Elimusertib, also known as BAY-1895344, is a potent and selective ATM inhibitor. BAY 1895344 shows potent anti-tumor efficacy in monotherapy and strong combination potential with the targeted alpha therapy Radium-223 dichloride.

MLN-120B is a potent and effective inhibitor of IκB kinase beta subunit (IKKβ) with IC50 value of 20 μM. MLN-120B blocks multiple myeloma cell growth in vitro and in vivo.

SKF89976A is a potent GABA uptake inhibitor, which is selective for GAT-1 (IC50 values are 0.13, 550, 944 and 7210 μM for hGAT-1, rGAT-2, hGAT-3 and hBGT-1 respectively). SKF89976A inhibits transport current competitively (Ki = 7 μM) and transmitter-gated current non-competitively (Ki = 0.03 nM). It is able to pass the blood-brain barrier after systemic administration and is active in vivo.

E4031 selectively blocks hERG K+ channels. E4031 inhibits the rapid delayed-rectifier K+ current (IKr) and reversibly prolongs action potential duration in guinea pig papillary muscle and isolated ventricular myocytes, without affecting Na+ or Ca2+ inward currents. E4031 is a class III antiarrhythmic agent.

RS 100329 is a subtype-selective α1A-adrenoceptor antagonist (pKi = 9.6 for human cloned α1A receptors). RS 100329 displays 126- and 50-fold selectivity over human α1B and α1D receptors respectively.

GDC-0575, also known as ARRY-575 and RG7741, is a potent and selective inhibitor of cell cycle checkpoint kinase 1 (Chk1) with an IC50 of 1.2 nM. Chk1 inhibitor GDC-0575 specifically binds to and inhibits Chk1; this may result in tumor cells bypassing Chk1-dependent cell cycle arrest in the S and G2/M phases, which permits the cells to undergo DNA repair prior to entry into mitosis.

Necrosulfonamide is a novel inhibitor of MLKL (mixed lineage kinase domain-like). Necrosulfonamide is a cell-permeable inhibitor that covalently modifies Cys88 and blocks human MLKL adaptor function. Necrosulfonamide Attenuates Spinal Cord Injury via Necroptosis Inhibition.

GW438014A is a selective NPY-Y5 receptor antagonist.

Nilotinib, also known as AMN-107, is an orally bioavailable aminopyrimidine-derivative Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity. Designed to overcome imatinib resistance, nilotinib binds to and stabilizes the inactive conformation of the kinase domain of the Abl protein of the Bcr-Abl fusion protein, resulting in the inhibition of the Bcr-Abl-mediated proliferation of Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) cells. This agent also inhibits the receptor tyrosine kinases platelet-derived growth factor receptor (PDGF-R) and c-kit, a receptor tyrosine kinase mutated and constitutively activated in most gastrointestinal stromal tumors (GISTs).

Acotiamide, also known as YM-443 and Z-338, is a drug approved in Japan for the treatment of postprandial fullness, upper abdominal bloating, and early satiation due to functional dyspepsia. It acts as an acetylcholinesterase inhibitor. Note: The Approved drug API is a cotiamide HCl trihydrate (1:1:3)

Givinostat hydrochloride is a novel histone deacetylase inhibitor with potential anti-inflammatory, anti-angiogenic, and antineoplastic activities.

AZD-5153 HNT salt, is a 6-hydroxy-2-naphthoic acid salt of AZD-5153. AZD 5153 a potetn and selective orally available, bivalent inhibitor of the bromodomain and extraterminal (BET) protein BRD4 (IC50 = 5 nM). AZD5153 is highly Active against Hematologic Malignancies.

AVN-101 is a very potent 5-HT7 receptor antagonist, with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors. It is a milti-target drug candidate for the treatment of CNS disorders.

Abaperidone, also known as FI 8602, is an atypical antipsychotic. Reduced hsp70 in the prefrontal cortex may play a critical role in the etiology of many schizophrenia symptoms and may be linked to an atypical profile of antipsychotics, such as abaperidone.

Paclitaxel-SMCC is a paclitaxel derivative with a SMCC linker. (Succinimidyl-4-( N-maleimidomethyl)cyclohexane-1-carboxylate). Maleimide in Paclitaxel-SMCC can react with sulfhydryl groups at pH 6.5-7.5 to form a stable thioether bond. Paclitaxel-SMCC can be used to synthesize Paclitaxel bioconjugates with proteins, enzymes; antobodies, antigens, and other biopolymers. Paclitaxel-SMCC is often used for drug delivery research.

BPDBA is a noncompetitive inhibitor of the betaine/GABA transporter 1 (BGT1).

Oclacitinib, also known as PF03394197, is a novel Janus kinase inhibitor with activity against cytokines involved in allergy. Oclacitinib inhibited JAK family members by 50% at concentrations (IC50 's) ranging from 10 to 99 nM and did not inhibit a panel of 38 non-JAK kinases (IC50 's > 1000 nm). Oclacitinib was most potent at inhibiting JAK1 (IC50 = 10 nm). Oclacitinib also inhibited the function of JAK1-dependent cytokines involved in allergy and inflammation (IL-2, IL-4, IL-6, and IL-13) as well as pruritus (IL-31) at IC50 's ranging from 36 to 249 nM.

BI-44370 is a CGRP (calcitonin gene-related peptide) receptor antagonist that can be used to treat migraines and other chronic pain.Efficacy of BI 44370 TA was shown in a dose-dependent manner in the treatment of acute migraine attacks.

Sitagliptin, also known as MK-0431, is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts. Sitagliptin is believed to exert its actions in patients with type 2 diabetes mellitus by slowing the inactivation of incretin hormones. By increasing and prolonging active incretin levels, sitagliptin increases insulin release and decreases glucagon levels in the circulation in a glucose-dependent manner. Sitagliptin demonstrates selectivity for DPP-4 and does not inhibit DPP-8 or DPP-9 activity in vitro at concentrations approximating those from therapeutic doses.

Phosphatidylcholines (PC) are a class of phospholipids that incorporate choline as a headgroup. They are a major component of biological membranes and can be easily obtained from a variety of readily available sources, such as egg yolk or soybeans, from which they are mechanically or chemically extracted using hexane. They are also a member of the lecithin group of yellow-brownish fatty substances occurring in animal and plant tissues. Dipalmitoyl phosphatidylcholine (aka: lecithin) is a major component of pulmonary surfactant and is often used in the L/S ratio to calculate fetal lung maturity.

TCS-401 (HCI) is a selective inhibitor of protein-tyrosine phosphatase 1B (PTP1B; Ki = 0.29 µM). It inhibits the protein phosphatases CD45 D1D2, PTPβ, PTPε D1, SHP-1, PTPα D1, and LAR D1D2 at much higher concentrations (Kis = 59, 560, 1,100, >2,000, >2,000, and >2,000 μM, respectively).1 Several PTPs have been proposed to act as negative regulators of insulin signaling, thus this enzyme is a potential drug target in diabetes.

BMS 182874 is an endothelin receptor antagonist and antihypertensive agent.

Belfosdil, also known as BMY 21891 and SR 7037, is an antihypertensive calcium channel blocker.

Selisistat racemate is a racemic mixture of EX-527, an inhibitor of sirtuin 1 (SIRT1; IC50 = 0.098 µM). It is selective for SIRT1 over SIRT2, and SIRT3 (IC50s = 19.6 and 48.7 µM, respectively) and the cytochrome P450 (CYP) isoforms CYP3A4, CYP2D6, CYP2C9, CYP2C19, and CYP1A2 at 1 µM. EX-527 (50 µM) induces cell cycle arrest at the G1 phase in MCF-7 cells.

BMS-863233, also known as XL-413, is an orally bioavailable cell division cycle 7 homolog (CDC7) kinase inhibitor with potential antineoplastic activity. CDC7 kinase inhibitor BMS-863233 binds to and inhibits the activity of CDC7, which may result in the inhibition of DNA replication and mitosis, the induction of tumor cell apoptosis, and the inhibition of tumor cell proliferation in CDC7-overexpressing tumor cells. CDC7, a serine-threonine kinase overexpressed in a variety of tumor cell types, plays an essential role in the initiation of DNA replication by activating origins of replication.

ABP-700 is an etomidate analog that is effective as an anesthetic.

NSC23766 is a potent Rac1 inhibitor. NSC23766 disrupted polar secretion of adhesive, polarization of endomembranes, and tip-focused growth in the rhizoid. NSC23766 can acts as a competitive antagonist at muscarinic acetylcholine receptors. NSC23766 exerts anti-influenza virus properties by affecting the viral polymerase complex activity. NSC23766 suppresses CREB signaling by targeting NMDA receptor function.

Pyridostatin stabilizes G-quadruplexes (G4s) in cells and elicits a DNA damage response by causing the formation of DNA double strand breaks (DSB). Pyridostatin promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin targets gene bodies containing clusters of sequences with a propensity for G-quadruplex formation. As a result, pyridostatin modulated the expression of these genes, including the proto-oncogene SRC.

RGX-104, also known as SB 742881, is a liver-X nuclear hormone receptor (LXR) agonist that modulates innate immunity via transcriptional activation of the ApoE gene.

THZ1 is a selective CDK7 inhibitor that preferentially diminishes transcription in cancer cells. THZ1 has the unprecedented ability to target a remote cysteine residue located outside of the canonical kinase domain, providing an unanticipated means of achieving selectivity for CDK7. Cancer cell-line profiling indicates that a subset of cancer cell lines, including human T-cell acute lymphoblastic leukaemia (T-ALL), have exceptional sensitivity to THZ1. Cyclin-dependent kinases (CDKs) are involved in temporal control of the cell cycle and transcription and play central roles in cancer development and metastasis.