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BioAssay: AID 44016

Concentration required to inhibit growth of CCRF-CEM cells in culture for 72 hr to 50% of control growth

A series of diarylsulfonylureas with exceptionally broad-spectrum activity against syngeneic rodent solid tumors in vivo is described. Their discovery resulted from a program dedicated to in vivo screening for novel oncolytics in solid tumor models, rather than traditional ascites leukemia models. The structures, oral efficacy, side-effect profile, and mechanism of action of these sulfonylureas more ..
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 Tested Compounds
 Tested Compounds
All(138)
 
 
Unspecified(138)
 
 
 Tested Substances
 Tested Substances
All(138)
 
 
Unspecified(138)
 
 
 Related BioAssays
 Related BioAssays
AID: 44016
Data Source: ChEMBL (41152)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-21
Modify Date: 2014-05-19

Data Table ( Complete ):           View All Data
Tested Compounds:
Description:
Title: Novel agents effective against solid tumors: the diarylsulfonylureas. Synthesis, activities, and analysis of quantitative structure-activity relationships.

Abstract: A series of diarylsulfonylureas with exceptionally broad-spectrum activity against syngeneic rodent solid tumors in vivo is described. Their discovery resulted from a program dedicated to in vivo screening for novel oncolytics in solid tumor models, rather than traditional ascites leukemia models. The structures, oral efficacy, side-effect profile, and mechanism of action of these sulfonylureas appear to be distinct from previously known classes of oncolytics. An extensive series of analogues was prepared to probe structure-activity relationships (SAR), with particular focus on the substituent patterns of each aryl domain. Quantitative analysis of these substituent SARs, using the method of cluster significance analysis, showed the lipophilicity of the substituents to be the dominant determinant of activity. One compound from the series, LY186641 (104, sulofenur), has progressed to Phase I clinical trials as an antitumor drug.
(PMID: 2391684)
Comment
Putative Target:
ChEMBL Target ID: 80064
Target Type: CELL-LINE
Cell Line: CCRF-CEM
Tissue: T-cell leukemia
Pref Name: CCRF-CEM
Organism: Homo sapiens
Tax ID: 9606
Confidence: Target assigned is non-molecular
Relationship Type: Non-molecular target assigned
Categorized Comment - additional comments and annotations
From ChEMBL:
Assay Type: Functional
Assay Data Source: Scientific Literature
BAO: Assay Format: cell-based format
Assay Cell Type: CCRF-CEM
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1IC50 activity commentIC50 activity commentString
2IC50 standard flagIC50 standard flagInteger
3IC50 qualifierIC50 qualifierString
4IC50 published valueIC50 published valueFloatug ml-1
5IC50 standard valueIC50 standard valueFloatug.mL-1

Data Table (Concise)
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