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BioAssay: AID 299460

Inhibition of Eg5 assessed as inhibition ATP hydrolysis by ATPase assay

Inhibition of Eg5 represents a novel approach for the treatment of cancer. Here, we report the synthesis and structure-activity relationship of S-trityl-L-cysteine (STLC) derivatives as Eg5 inhibitors. Some of these derivatives such as 4f demonstrated enhanced inhibitory activity against Eg5 and induced mitotic arrest with characteristic monoastral spindles in HeLa cells. ..more
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 Tested Compounds
 Tested Compounds
All(21)
 
 
Active(7)
 
 
Unspecified(14)
 
 
 Tested Substances
 Tested Substances
All(21)
 
 
Active(7)
 
 
Unspecified(14)
 
 
 Related BioAssays
 Related BioAssays
AID: 299460
Data Source: ChEMBL (447486)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-25
Modify Date: 2014-05-23

Data Table ( Complete ):           View Active Data    View All Data
BioActive Compounds: 7
Description:
Title: Synthesis and biological evaluation of L-cysteine derivatives as mitotic kinesin Eg5 inhibitors.

Abstract: Inhibition of Eg5 represents a novel approach for the treatment of cancer. Here, we report the synthesis and structure-activity relationship of S-trityl-L-cysteine (STLC) derivatives as Eg5 inhibitors. Some of these derivatives such as 4f demonstrated enhanced inhibitory activity against Eg5 and induced mitotic arrest with characteristic monoastral spindles in HeLa cells.
(PMID: 17524640)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Putative Target:

ChEMBL Target ID: 100166
Target Type: SINGLE PROTEIN
Pref Name: Kinesin-like protein 1
Synonyms: Kinesin-like protein 1;Kinesin-like protein KIF11;Kinesin-like spindle protein HKSP;Kinesin-related motor protein Eg5;Thyroid receptor-interacting protein 5;TR-interacting protein 5;TRIP-5;
Gene Name: EG5 ;KIF11;KNSL1;TRIP5;
Protein Accession: P52732;
Protein GI: 116242604;
Organism: Homo sapiens
Tax ID: 9606
Target Classification: cytosolic other
Confidence: Homologous single protein target assigned
Relationship Type: Homologous protein target assigned
Categorized Comment - additional comments and annotations
From ChEMBL:
Assay Type: Functional
Assay Data Source: Scientific Literature
Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1IC50*IC50 PubChem standard valueFloatμM
2IC50 activity commentIC50 activity commentString
3IC50 standard flagIC50 standard flagInteger
4IC50 qualifierIC50 qualifierString
5IC50 published valueIC50 published valueFloatμM
6IC50 standard valueIC50 standard valueFloatnM
7Inhibition activity commentInhibition activity commentString
8Inhibition standard flagInhibition standard flagInteger
9Inhibition qualifierInhibition qualifierString
10Inhibition published valueInhibition published valueFloat%
11Inhibition standard valueInhibition standard valueFloat%

* Activity Concentration.

Data Table (Concise)
Data Table ( Complete ):     View Active Data    View All Data
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