Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 1

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 3, 2010, Pages 1177-1180

  Rist, Øystein ^a   Grimstrup, Marie ^a   Receveur, Jean Marie ^a   Frimurer, Thomas M ^a   Ulven, Trond ^a   Kostenis, Evi ^a   Högberg, Thomas ^a  

^a 7TM Pharma A S   (Denmark)

Author keywords

[No Author keywords available]

Indexed keywords

ACETIC ACID DERIVATIVE; ANTIINFLAMMATORY AGENT; CHEMOATTRACTANT RECEPTOR HOMOLOGOUS MOLECULE EXPRESSED ON TH2 CELLS ANTAGONIST; PROSTAGLANDIN D2 DERIVATIVE; THIAZOLEACETIC ACID; UNCLASSIFIED DRUG; ACETIC ACID; IMMUNOGLOBULIN RECEPTOR; PEPTIDE LIBRARY; PROSTAGLANDIN D2 RECEPTOR; PROSTAGLANDIN RECEPTOR; PROTEIN BINDING; THIAZOLE DERIVATIVE;

ALLERGIC DISEASE; ARTICLE; ASTHMA; BINDING AFFINITY; CELL STRAIN COS7; CHEMICAL STRUCTURE; CHRONIC OBSTRUCTIVE LUNG DISEASE; COMPUTER MODEL; HUMAN; HUMAN CELL; IC 50; PHARMACOPHORE; PROTEIN EXPRESSION; RHINOCONJUNCTIVITIS; STRUCTURE ACTIVITY RELATION; TH2 CELL; ANIMAL; ANTAGONISTS AND INHIBITORS; CHLOROCEBUS AETHIOPS; COMPARATIVE STUDY; COS 1 CELL LINE; METABOLISM; PEPTIDE LIBRARY; PHYSIOLOGY; SYNTHESIS;

ACETIC ACID; ANIMALS; CERCOPITHECUS AETHIOPS; COS CELLS; HUMANS; PEPTIDE LIBRARY; PROTEIN BINDING; RECEPTORS, IMMUNOLOGIC; RECEPTORS, PROSTAGLANDIN; THIAZOLES;

EID: 74049109689     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.12.008     Document Type: Article

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26. 2 was then added to each well to elicit about 75-80% of the maximal agonist efficacy and cells were further incubated for 5 min. After the incubation period, the 96-well microplate was placed in the Mithras LB 940 instrument and DeepBlueC coelenterazine was injected to one well at a time. Five seconds after the injection, the light output from the well was measured sequentially at 400 nm and 515 nm. The BRET signal was calculated by the ratio of the fluorescence emitted by GFP2-β-arr2 (515 nm) over the light emitted by the receptor-Rluc (400 nm).