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BioAssay: AID 331283

Inhibition of melanin production in mouse B16 cells at 100 uM

A series of N-hydroxy-N'-phenylthiourea and N-hydroxy-N'-phenylurea analogues were prepared and evaluated as inhibitors of tyrosinase and melanin formation. The most active analogue 1 inhibited mushroom tyrosinase with an IC(50) of around 0.29 microM and also retained a substantial potency in cell culture by reducing pigment synthesis by 78%. Therefore, compound 1 could be considered as a promising candidate for preclinical drug development for skin hyperpigmentation application. ..more
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 Tested Compounds
 Tested Compounds
All(24)
 
 
Inactive(10)
 
 
Inconclusive(4)
 
 
Unspecified(10)
 
 
 Tested Substances
 Tested Substances
All(24)
 
 
Inactive(10)
 
 
Inconclusive(4)
 
 
Unspecified(10)
 
 
 Related BioAssays
 Related BioAssays
AID: 331283
Data Source: ChEMBL (479309)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-25
Modify Date: 2013-11-20

Data Table ( Complete ):           All
Tested Compounds:
Description:
Title: Analogues of N-hydroxy-N'-phenylthiourea and N-hydroxy-N'-phenylurea as inhibitors of tyrosinase and melanin formation.

Abstract: A series of N-hydroxy-N'-phenylthiourea and N-hydroxy-N'-phenylurea analogues were prepared and evaluated as inhibitors of tyrosinase and melanin formation. The most active analogue 1 inhibited mushroom tyrosinase with an IC(50) of around 0.29 microM and also retained a substantial potency in cell culture by reducing pigment synthesis by 78%. Therefore, compound 1 could be considered as a promising candidate for preclinical drug development for skin hyperpigmentation application.
(PMID: 18501598)
Comment
Putative Target:

ChEMBL Target ID: 80035
Target Type: CELL-LINE
Cell Line: B16
Tissue: Melanoma cells
Pref Name: B16
Organism: Mus musculus
Tax ID: 10090
Confidence: Target assigned is non-molecular
Relationship Type: Non-molecular target assigned
Categorized Comment
ChEMBL Assay Type: Functional

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Assay Cell Type: B16

Result Definitions
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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
6Inhibition activity commentInhibition activity commentString
7Inhibition standard flagInhibition standard flagInteger
8Inhibition qualifierInhibition qualifierString
9Inhibition published valueInhibition published valueFloat%
10Inhibition standard valueInhibition standard valueFloat%

Data Table (Concise)
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