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Assay Detail

CHEMBL5355299

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

Binding
Inhibition of C-terminal His-tagged truncated form of human tyrosinase (1 to 456 residues) expressed in HEK293T cells using L-DOPA as substrate assessed as inhibition constant incubated for 1 hr by microplate reader analysis
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293T
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
Ki 3 6.43 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5408197 1 6.60
CHEMBL5399906 1 6.26
CHEMBL287556 KOJIC ACID 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5408197 Ki = 250.0 nM 6.60
CHEMBL5399906 Ki = 550.0 nM 6.26
CHEMBL287556 KOJIC ACID Ki = 1100000.0 nM -