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Calcium Channel Blockers

Calcium Channel Blockers focused libraryCalcium channel blockers (CCBs) disrupt the movement of calcium (Ca2+) through calcium channels. They are used as antihypertensive drugs, i.e., as medications to decrease blood pressure in patients with hypertension. CCBs are particularly effective against large vessel stiffness, one of the common causes of elevated systolic blood pressure in elderly patients.

Potassium Channel Blockers

Kv1.5 Potassium Channel BlockerAtrial fibrillation is the most common sustained cardiac rhythm disorder, and confers a substantial mortality and morbidity from stroke, thromboembolism, heart failure, and impaired quality of life. With the increasingly elderly population in the developed world, the prevalence of atrial fibrillation is increasing, resulting in a major public-health problem.

HCN Channel Blocker Library

HCN Channel BlockerThe current produced by hyperpolarization-activated cyclic nucleotide-gated (HCN) channels (termed If, cardiac pacemaker “funny” current, and Ih in neurons) is also considered a “pacemaker current” because it plays a key role in controlling the rhythmic activity of cardiac pacemaker cells and spontaneously firing neurons.

Solubility Fragment Library

Solubility Fragment Library

The Solubility Fragment Library consists of about 957 low molecular fragments with "Rule-of-Three" compliance and assured solubility in both DMSO (200mM) and PBS buffer (1mM). The library design included diversity filtering in order to provide chemical structure variety for your fragment screening program.



CREBBP Targeted Library

CREBBP focused libraryCREB Binding Protein (CREBBP) is a coactivator of transcription factor CREB that activates genes in cAMP transcriptional pathway. The coactivator binds to transcription factor activation domains positions histone acetyltransferases near specific nucleosomes in target gene promoter regions, recognizing the acetylated lysine residue.

Halogen-Enriched Fragments

Halogen-Enriched Fragment LibraryOur Halogen-Enriched Fragment Library comprises 708 brominated fragments that can explore binding sites for favorable halogen bond interactions to identify unique binding modes that are complementary to those obtained from classical fragment-based screening.

Chelator Fragment Library

Chelator Fragments LibraryFragment-based lead design (FBLD) could be used to identify new metal-binding groups for metalloenzyme inhibitors. Several small-molecule chelators have been shown to effectively inhibit metalloproteins, therefore the design,

DNMTs Targeted Libraries

DNMT focused librariesEnzymes involved in the epigenetic regulation of the genome represent promising starting points for therapeutic intervention by small molecules, and DNA methyltransferases (DNMT) are emerging targets for the development of a new class of cancer therapeutics.

BRD4 Targeted Library

Bromodomain-containing Protein 4 (BRD4)Epigenetic regulators are new popular targets for cancer treatment. One of the promising epigenetic drug targets is Bromodomain-containing Protein 4 (BRD4) that binds to acetylated histone lysine residues and stimulates transcriptional elongation leading to expression of growth-promoting genes. 

General Fragments Library

Supplier stockUPDATED! The library has been just updated!
The central purpose of this specially designed Fragment Library is to provide

Hsp90 Targeted Library

Hsp90 focused libraryHsp90 (heat shock protein 90) is a highly abundant and ubiquitous molecular chaperone which plays an important role in the folding of newly synthesized proteins or stabilizing and refolding denatured proteins after stress. Its expression is associated with many types of tumors including breast cancer, pancreatic carcinoma, human leukemia and others.

Glycomimetic Focused Library

Glycomimetic Focused LibrarySeveral glycoprocessing enzymes and glycoreceptors have been recognized as important targets for therapeutic intervention. This concept has inspired the development of important classes of therapeutics, such as anti-influenza, anti-inflammatory, Gaucher’s disease, hepatitis and cancer drugs.

GCR Antagonist Library

Glucocorticoid Receptor Antagoniat focused libraryGlucocorticoids (GCs) are secreted from the adrenal gland in response to exposure to emotional and physiologic stressors and are responsible for modulating essential metabolic, cardiovascular, immune, and behavioral functions [1–3]. The glucocorticoid receptor (GR) belongs to a family of nuclear hormone receptors that are ligand-dependent transcription factors.

11β-HSD1 Targeted Library

11beta-hydroxysteroid dehydrogenase type I focused library11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1, cortisone reductase, HSD11B1, 11beta-hydroxysteroid dehydrogenase type 1,11beta-HSD1) is an enzyme that is involved in glucocorticoid regulation by catalyzing the conversion of inactive cortisone to its active form cortisol. These hormones regulate several physiological processes, and modulation of glucocorticoid action has been implicated as a potential treatment for a variety of diseases.

Histamine Receptor Antagonist Library

Histamine receptor focused libraryIt is generally acknowledged that histamine is an important regulator of a plethora of (patho) physiological conditions and exerts its actions through the interaction with four histamine receptor subtypes. All these receptors belong to the family of heptahelical GPCR's and are considered as a promising molecular targets for drug development.

HATs Targeted Library

Histone Acetyltransferase target-focused libraryPost-translational modifications, such as acetylation or phosphorylation, play a crucial role in the regulation of gene transcription in eukaryotes. Different subtypes of histone acetyltransferases (HATs) catalyze the acetylation of histones on specific lysine residues. 

Liver X Receptor Beta Library

Liver X receptor ? (LXR Beta) modulatorsLiver X receptors (LXRs) are nuclear receptors that regulate the metabolism of cholesterol and bile acids. LXRs function as nuclear cholesterol sensors that are activated in response to elevated intracellular cholesterol levels in multiple cell types.

HDAC Targeted Libraries

GPCR focused librariesClassical histone deacetylases (HDACs classes I, II, and IV) are a promising novel class of epigenetic anti-cancer drug targets. Inhibition of histone deacetylases results in hyperacetylation of histones and modulates gene expression by creating an open chromatin state that leads to expression of previously silenced genes.

DOT1L Targeted Library

GPCR focused librariesHistone methyltransferases are promising epigenetic drug targets. Several drugs that inhibit histone methyltransferases have been developed for anticancer therapy. DOT1L histone H3 methyltransferase methylates lysine 79 on histone H3 (H3K79), within the globular histone domain upon which DNA is wrapped.

inhib.jpgOTAVAchemicals offers a number of INHIBITORS and other biologically active compounds modulating activity of distinct macromolecular targets

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