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Assay Detail

CHEMBL4430738

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

Binding
Activation of mushroom tyrosinase using L-tyrosine as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by ELISA
30
Total Activities
30
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

Synthesis and bioactivity of novel isoxazole chalcone derivatives on tyrosinase and melanin synthesis in murine B16 cells for the treatment of vitiligo.
Niu C, Yin L, Nie LF, Dou J, Zhao JY, Li G, Aisa HA.
Bioorg Med Chem (2016) 24 : 5440 -5448
PubMed 27622747 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 30 4.83 5.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4475422 1 5.89
CHEMBL4440265 1 5.77
CHEMBL4465047 1 5.60
CHEMBL4464052 1 5.52
CHEMBL4470012 1 5.25
CHEMBL4522700 1 5.19
CHEMBL4545495 1 5.09
CHEMBL4469401 1 5.02
CHEMBL4463325 1 4.94
CHEMBL4460236 1 4.92
CHEMBL4581303 1 4.90
CHEMBL4462337 1 4.84
CHEMBL416 METHOXSALEN 4.0 1 4.83
CHEMBL4473442 1 4.77
CHEMBL4559940 1 4.68
CHEMBL4466784 1 4.67
CHEMBL4453720 1 4.62
CHEMBL4462990 1 4.62
CHEMBL4567344 1 4.59
CHEMBL3409828 1 4.59
CHEMBL4548215 1 4.54
CHEMBL4468479 1 4.51
CHEMBL4446279 1 4.45
CHEMBL4592732 1 4.43
CHEMBL4594133 1 4.33
CHEMBL4469461 1 4.25
CHEMBL4522932 1 4.18
CHEMBL4471626 1 4.11
CHEMBL4542422 1 -
CHEMBL4473153 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4475422 EC50 = 1300.0 nM 5.89
CHEMBL4440265 EC50 = 1710.0 nM 5.77
CHEMBL4465047 EC50 = 2500.0 nM 5.60
CHEMBL4464052 EC50 = 3000.0 nM 5.52
CHEMBL4470012 EC50 = 5600.0 nM 5.25
CHEMBL4522700 EC50 = 6400.0 nM 5.19
CHEMBL4545495 EC50 = 8100.0 nM 5.09
CHEMBL4469401 EC50 = 9600.0 nM 5.02
CHEMBL4463325 EC50 = 11400.0 nM 4.94
CHEMBL4460236 EC50 = 11900.0 nM 4.92
CHEMBL4581303 EC50 = 12700.0 nM 4.90
CHEMBL4462337 EC50 = 14600.0 nM 4.84
CHEMBL416 METHOXSALEN EC50 = 14800.0 nM 4.83
CHEMBL4473442 EC50 = 17100.0 nM 4.77
CHEMBL4559940 EC50 = 21100.0 nM 4.68
CHEMBL4466784 EC50 = 21300.0 nM 4.67
CHEMBL4453720 EC50 = 23800.0 nM 4.62
CHEMBL4462990 EC50 = 23900.0 nM 4.62
CHEMBL4567344 EC50 = 25500.0 nM 4.59
CHEMBL3409828 EC50 = 25800.0 nM 4.59
CHEMBL4548215 EC50 = 28900.0 nM 4.54
CHEMBL4468479 EC50 = 30600.0 nM 4.51
CHEMBL4446279 EC50 = 35600.0 nM 4.45
CHEMBL4592732 EC50 = 37400.0 nM 4.43
CHEMBL4594133 EC50 = 47200.0 nM 4.33
CHEMBL4469461 EC50 = 56200.0 nM 4.25
CHEMBL4522932 EC50 = 65300.0 nM 4.18
CHEMBL4471626 EC50 = 78100.0 nM 4.11
CHEMBL4542422 EC50 > 100000.0 nM -
CHEMBL4473153 EC50 > 100000.0 nM -