A potent, selective KDM5 sub-family(JARID1) inhibitor with biochemical IC50 of 71/19/69/69 nM for KDM5A/B/C/D, respectively.

PK 11195 is a ligand of translocator protein. It targets Leishmania chemotherapy (IC50s of 14.2 μM, 8.2 μM, 3.5 μM for L. amazonensis, L. major and L. braziliensis, respectively).

A potent, ATP-competetive CDKs inhibitor with IC50 of 7, 7, 7, 3 uM for Cdc2/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, and Cdk/p35 kinase.

Iperoxo is a superagonist of the muscarinic acetylcholine receptors and an OxotremorineM analog.

BL-1249 is a nonsteroidal anti-inflammatory drug (NSAID) and a potassium channel activator. BL-1249 exhibits more selective for the bladder (EC50 of 1.26 μM) than vascular tissue (EC50 of 21.0 μM). BL-1249 extracellular application activates all TREK subfamily members but has no effect on other K2P subfamilies. BL-1249 potently activates K2P2.1 (TREK-1) and K2P10.1 (TREK-2) with EC50 values of 5.5 μM and 8.0 μM, respectively

Fosmidomycin sodium salt is a phosphonic acid antibiotic and a antimalarial drug, which is active against both Gram-negative and Gram-positive bacteria.

AC-55649 is a potent, highly isoform-selective agonist of human RARβ2 receptor, with a pEC50 of 6.9.

Pinacidil monohydrate, an antihypertensive drug, is a potassium channel activator.

Dodecanoylcarnitine is present in fatty acid oxidation disorders such as long-chain acyl CoA dehydrogenase deficiency, carnitine palmitoyltransferase I/II deficiency, and is also associated with celiac disease.

Eicosadienoic acid is a rare, naturally occurring n-6 polyunsaturated fatty acid found mainly in animal tissues.

Fluspirilene is a non-competitive antagonist of L-type calcium channels with an IC50 of 0.03 μM. Fluspirileneis a long-acting injectable depot antipsychotic drug used for schizophrenia.

LMT-28 (LMT28) is a specific blocker of IL-6 signaling via inhibits IL-6Rβ (gp130) with IC50 of 5.9 uM (IL-6–induced luciferase activity), selectively inhibits IL-6–induced phosphorylation of STAT3, JAK2, and gp130.

KH7 is a soluble adenylyl cyclase (sAC)-specific inhibitor, with IC50s of 3-10 μM toward both recombinant purified human sACt protein and heterologously expressed sACt in cellular assays.

Calmidazolium chloride (R 24571) is a calmodulin (CaMK) antagonist, antagonizing CaM-dependent phosphodiesterase and calmodulin-induced activation of erythrocyte Ca2+-transporting ATPase with IC50s of 0.15 and 0.35 μM, respectively. Also in anti-cancer re

SPD304 is a selective inhibitor of tumor necrosis factor α (TNFα) and promotes dissociation of TNF trimers and therefore blocks the interaction of TNF and its receptor, with an IC50 of 22 µM for inhibiting in vitro TNF receptor 1 (TNFR1) binding to TNF-α.

PF 750 is a selective and covalent fatty acid amide hydrolase (FAAH) inhibitor, with IC50s varied from 16.2-595 nM in different pre-incubation times. Covalently modifies the enzyme’s active site serine nucleophile.

L-165041 is a potent PPARδ agonist (Ki = 6 nM).

SB-612111 is a potent, selective nociceptin/orphanin FQ receptor (NOP receptor) antagonist with Ki of 0.33 nM.

A potent blocker of high-conductance Ca2+-activated K+ (BKCa, KCa1.1) channels that binds to the α-subunit of BKCa with Ki of 1.9 nM.

A potent, orally active microsomal triglyceride transfer protein (MTP) inhibitor that inhibits both human and rodent MTP with IC50 of 2 nM.

LMI070 (NVS-SM1) is a highly potent, selective and orally active small molecule SMN2 splicing modulator.

LMPTP inhibitor 1 is a potent molecule for diabetes which can increase liver IR phosphorylation in vivo and reverses high-fat diet-induced diabetes by inhibiting the IR phosphatase LMPTP.

LOC-14 is a small molecule reversible Protein disulfide isomerase (PDI) inhibitor with Kd of 62 nM.

Loflucarban is an antiinfective drug

LOXO-195 is a next-generation TRK kinase (TKI) inhibitor, with IC50s of 0.6±0.1 nM, <2.5 nM for TRKA and TRKC respectively.

LP-211 is a selective and blood−brain barrier penetrant 5-HT7 receptor agonist, with a Ki of 0.58 nM, with high selectivity over 5-HT1A receptor (Ki, 188 nM) and D2 receptor (Ki, 142 nM).

CCK Octapeptide (Sincalide, Cholecystokinin Octapeptide, CCK-OP, CCK-8, SQ 19,844) is a endogenous peptide hormone found in the intestine and brain that stimulates digestion.

MiTMAB is a selective dynamin inhibitor that targets the dynamin-phospholipid interaction. MiTMAB inhibits dynamin GTPase activity with a Ki of 940 nM.

DL-α-Tocopherol acetate (DL-Alpha-tocopherol acetate , Vitamin E acetate), a vitamin E derivative, is used as a vitamin E supplement in poultry feeds.

Heptamidine (SBi4211) Dimethanesulfonate is a novel and potent Pentamidine-related inhibitor of the calcium-binding protein S100B with a Kd of 6.9 μM.