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Assay Detail

CHEMBL4723114

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

Binding
Inhibition of human tyrosinase using L- DOPA as substrate by MBTH based assay
15
Total Activities
15
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
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 5.43 5.85
Ki 7 4.34 4.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4763438 1 5.85
CHEMBL4792744 1 5.80
CHEMBL4795966 1 5.60
CHEMBL590969 1 5.58
CHEMBL4782537 1 5.50
CHEMBL1491393 1 5.50
CHEMBL4757374 1 5.34
CHEMBL1269349 1 4.72
CHEMBL1269350 1 4.57
CHEMBL4751526 1 4.34
CHEMBL1269399 1 4.34
CHEMBL4746238 1 4.30
CHEMBL541251 1 4.29
CHEMBL4794995 1 4.12
CHEMBL4777553 1 4.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4763438 IC50 = 1400.0 nM 5.85
CHEMBL4792744 IC50 = 1600.0 nM 5.80
CHEMBL4795966 IC50 = 2500.0 nM 5.60
CHEMBL590969 IC50 = 2600.0 nM 5.58
CHEMBL4782537 IC50 = 3200.0 nM 5.50
CHEMBL1491393 IC50 = 3200.0 nM 5.50
CHEMBL4757374 IC50 = 4600.0 nM 5.34
CHEMBL1269349 Ki = 19000.0 nM 4.72
CHEMBL1269350 Ki = 27000.0 nM 4.57
CHEMBL4751526 Ki = 46000.0 nM 4.34
CHEMBL1269399 Ki = 46000.0 nM 4.34
CHEMBL4746238 Ki = 50000.0 nM 4.30
CHEMBL541251 IC50 = 51000.0 nM 4.29
CHEMBL4794995 Ki = 75000.0 nM 4.12
CHEMBL4777553 Ki = 100000.0 nM 4.00