Analyzer · Sparsifire

Analyze how specific documents activate the features of the SAE. Select a dataset, a run and a document to begin.

Dataset

SAE Model

Document

Active Features

1551

MIN ACTIVATION

0.0

Details List

#708 Drug Resistance Mechanisms in Cancer

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#2972 Sensory-Motor Integration

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#2171 Molecular and Cellular Biological Processes

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#1424 Feature 1424

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#23 Neuronal Circuitry and Cellular Processes

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Document Content

2,4-Diaminopyrimidine inhibitors of c-Met kinase bearing benzoxazepine anilines.
Elaboration of the SAR around a series of 2,4-diaminopyrimidines led to a number of c-Met inhibitors in which kinase selectivity was modulated by substituents appended on the C4-aminobenzamide ring and the nature of the C2-aminoaryl ring. Further lead optimization of the C2-aminoaryl group led to benzoxazepine analogs whose pharmaceutical properties were modulated by the nature of the substituent on the benzoxazepine nitrogen. Tumor stasis (with partial regressions) were observed when an orally bioavailable analog was evaluated in a GTL-16 tumor xenograft mouse model. Subsequent PK/PD studies suggested that a metabolite contributed to the overall in vivo response.

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