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Assay Detail

CHEMBL679541

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

Binding
Inhibitory activity againist Estrone sulfatase from MCF-7 cells (placental microsomes)
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type MCF7
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Steryl-sulfatase (CHEMBL3559)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A novel type of nonsteroidal estrone sulfatase inhibitors.
Jütten P, Schumann W, Härtl A, Heinisch L, Gräfe U, Werner W, Ulbricht H.
Bioorg Med Chem Lett (2002) 12 : 1339 -1342
PubMed 11992772 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 5.10 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL122708 EMATE 1 7.10
CHEMBL231602 MHL CYCLOHEXYLTHIOSEMICARBAZONE 1 6.34
CHEMBL26541 1 5.85
CHEMBL27369 1 5.75
CHEMBL11185 1 5.58
CHEMBL26969 1 5.50
CHEMBL25760 1 5.40
CHEMBL26414 1 5.32
CHEMBL284412 1 5.22
CHEMBL285331 1 5.22
CHEMBL25794 1 5.16
CHEMBL26041 1 5.10
CHEMBL286960 1 5.10
CHEMBL27198 1 5.05
CHEMBL27864 1 4.96
CHEMBL26970 1 4.92
CHEMBL287229 1 4.89
CHEMBL27368 1 4.82
CHEMBL27657 1 4.80
CHEMBL286712 1 4.75
CHEMBL27197 1 4.72
CHEMBL27721 1 4.70
CHEMBL27057 1 4.66
CHEMBL26958 1 4.64
CHEMBL286518 1 4.62
CHEMBL26647 1 4.60
CHEMBL27775 1 4.54
CHEMBL422576 1 4.39
CHEMBL285011 1 4.30
CHEMBL26480 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL122708 EMATE IC50 = 80.0 nM 7.10
CHEMBL231602 MHL CYCLOHEXYLTHIOSEMICARBAZONE IC50 = 460.0 nM 6.34
CHEMBL26541 IC50 = 1400.0 nM 5.85
CHEMBL27369 IC50 = 1800.0 nM 5.75
CHEMBL11185 IC50 = 2600.0 nM 5.58
CHEMBL26969 IC50 = 3200.0 nM 5.50
CHEMBL25760 IC50 = 4000.0 nM 5.40
CHEMBL26414 IC50 = 4800.0 nM 5.32
CHEMBL284412 IC50 = 6000.0 nM 5.22
CHEMBL285331 IC50 = 6000.0 nM 5.22
CHEMBL25794 IC50 = 7000.0 nM 5.16
CHEMBL26041 IC50 = 8000.0 nM 5.10
CHEMBL286960 IC50 = 8000.0 nM 5.10
CHEMBL27198 IC50 = 9000.0 nM 5.05
CHEMBL27864 IC50 = 11000.0 nM 4.96
CHEMBL26970 IC50 = 12000.0 nM 4.92
CHEMBL287229 IC50 = 13000.0 nM 4.89
CHEMBL27368 IC50 = 15000.0 nM 4.82
CHEMBL27657 IC50 = 16000.0 nM 4.80
CHEMBL286712 IC50 = 18000.0 nM 4.75
CHEMBL27197 IC50 = 19000.0 nM 4.72
CHEMBL27721 IC50 = 20000.0 nM 4.70
CHEMBL27057 IC50 = 22000.0 nM 4.66
CHEMBL26958 IC50 = 23000.0 nM 4.64
CHEMBL286518 IC50 = 24000.0 nM 4.62
CHEMBL26647 IC50 = 25000.0 nM 4.60
CHEMBL27775 IC50 = 29000.0 nM 4.54
CHEMBL422576 IC50 = 41000.0 nM 4.39
CHEMBL285011 IC50 = 50000.0 nM 4.30
CHEMBL26480 IC50 > 100000.0 nM -
CHEMBL26959 IC50 > 100000.0 nM -
CHEMBL283933 IC50 > 100000.0 nM -
CHEMBL26360 IC50 > 100000.0 nM -
CHEMBL25967 IC50 > 100000.0 nM -