Title : Discovery of tricyclic indoles that potently inhibit Mcl-1 using fragment-based methods and structure-based design.

Pub. Date : 2015 May 14

PMID : 25844895






1 Functional Relationships(s)
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1 Here, we describe the discovery of potent tricyclic 2-indole carboxylic acid inhibitors that exhibit single digit nanomolar binding affinity to Mcl-1 and greater than 1700-fold selectivity over Bcl-xL and greater than 100-fold selectivity over Bcl-2. indole-2-carboxylic acid MCL1 apoptosis regulator, BCL2 family member Homo sapiens