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Assay Detail

CHEMBL5355298

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

Binding
Inhibition of tyrosinase in human MNT-1 cell lysates using L-DOPA as substrate assessed as reduction in melanin formation preincubated for 10 mins followed by substrate addition and measured by microplate reader analysis
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MNT-1
Subcellular Lysates
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Tyrosinase (CHEMBL1973)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Resorcinol-based hemiindigoid derivatives as human tyrosinase inhibitors and melanogenesis suppressors in human melanoma cells.
Roulier B, Rush I, Lazinski LM, Pérès B, Olleik H, Royal G, Fishman A, Maresca M, Haudecoeur R.
Eur J Med Chem (2023) 246 : 114972 -114972
PubMed 36462443 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 41 4.91 5.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5399906 1 5.80
CHEMBL5408197 1 5.80
CHEMBL5416835 1 5.64
CHEMBL5394983 1 5.47
CHEMBL5274383 1 5.24
CHEMBL5405017 1 5.24
CHEMBL5428256 1 5.23
CHEMBL1807311 1 5.19
CHEMBL1807492 1 5.16
CHEMBL1814444 1 5.11
CHEMBL5404839 1 5.09
CHEMBL450195 RUCINOL 1 5.08
CHEMBL5412546 1 4.93
CHEMBL5403418 1 4.90
CHEMBL3978212 1 4.82
CHEMBL5396899 1 4.82
CHEMBL5396212 1 4.75
CHEMBL5425960 1 4.74
CHEMBL5418068 1 4.72
CHEMBL1814434 1 4.60
CHEMBL5394207 1 4.50
CHEMBL5421537 1 4.32
CHEMBL373249 1 4.22
CHEMBL5418183 1 4.10
CHEMBL5427200 1 4.10
CHEMBL5405551 1 4.06
CHEMBL5420730 1 -
CHEMBL5400410 1 -
CHEMBL5426749 1 -
CHEMBL1374610 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5399906 IC50 = 1570.0 nM 5.80
CHEMBL5408197 IC50 = 1600.0 nM 5.80
CHEMBL5416835 IC50 = 2300.0 nM 5.64
CHEMBL5394983 IC50 = 3400.0 nM 5.47
CHEMBL5274383 IC50 = 5800.0 nM 5.24
CHEMBL5405017 IC50 = 5800.0 nM 5.24
CHEMBL5428256 IC50 = 5900.0 nM 5.23
CHEMBL1807311 IC50 = 6400.0 nM 5.19
CHEMBL1807492 IC50 = 6900.0 nM 5.16
CHEMBL1814444 IC50 = 7700.0 nM 5.11
CHEMBL5404839 IC50 = 8200.0 nM 5.09
CHEMBL450195 RUCINOL IC50 = 8300.0 nM 5.08
CHEMBL5412546 IC50 = 11800.0 nM 4.93
CHEMBL5403418 IC50 = 12700.0 nM 4.90
CHEMBL5396899 IC50 = 15000.0 nM 4.82
CHEMBL3978212 IC50 = 15000.0 nM 4.82
CHEMBL5396212 IC50 = 18000.0 nM 4.75
CHEMBL5425960 IC50 = 18400.0 nM 4.74
CHEMBL5418068 IC50 = 19000.0 nM 4.72
CHEMBL1814434 IC50 = 25000.0 nM 4.60
CHEMBL5394207 IC50 = 32000.0 nM 4.50
CHEMBL5421537 IC50 = 48000.0 nM 4.32
CHEMBL373249 IC50 = 60000.0 nM 4.22
CHEMBL5418183 IC50 = 80000.0 nM 4.10
CHEMBL5427200 IC50 = 80000.0 nM 4.10
CHEMBL5405551 IC50 = 88000.0 nM 4.06
CHEMBL5411705 IC50 > 100000.0 nM -
CHEMBL5426205 IC50 > 100000.0 nM -
CHEMBL5435799 IC50 > 100000.0 nM -
CHEMBL1172321 IC50 > 100000.0 nM -
CHEMBL5432681 IC50 > 100000.0 nM -
CHEMBL5399513 IC50 > 100000.0 nM -
CHEMBL287556 KOJIC ACID IC50 > 100000.0 nM -
CHEMBL5404928 IC50 > 100000.0 nM -
CHEMBL5400587 IC50 > 100000.0 nM -
CHEMBL5397672 IC50 > 100000.0 nM -
CHEMBL5423130 IC50 > 100000.0 nM -
CHEMBL1374610 IC50 > 100000.0 nM -
CHEMBL5426749 IC50 > 100000.0 nM -
CHEMBL5400410 IC50 > 100000.0 nM -
CHEMBL5420730 IC50 > 100000.0 nM -