Vigabatrin(γ-Vinyl-GABA; Sabril) is a structural analog of the inhibitory neurotransmitter γ-aminobutyric acid (GABA) that irreversibly inhibits the catabolism of GABA by GABA transaminase. IC50 value: Target: GABA transaminase Clinical studies have sh

Nefazodone hydrochloride is an antidepressant drug.

SB-674042 is a potent and selective non-peptide orexin OX1 receptor antagonist (Kd = 3.76 nM); exhibits 100-fold selectivity for OX1 over OX2 receptors.

Bay 60-7550 is a potent PDE2 inhibitor with IC50 values of 2.0 nM (bovine) and 4.7 nM (human); 50-fold more selective for PDE2 compared to PDE1 and greater than 100-fold selective compared to PDE5, PDE3B, PDE4B, PDE7B, PDE8A, PDE9A, PDE10A, and PDE11A.

D609 is a selective competitive phosphatidyl choline-specific phospholipase C (PC-PLC) inhibitor (Ki = 6.4 μM); antiviral and antitumor agent.

TRAM-34 is a highly selective blocker of intermediate conductance Ca2+-activated K+ channels (KCa3.1) (Kd = 20 nM).

Ingenol 3-Angelate is a PKC(protein kinase C)activator; anti-cancer drug and an active ingredient in Euphorbia peplus.

Cinnarizine is a medication derivative of piperazine, and characterized as an antihistamine and a calcium channel blocker.

VO-Ohpic is a potent inhibitor of PTEN (phosphatase and tensin homolog) with IC50 of 35 nM.

Mexiletine hydrochloride is a non-selective voltage-gated sodium channel blocker; Class IB anti-arrhythmic compound.

Stavudine is a nucleoside analog that inhibits reverse transcriptase and has in vitro activity against HIV.

Salsalate is a nonsteroidal anti-inflammatory drug (NSAID).

BP897 is a partially selective D3 dopamine receptor agonist.

Trk-IN-3 is a potent pan-Trk inhibitor in cell-based assays with IC50s of 8.4 nM, 6.2 nM and 2.2 nM for TrkA, TrkB and TrkC, respectively. Anti-hyperalgesic effect.

6-Hydroxy-DL-DOPA is a small-molecule that disrupts with RAD52 oligomerization, inhibits ssDNA binding by RAD52 with IC50 of 1.1 uM and by RAD52 (1 209) with IC50 of 1.6 uM.

Calhex-231 is a potent negative allosteric modulator of CaSR that blocks calcium-mediated activation with IC50 of 0.39 uM.

DC_AC50 (DCAC50) is a small molecule that inhibits the human copper chaperones Atox1 and CCS (Kd=6.8 and 8.2 uM), blocks copper trafficking and significantly attenuates cancer cell proliferation.

Edelfosine is a synthetic lysophospholipid analog that selectively inhibits PLC with IC50 of 9.6 uM in fibroblasts and adenocarcinoma cells.

CC-671 is a potent, selective, dual TTK (Mps1)/CLK2 inhibitor with IC50 of 5/3 nM, respectively.

CRANAD-2 is a difluoroboron-derivatized curcumins as near-infrared probe for in vivo detection of amyloid-beta deposits. Upon interacting with Abeta aggregates, CRANAD-2 undergoes a range of changes, which include a 70-fold fluorescence intensity increase, a 90 nm blue shift (from 805 to 715 nm), and a large increase in quantum yield. Moreover, this probe also shows a high affinity for Abeta aggregates (K(d) = 38.0 nM), a reasonable log P value (log P = 3), considerable stability in serum, and a weak interaction with albumin. After intravenous injection of this probe, 19-month-old Tg2576 mice exhibited significantly higher relative signal than that of the control mice over the same period of time.

A286982 is an inhibitor that blocks the integrin-ligand interaction between leukocyte function-associated antigen-1 (LFA-1) and intercellular adhesion molecule-1.

MELK-T1 is a potent and selective inhibitor of protein kinase MELK.

Merimepodib(VX-497) is a novel noncompetitive inhibitor of IMPDH (Inosine monophosphate dehydrogenase).

MI-136 inhibits DHT-induced expression of androgen receptor (AR) target genes.

MI-503 is a highly potent and orally bioavailable small molecule inhibitor of the menin-MLL interaction.

MI-77301 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.

Migalastat hydrochloride (1-Deoxygalactonojirimycin hydrochloride) is a potent and competitive inhibitor of α-galactosidase A (α-Gal A) with an IC50 of 0.04 μM for human α-Gal A.

Mirin is a Mre11-Rad50-Nbs1 (MRN)-ATM pathway inhibitor that blocks the 3' and 5' exonuclease activity associated with Mre11.

Mirogabalin (DS-5565) is a novel, preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium-channel complexes in the CNS.

Mitapivat is an activator of pyruvate kinase isoenzyme M2 (PKM2),