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BioAssay: AID 626569

Inhibition of mushroom tyrosinase activity using L-tyrosine as substrate at 10 uM by spectrometric analysis

Effect of a series of 1-phenylthioureas 1a-k and 1,3-disubstituted thioureas 2a-k were evaluated against melanin formation in melanoma B16 cell line and mushroom tyrosinase. Inhibitory activity of tyrosinase of 1-phenylthioureas 1a-k is parallel to their melanogenic inhibition. Thus, the melanogenic inhibition in melanoma B16 cells of 1-phenylthioureas could be the result of inhibition of more ..
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 Tested Compounds
 Tested Compounds
All(23)
 
 
Unspecified(23)
 
 
 Tested Substances
 Tested Substances
All(23)
 
 
Unspecified(23)
 
 
 Related BioAssays
 Related BioAssays
AID: 626569
Data Source: ChEMBL (776075)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-09-09
Modify Date: 2014-08-25

Data Table ( Complete ):           View All Data
Target
Sequence: RecName: Full=Polyphenol oxidase 2; Short=PPO2; Short=Phenolase 2; AltName: Full=Cresolase 2; AltName: Full=Tyrosinase 2; Flags: Precursor
Description ..   
Protein Family: Common central domain of tyrosinase
Comment ..   

Related Protein 3D Structures     More BioActivity Data..
Tested Compounds:
Description:
Title: Structural requirement of phenylthiourea analogs for their inhibitory activity of melanogenesis and tyrosinase.

Abstract: Effect of a series of 1-phenylthioureas 1a-k and 1,3-disubstituted thioureas 2a-k were evaluated against melanin formation in melanoma B16 cell line and mushroom tyrosinase. Inhibitory activity of tyrosinase of 1-phenylthioureas 1a-k is parallel to their melanogenic inhibition. Thus, the melanogenic inhibition in melanoma B16 cells of 1-phenylthioureas could be the result of inhibition of tyrosinase. However, 1,3-diaryl or 1-phenyl-3-alkylthioureas, 2a-k, appears as melanogenic inhibitor without inhibition of tyrosinase. The molecular docking study of 1e and 2b to binding pocket of tyrosinase provided convincing explanation regarding the necessity of direct connection of planar phenyl to thiourea unit without N'-substitution of phenylthioureas 1 as tyrosinase inhibitor and 2 as non-tyrosinase inhibitor.
(PMID: 21978680)
Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay Type: Binding
Target Type: Target is a single protein chain
Assay Data Source: Scientific Literature
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Inhibition activity commentInhibition activity commentString
2Inhibition standard flagInhibition standard flagInteger
3Inhibition qualifierInhibition qualifierString
4Inhibition published valueInhibition published valueFloat%
5Inhibition standard valueInhibition standard valueFloat%

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