptor agonist. The pKi values for MT1 and MT2 are 10.7 and 10.4.

MCL0020 is a potent and selective melanocortin MC4 receptor antagonist, with an IC50 of 11.63 nM. MCL0020 dose-dependently and significantly attenuates restraint stress-induced anorexia without affecting food intake.

(S)-(+)-Dimethindene maleate, an enantiomer, is a potent M2-selective muscarinic receptor antagonist (pA2 = 7.86/7.74; pKi = 7.78). (S)-(+)-Dimethindene maleate shows lower affinities for the muscarinic M1 (pA2 = 6.83/6.36; pKi = 7.08), the M3 (pA2 = 6.92/6.96; pKi = 6.70) and the M4 receptors (pKi = 7.00), respectively. (S)-(+)-Dimethindene maleate also is a histamine H1 receptor antagonist (pA2 = 7.8).

Cipralisant (GT-2331) (maleate) is an orally active, low-toxicity, potent, selective, high affinity histamine H3 receptor full antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor. Cipralisant (maleate) has the potential for attention-deficit hyperactivity disorder research.

Quinelorane dihydrochloride (LY163502) is a potent dopamine D3/D2 receptor agonist. Quinelorane has the potential for neurological and psychiatric disorders research.

(±)-Penbutolol-d9 ((Rac)-Penbutolol-d9) hydrochloride is a deuterium labeled (±)-Penbutolol hydrochloride. (+)-Penbutolol hydrochloride is a β-adrenoceptor antagonist, with an IC50 of 0.74 μM.

SB 258719 (hydrochloride) is a selective 5-HT7 receptor antagonist displayed high affnity (pKi=7.5) for the receptor. SB-258719 (hydrochloride) shows apparent partial inverse agonism.

Felcisetrag (TD-8954) is an orally active, potent and selective 5-HT4 receptor agonist with gastrointestinal prokinetic properties. Felcisetrag has high affinity (pKi =9.4) for human 5-HT4(c) receptors.

XVA143, an α/β I-like allosteric antagonist, inhibits LFA-1 dependent firm adhesion, while at the same time it enhances adhesion in shear flow and rolling both in vitro and in vivo.

T-2513 hydrochloride is a selective topoisomerase I inhibitor. T-2513 hydrochloride binds covalently to and stabilizes the topoisomerase I-DNA complex and inhibits DNA replication and RNA synthesis, ultimately leading to cell death.

Intoplicine (RP 60475) dimesylate, an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNA topoisomerase I and II inhibitor. Intoplicine dimesylate strongly binds DNA (KA = 2 x 105 /M) and thereby increases the length of linear DNA.

Cotosudil is a ROCK kinase inhibitor, which can be used for glaucoma or ocular hypertension research.

Fostroxacitabine bralpamide (MIV-818) is an orally active Troxacitabine-based nucleotide prodrug. Fostroxacitabine bralpamide has anticancer effects.

(-)-Irofulven (MGI 114), an Illudin S analog, is a DNA alkylating agent. (-)-Irofulven inhibits the replication of DNA, induces tumor cells apoptosis, and has potent antitumor activity.