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Assay Detail

CHEMBL4133417

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Binding
Inhibition of mushroom tyrosinase diphenolase activity assessed as decrease in dopachrome formation using L-DOPA as substrate preincubated for 10 mins followed by substrate addition measured for 1 min
ChEMBL ↗
53
Total Activities
53
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Agaricus bisporus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Tyrosinase (CHEMBL3318) ↗
Type SINGLE PROTEIN
Organism Agaricus bisporus

Publication

Study on the design, synthesis and structure-activity relationships of new thiosemicarbazone compounds as tyrosinase inhibitors.
Song S, You A, Chen Z, Zhu G, Wen H, Song H, Yi W.
Eur J Med Chem (2017) 139 : 815 -825
PubMed 28865277 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 53 5.78 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4162131 — — 1 6.85
CHEMBL4169693 — — 1 6.75
CHEMBL4161762 — — 1 6.63
CHEMBL4165568 — — 1 6.63
CHEMBL3197927 — — 1 6.56
CHEMBL4162156 — — 1 6.56
CHEMBL4173533 — — 1 6.49
CHEMBL4177091 — — 1 6.47
CHEMBL4162828 — — 1 6.45
CHEMBL323975 — — 1 6.42
CHEMBL4172806 — — 1 6.41
CHEMBL4166658 — — 1 6.36
CHEMBL4159466 — — 1 6.36
CHEMBL4169234 — — 1 6.35
CHEMBL4170082 — — 1 6.34
CHEMBL4167399 — — 1 6.32
CHEMBL4177284 — — 1 6.31
CHEMBL4163943 — — 1 6.30
CHEMBL4176884 — — 1 6.25
CHEMBL4163520 — — 1 6.21
CHEMBL1980327 — — 1 6.20
CHEMBL4174215 — — 1 6.02
CHEMBL4161071 — — 1 5.82
CHEMBL4169025 — — 1 5.78
CHEMBL4161961 — — 1 5.72
CHEMBL4172366 — — 1 5.70
CHEMBL4172404 — — 1 5.70
CHEMBL4176010 — — 1 5.62
CHEMBL4164484 — — 1 5.61
CHEMBL4165401 — — 1 5.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4162131 — IC50 = 142.0 nM 6.85
CHEMBL4169693 — IC50 = 177.0 nM 6.75
CHEMBL4165568 — IC50 = 232.0 nM 6.63
CHEMBL4161762 — IC50 = 236.0 nM 6.63
CHEMBL3197927 — IC50 = 278.0 nM 6.56
CHEMBL4162156 — IC50 = 278.0 nM 6.56
CHEMBL4173533 — IC50 = 325.0 nM 6.49
CHEMBL4177091 — IC50 = 339.0 nM 6.47
CHEMBL4162828 — IC50 = 358.0 nM 6.45
CHEMBL323975 — IC50 = 384.0 nM 6.42
CHEMBL4172806 — IC50 = 394.0 nM 6.41
CHEMBL4166658 — IC50 = 437.0 nM 6.36
CHEMBL4159466 — IC50 = 441.0 nM 6.36
CHEMBL4169234 — IC50 = 448.0 nM 6.35
CHEMBL4170082 — IC50 = 458.0 nM 6.34
CHEMBL4167399 — IC50 = 483.0 nM 6.32
CHEMBL4177284 — IC50 = 485.0 nM 6.31
CHEMBL4163943 — IC50 = 495.0 nM 6.30
CHEMBL4176884 — IC50 = 562.0 nM 6.25
CHEMBL4163520 — IC50 = 610.0 nM 6.21
CHEMBL1980327 — IC50 = 632.0 nM 6.20
CHEMBL4174215 — IC50 = 960.0 nM 6.02
CHEMBL4161071 — IC50 = 1513.0 nM 5.82
CHEMBL4169025 — IC50 = 1661.0 nM 5.78
CHEMBL4161961 — IC50 = 1912.0 nM 5.72
CHEMBL4172366 — IC50 = 1992.0 nM 5.70
CHEMBL4172404 — IC50 = 1982.0 nM 5.70
CHEMBL4176010 — IC50 = 2382.0 nM 5.62
CHEMBL4164484 — IC50 = 2466.0 nM 5.61
CHEMBL4165401 — IC50 = 2781.0 nM 5.56
CHEMBL242106 — IC50 = 2830.0 nM 5.55
CHEMBL4168825 — IC50 = 3101.0 nM 5.51
CHEMBL4168996 — IC50 = 5901.0 nM 5.23
CHEMBL4163960 — IC50 = 8120.0 nM 5.09
CHEMBL4160152 — IC50 = 9490.0 nM 5.02
CHEMBL4163213 — IC50 = 13904.0 nM 4.86
CHEMBL4173936 — IC50 = 17566.0 nM 4.75
CHEMBL287556 KOJIC ACID IC50 = 28200.0 nM 4.55
CHEMBL4170794 — IC50 = 28810.0 nM 4.54
CHEMBL4164288 — IC50 = 35350.0 nM 4.45
CHEMBL4166669 — IC50 = 56670.0 nM 4.25
CHEMBL4159067 — IC50 = 88970.0 nM 4.05
CHEMBL4174585 — IC50 = 98310.0 nM 4.01
CHEMBL4172618 — IC50 > 200000.0 nM -
CHEMBL4175777 — IC50 > 50000.0 nM -
CHEMBL4170072 — IC50 > 50000.0 nM -
CHEMBL4170497 — IC50 > 50000.0 nM -
CHEMBL4159844 — IC50 > 50000.0 nM -
CHEMBL4167919 — IC50 > 50000.0 nM -
CHEMBL1269810 — IC50 > 100000.0 nM -