Thieno[2,3-b]pyridines as negative allosteric modulators of metabotropic GluR5 receptors: Lead optimization

Bioorganic and Medicinal Chemistry Letters

Volumn 25, Issue 8, 2015, Pages 1724-1729

  Nógrádi, Katalin ^a   Wágner, Gábor ^a   Domány, György ^a   Bobok, Amrita ^a   Magdó, Ildikó ^a   Kolok, Sándor ^a   Mikó Bakk, Mónika L ^a   Vastag, Mónika ^a   Sághy, Katalin ^a   Gyertyán, István ^a   Kóti, János ^a   Gál, Krisztina ^a   Farkas, Sándor ^a   Keseru, György M ^a   Greiner, István ^a   Szombathelyi, Zsolt ^a  

^a GEDEON RICHTER LTD   (Hungary)

Author keywords

mGluR5; Negative allosteric modulator; Thieno 2,3 b pyridines

Indexed keywords

METABOTROPIC RECEPTOR 5; PROTEIN BINDING; PYRIMIDINE DERIVATIVE; THIENO(2,3-D)PYRIMIDINE;

ALLOSTERISM; ANIMAL; CHEMISTRY; HIGH THROUGHPUT SCREENING; HUMAN; METABOLISM; RAT; STRUCTURE ACTIVITY RELATION;

ALLOSTERIC REGULATION; ANIMALS; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; PROTEIN BINDING; PYRIMIDINES; RATS; RECEPTOR, METABOTROPIC GLUTAMATE 5; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84939995735     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2015.02.073     Document Type: Article

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25. M = affinity constant of substrate concentration; V = actual rate of enzyme reaction under first order conditions
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