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Assay Detail

CHEMBL5506766

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of tyrosinase in human MNT-1 cells using L-DOPA as substrate preincubated for 10 mins followed by substrate addition measured after 180 mins by absorbance based spectramax microplate reader assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MNT-1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Tyrosinase (CHEMBL1973)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of 4-amino-2',4'-dihydroxyindanone derivatives as potent inhibitors of tyrosinase and melanin biosynthesis in human melanoma cells.
Lazinski LM, Beaumet M, Roulier B, Gay R, Royal G, Maresca M, Haudecoeur R.
Eur J Med Chem (2024) 266 : 116165 -116165
PubMed 38262119 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 5.72 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5562348 1 6.85
CHEMBL5558420 1 6.82
CHEMBL4743159 1 6.77
CHEMBL5555033 1 6.75
CHEMBL5566780 1 6.46
CHEMBL5556099 1 6.14
CHEMBL5557086 1 6.07
CHEMBL5557324 1 6.05
CHEMBL5558083 1 5.75
CHEMBL5566466 1 5.70
CHEMBL5527846 1 5.50
CHEMBL5555075 1 5.36
CHEMBL5558133 1 5.05
CHEMBL5563317 1 4.82
CHEMBL5567977 1 4.62
CHEMBL5557491 1 4.30
CHEMBL5532313 1 4.18
CHEMBL5532330 1 -
CHEMBL287556 KOJIC ACID 1 -
CHEMBL5560542 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5562348 IC50 = 140.0 nM 6.85
CHEMBL5558420 IC50 = 150.0 nM 6.82
CHEMBL4743159 IC50 = 170.0 nM 6.77
CHEMBL5555033 IC50 = 180.0 nM 6.75
CHEMBL5566780 IC50 = 350.0 nM 6.46
CHEMBL5556099 IC50 = 720.0 nM 6.14
CHEMBL5557086 IC50 = 850.0 nM 6.07
CHEMBL5557324 IC50 = 890.0 nM 6.05
CHEMBL5558083 IC50 = 1800.0 nM 5.75
CHEMBL5566466 IC50 = 2000.0 nM 5.70
CHEMBL5527846 IC50 = 3200.0 nM 5.50
CHEMBL5555075 IC50 = 4400.0 nM 5.36
CHEMBL5558133 IC50 = 9000.0 nM 5.05
CHEMBL5563317 IC50 = 15000.0 nM 4.82
CHEMBL5567977 IC50 = 24000.0 nM 4.62
CHEMBL5557491 IC50 = 50000.0 nM 4.30
CHEMBL5532313 IC50 = 66000.0 nM 4.18
CHEMBL5532330 IC50 > 100000.0 nM -
CHEMBL287556 KOJIC ACID IC50 > 100000.0 nM -
CHEMBL5560542 IC50 > 100000.0 nM -