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Assay Detail

CHEMBL4723101

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

Binding
Inhibition of human His-tagged tyrosinase expressed in HEK 293 cells using L-DOPA as substrate by MBTH based assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Tyrosinase (CHEMBL1973)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Advances in the Design of Genuine Human Tyrosinase Inhibitors for Targeting Melanogenesis and Related Pigmentations.
Roulier B,Pérès B,Haudecoeur R
J Med Chem (2020) 63 : 13428 -13443
PubMed 32787103 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 4.89 5.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4743159 1 5.96
CHEMBL450195 RUCINOL 1 4.68
CHEMBL443605 HEXYLRESORCINOL -1.0 1 4.03
CHEMBL537 HYDROQUINONE 4.0 1 -
CHEMBL287556 KOJIC ACID 1 -
CHEMBL3961037 1 -
CHEMBL232202 ARBUTIN 2.0 1 -
CHEMBL24147 RESORCINOL -1.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4743159 IC50 = 1100.0 nM 5.96
CHEMBL450195 RUCINOL IC50 = 21000.0 nM 4.68
CHEMBL443605 HEXYLRESORCINOL IC50 = 94000.0 nM 4.03
CHEMBL537 HYDROQUINONE IC50 = 4400000.0 nM -
CHEMBL287556 KOJIC ACID IC50 = 500000.0 nM -
CHEMBL3961037 IC50 = 131000.0 nM -
CHEMBL232202 ARBUTIN IC50 = 6500000.0 nM -
CHEMBL24147 RESORCINOL IC50 > 3000000.0 nM -