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Assay Detail

CHEMBL3888858

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

Binding
Inhibition Assay: Reader: Synergy HT program: tyrosinase 280-490 kinetics: kinetics over 45 minutes, reading at t=10 minutes, Tests in transparent 96-well plates, Phosphate buffer (pH 6.8), Enzyme: mushroom tyrosinase (T-3824, Sigma), Substrate: L-tyrosine (T-3754, Sigma), Positive control: Kojic acid (KA) (60890, Fluka) (reference inhibitor). Reference Molecules for the Test: Kojic acid: 9 μM<IC50<20 μM (PPO), 3 &muM<IC50<7 μM (MPMO); Vitamin C: 20 μM<IC50<40 μM (PPO); Reduced glutathione: 55% inhibition at 25 μM (PPO), IC50=1-2 μM (MPMO); Hydroquinone: IC50=3-4 μM (MPMO); Arbutin: 57% inhibition at 88 μM (MPMO).
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Polyphenol oxidase 1 (CHEMBL3988582)
Type SINGLE PROTEIN
Organism Agaricus bisporus

Publication

Heterocyclic resorcinol derivatives, preparation of same and cosmetic uses thereof
(2016)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.00 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3965042 1 7.10
CHEMBL3901907 1 7.05
CHEMBL3961037 1 7.00
CHEMBL3894834 1 6.70
CHEMBL3921984 1 6.40
CHEMBL450195 RUCINOL 1 6.00
CHEMBL3985209 1 5.82
CHEMBL3983018 1 5.70
CHEMBL3895559 1 5.31
CHEMBL287556 KOJIC ACID 1 4.82
CHEMBL4109994 1 4.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3965042 IC50 = 80.0 nM 7.10
CHEMBL3901907 IC50 = 90.0 nM 7.05
CHEMBL3961037 IC50 = 100.0 nM 7.00
CHEMBL3894834 IC50 = 200.0 nM 6.70
CHEMBL3921984 IC50 = 400.0 nM 6.40
CHEMBL450195 RUCINOL IC50 = 1000.0 nM 6.00
CHEMBL3985209 IC50 = 1500.0 nM 5.82
CHEMBL3983018 IC50 = 2000.0 nM 5.70
CHEMBL3895559 IC50 = 4900.0 nM 5.31
CHEMBL287556 KOJIC ACID IC50 = 15000.0 nM 4.82
CHEMBL4109994 IC50 = 90000.0 nM 4.05