U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 1151 - 1160 of 2596 results

Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

A-286982 was discovered as a potent, allosteric inhibitor of LFA-1/ICAM-1 interaction, it is known, that A-286982 binds to the IDAS (I domain allosteric site of LFA-1). Lymphocyte function-associated antigen-1 (LFA-1) is a member of leukocyte integrins family and involves in T cells binding to antigen presenting cells. Intracellular adhesion molecule-1 (ICAM-1) is a type of intercellular adhesion molecule and plays a pivotal role in cell-cell interactions. LFA-1/ICAM-1 interaction plays an important role in the pathogenesis of inflammatory disease.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

D-cloprostenol, also called (+)-cloprostenol is a highly potent prostaglandin F2-alpha receptor agonist. (+)-Cloprostenol is a 15(R) enantiomer of cloprostenol responsible for the majority of its biological activity and is commonly used in bovine reproduction that increases myometral contractility.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)

Conditions:

Colocynthin is the active medicinal principle of colocynth; a bitter, yellow, crystalline substance, regarded as a glucoside. Colocynthin is cytotoxic with respect to HeLa cells.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Thiadiazole-pyridazine derivative MF-438 has been identified as a potent stearoyl-CoA desaturase 1 (SCD1) inhibitor. Recently it has been shown that the upregulation of lung-cancer stem cell (CSC) markers can be reverted with a combination of MF-438 and cisplatin. The combination of MF-438 and cisplatin strongly synergizes the inhibition of 3D spheroid formation and induces CSC apoptosis.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)

Conditions:

Levofloxacin Q-acid is an intermediate of Levofloxacin, - an inhibitor of bacterial DNA gyrase and topoisomerase IV with a minimum inhibitory concentration (MIC) of 0.75 ug/mL against penicillin-resistant Streptococcus pneumoniae.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

6-ketocholestanol (5 alpha-Cholestan-3 beta-ol-6-one), a compound increases the membrane dipole potential, it was shown that 6-ketocholestanol was incorporated into unilamellar liposomes and was used as a skin pre-treatment. There was a positive effect of 6-ketocholestanol on the sodium-fluorescein diffusion in all skin types.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

p-Cresyl Acetate is used in formulating perfumeries, fragrances, and disinfectants. p-Cresyl acetate is used as the starting material for the synthesis of 2-acetyl-4-methylphenol.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)

Conditions:

Lysergide (LSD) is a semi-synthetic hallucinogen and is one of the most potent drugs known. Recreational use became popular between the 1960s to 1980s, but is now less common. During the 1960s, LSD was investigated for a variety of psychiatric indications, including the following: as an aid in the treatment of schizophrenia; as a means of creating a "model psychosis"; as a direct antidepressant; and as an adjunct to psychotherapy. LSD is listed in Schedule I of the United Nations 1971 Convention on Psychotropic Substances. LSD possesses a complex pharmacological profile that includes direct activation of serotonin, dopamine and norepinephrine receptors. In addition, one of its chief sites of action is that of compound-specific (“allosteric”) alterations in secondary messengers associated with 5HT2A and 5HT2C receptor activation and changes in gene expression. The hallucinogenic effects of LSD are likely due to agonism at 5HT2A and 5HT2C receptors. LSD is also an agonist at the majority of known serotonin receptors, including 5HT1A, 5HT1B, 5HT1D, 5HT5A, 5HT6 and 5HT7 receptors. L-Lysergide (L-LSD) is a non-psychoactive enantiomer of LSD. D-LSD not only completely eradicated the response to 10 muM dopamine in rat hippocampus preparations but also consistently stimulated adenylate cyclase activity. L-LSD (80 muM) was without effect. Also both D- and L-LSD bind to solubilized 5-HT1 sites with comparable high affinities, whereas D-LSD has a markedly higher affinity for the membrane 5-HT1 site. In crude bovine frontal cortical membranes, D-LSD has high affinity for the 5-HT 1 binding site (IC50 = 40 nM), while L-LSD has the very low affinity (IC50 = 10,000 nM versus [3H]5-HT). Solubilized 5-HT1 sites retain high affinity for D-LSD binding site (IC50 = 75 nM). However, L-LSD also has a high affinity for the soluble binding site (IC50 of 200 nM). Thus while the membrane-bound binding site strongly differentiates between D- and L-LSD, both stereoisomers bind to the soluble binding site with relatively high affinity. Lovell and Freedman have suggested that the lone-pair electrons on the 3 nitrogen atoms in D-LSD are oriented downward from the plane of the molecule and form a tripod of electron donor pairs which interact with the 5-HT 1 binding site. This area of attachment of D-LSD would be expected to be much larger than the area of attachment of 5-HT to the binding site, and to overlap or encompass the 5- HT binding region. The lower affinity of L-LSD for the membrane binding site would be due to the fact that one or more of the lone-pair electrons is oriented above the plane of the molecule. The diethylamide group of L-LSD would also be oriented differently. It would therefore either be unavailable for interactions with the binding site or its orientation would be a steric hindrance to binding.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Nystatin A1 is the one of the first member of important class of a macrocyclic polyene and poly-ol antibiotics isolated from Streptomyces noursei in 1950. Nystatin A1 binds to ergosterol, a major component of the fungal cell membrane. When present in sufficient concentrations, it forms pores in the membrane that lead to K+ leakage, acidification, and death of the fungus. Nystatin A1 is major component of Nystatin an important antifungal antibiotic, which for over half a century has been broadly used in medicine for the treatment of topical fungal infections caused by a broad spectrum of fungal pathogens comprising yeast-like and filamentous species.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

17β-Carboxyandrost-4-en-3-one is an intermediate in the synthesis of the drugs Dutasteride (D735000) and Finasteride. 17β-Carboxyandrost-4-en-3-one shows weak inhibition of Steroid 5-alpha-reductase and Androgen Receptor antagonism.

Showing 1151 - 1160 of 2596 results