Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptor
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- Modify:2022-08-30
Title: Endothelin antagonists: evaluation of 2,1,3-benzothiadiazole as a methylendioxyphenyl bioisoster.
Abstract: The methylendioxyphenyl group is present in a number of endothelin receptor antagonists thus far reported. By means of a Kohonen neural network we discovered with a benzothiadiazole a bioisosteric replacement instead. This group should be devoid of the negative metabolic interactions with cytochrome P450 ascribed to methylendioxyphenyl in vivo. The synthesis of a potent benzothiadiazole analogue EMD 122801 together with in vitro studies of different methylendioxyphenyl, benzothiadiazole and benzofurazan derivatives is described.
Compounds with activity <= 10uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.
Journal: Bioorg Med Chem Lett
Year: 1998
Volume: 8
Issue: 1
First Page: 17
Last Page: 22
DOI: 10.1016/s0960-894x(97)10151-2
Target ChEMBL ID: CHEMBL1785
ChEMBL Target Name: Endothelin receptor ET-B
ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain
Relationship Type: H - Homologous protein target assigned
Confidence: Homologous single protein target assigned
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