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Assay Detail

CHEMBL4402617

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Binding
Inhibition of monophenolase activity of mushroom tyrosinase assessed as inhibition constant for free enzyme-inhibitor complex by measuring reduction in dopachrome formation using L-Tyrosine substrate by UV-Vis spectrophotometry
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Agaricus bisporus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Tyrosinase (CHEMBL3318)
Type SINGLE PROTEIN
Organism Agaricus bisporus

Publication

Tyrosinase inhibitory study of flavonolignans from the seeds of Silybum marianum (Milk thistle).
Kim JY, Kim JY, Jenis J, Li ZP, Ban YJ, Baiseitova A, Park KH.
Bioorg Med Chem (2019) 27 : 2499 -2507
PubMed 30871862 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 5.68 6.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL9509 SILIBININ 3.0 1 6.16
CHEMBL592676 ISOSILYBIN A 1 5.96
CHEMBL2397733 SILIDIANIN 2.0 1 5.68
CHEMBL130493 SILICRISTIN A 1 5.68
CHEMBL589325 SILICRISTIN B 1 5.55
CHEMBL3542340 ISOSILYBIN B 1 5.37
CHEMBL4076992 1 5.34
CHEMBL287556 KOJIC ACID 1 -
CHEMBL66 (+)-TAXIFOLIN 1 -
CHEMBL9323 DIHYDROKAEMPFEROL 1 -
CHEMBL9353 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL9509 SILIBININ Ki = 700.0 nM 6.16
CHEMBL592676 ISOSILYBIN A Ki = 1100.0 nM 5.96
CHEMBL2397733 SILIDIANIN Ki = 2100.0 nM 5.68
CHEMBL130493 SILICRISTIN A Ki = 2100.0 nM 5.68
CHEMBL589325 SILICRISTIN B Ki = 2800.0 nM 5.55
CHEMBL3542340 ISOSILYBIN B Ki = 4300.0 nM 5.37
CHEMBL4076992 Ki = 4600.0 nM 5.34
CHEMBL287556 KOJIC ACID Ki - -
CHEMBL66 (+)-TAXIFOLIN Ki - -
CHEMBL9323 DIHYDROKAEMPFEROL Ki - -
CHEMBL9353 Ki - -