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Assay Detail

CHEMBL5506765

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

Binding
Inhibition of mushroom tyrosinase using L-DOPA as substrate preincubated for 10 mins followed by substrate addition measured after 10 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 Agaricus bisporus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Mushroom tyrosinase (CHEMBL6066154)
Type PROTEIN FAMILY
Organism Agaricus bisporus

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 6.99 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5555033 1 8.22
CHEMBL5562348 1 8.05
CHEMBL5557324 1 7.85
CHEMBL5558420 1 7.85
CHEMBL5563317 1 7.72
CHEMBL5556099 1 7.57
CHEMBL5566780 1 7.22
CHEMBL5567977 1 7.08
CHEMBL5532313 1 7.07
CHEMBL5408197 1 7.05
CHEMBL5555075 1 7.00
CHEMBL5558133 1 6.82
CHEMBL5558083 1 6.80
CHEMBL5532330 1 6.80
CHEMBL5560542 1 6.75
CHEMBL5557491 1 6.58
CHEMBL5566466 1 6.41
CHEMBL5527846 1 6.34
CHEMBL5557086 1 6.22
CHEMBL287556 KOJIC ACID 1 4.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5555033 IC50 = 6.0 nM 8.22
CHEMBL5562348 IC50 = 9.0 nM 8.05
CHEMBL5557324 IC50 = 14.0 nM 7.85
CHEMBL5558420 IC50 = 14.0 nM 7.85
CHEMBL5563317 IC50 = 19.0 nM 7.72
CHEMBL5556099 IC50 = 27.0 nM 7.57
CHEMBL5566780 IC50 = 60.0 nM 7.22
CHEMBL5567977 IC50 = 83.0 nM 7.08
CHEMBL5532313 IC50 = 86.0 nM 7.07
CHEMBL5408197 IC50 = 90.0 nM 7.05
CHEMBL5555075 IC50 = 100.0 nM 7.00
CHEMBL5558133 IC50 = 150.0 nM 6.82
CHEMBL5558083 IC50 = 160.0 nM 6.80
CHEMBL5532330 IC50 = 160.0 nM 6.80
CHEMBL5560542 IC50 = 180.0 nM 6.75
CHEMBL5557491 IC50 = 260.0 nM 6.58
CHEMBL5566466 IC50 = 390.0 nM 6.41
CHEMBL5527846 IC50 = 460.0 nM 6.34
CHEMBL5557086 IC50 = 600.0 nM 6.22
CHEMBL287556 KOJIC ACID IC50 = 33000.0 nM 4.48