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BioAssay: AID 497308

Cytotoxicity against mouse Melan-a cells assessed as cell viability at 30 uM

On the basis of a hit from random screening, biaryl amide derivatives were prepared in a combinatorial manner via parallel solution-phase synthesis, and their effects on melanocytes were investigated to discover new effective skin depigmenting agents. Among the 120 derivatives prepared, five members exhibited a >30% reduction of melanin production at 30 microM with a cell viability of >90%. more ..
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 Tested Compounds
 Tested Compounds
All(122)
 
 
Unspecified(122)
 
 
 Tested Substances
 Tested Substances
All(122)
 
 
Unspecified(122)
 
 
 Related BioAssays
 Related BioAssays
AID: 497308
Data Source: ChEMBL (647348)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2011-02-25
Modify Date: 2014-08-24

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Tested Compounds:
Description:
Title: Identification of a potent and noncytotoxic inhibitor of melanin production.

Abstract: On the basis of a hit from random screening, biaryl amide derivatives were prepared in a combinatorial manner via parallel solution-phase synthesis, and their effects on melanocytes were investigated to discover new effective skin depigmenting agents. Among the 120 derivatives prepared, five members exhibited a >30% reduction of melanin production at 30 microM with a cell viability of >90%. In particular, compound A(3)/B(5) exhibited effective inhibitory activity on melanin synthesis. Although the inhibition percentage of A(3)/B(5) was slightly lower than that of the positive reference compound, phenylthiourea (PTU), A(3)/B(5) demonstrated a much better cell viability than PTU. In vivo evaluation of A(3)/B(5) also showed a significant decrease of melanin pigments. In addition, the in silico classification model was built based on the experimental data of library members. Our results suggest that these biaryl amide derivatives may act as potent skin depigmenting agents.
(PMID: 20615711)
Comment
Putative Target:

ChEMBL Target ID: 22224
Target Type: ADMET
Pref Name: ADMET
Confidence: Default value - Target unknown or has yet to be assigned
Relationship Type: Default value - Target has yet to be curated
Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay Type: ADME
Assay Data Source: Scientific Literature
BAO: Assay Format: cell-based format
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Activity activity commentActivity activity commentString
2Activity standard flagActivity standard flagInteger
3Activity qualifierActivity qualifierString
4Activity published valueActivity published valueFloat%
5Activity standard valueActivity standard valueFloat%

Data Table (Concise)
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