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Assay Detail

CHEMBL4422542

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

Binding
Inhibition of GST-fused human Eya2 ED (253 to 538 residues) expressed in Escherichia coli pre-incubated for 10 mins followed by OMFP substrate addition and further incubated for 30 mins by fluorescence based assay
21
Total Activities
20
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

Eyes absent homolog 2 (CHEMBL1293275)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Inhibitors of eya2
(2012)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 4.90 5.75
Inhibition 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4463681 1 5.75
CHEMBL3191598 1 5.64
CHEMBL4459891 1 5.46
CHEMBL4530754 2 5.40
CHEMBL1975051 1 5.14
CHEMBL3195222 1 4.75
CHEMBL4445513 1 4.75
CHEMBL3189517 1 4.54
CHEMBL858 EDETIC ACID 3.0 1 4.19
CHEMBL3190554 1 4.14
CHEMBL4446792 1 4.10
CHEMBL4458563 1 -
CHEMBL4476815 1 -
CHEMBL4532983 1 -
CHEMBL4446652 1 -
CHEMBL87223 AMINOQUINURIDE 2.0 1 -
CHEMBL4449839 1 -
CHEMBL1232903 GLYCERYLPHOSPHATE 1 -
CHEMBL1528 SODIUM FLUORIDE 4.0 1 -
CHEMBL179166 SODIUM ORTHOVANAD 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4463681 IC50 = 1800.0 nM 5.75
CHEMBL3191598 IC50 = 2300.0 nM 5.64
CHEMBL4459891 IC50 = 3450.0 nM 5.46
CHEMBL4530754 IC50 = 4000.0 nM 5.40
CHEMBL1975051 IC50 = 7300.0 nM 5.14
CHEMBL3195222 IC50 = 18000.0 nM 4.75
CHEMBL4445513 IC50 = 18000.0 nM 4.75
CHEMBL3189517 IC50 = 29000.0 nM 4.54
CHEMBL858 EDETIC ACID IC50 = 65000.0 nM 4.19
CHEMBL3190554 IC50 = 73000.0 nM 4.14
CHEMBL4446792 IC50 = 79110.0 nM 4.10
CHEMBL179166 SODIUM ORTHOVANAD IC50 = 1800000.0 nM -
CHEMBL1528 SODIUM FLUORIDE IC50 = 6600000.0 nM -
CHEMBL1232903 GLYCERYLPHOSPHATE IC50 = 8200000.0 nM -
CHEMBL4449839 IC50 = 11300000.0 nM -
CHEMBL4446652 Inhibition - % -
CHEMBL4476815 Inhibition - % -
CHEMBL4458563 IC50 < 35000.0 nM -
CHEMBL4532983 IC50 < 35000.0 nM -
CHEMBL87223 AMINOQUINURIDE IC50 < 35000.0 nM -
CHEMBL4530754 Inhibition - % -