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Assay Detail

CHEMBL4034741

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

Binding
Inhibition of recombinant human full length GST-tagged CDC25A expressed in Escherichia coli BL21-DE3 pLysS using 3-O-methylfluorescein phosphate as substrate after 2 hrs by fluorimetric analysis
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

M-phase inducer phosphatase 1 (CHEMBL3775)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel coumarin- and quinolinone-based polycycles as cell division cycle 25-A and -C phosphatases inhibitors induce proliferation arrest and apoptosis in cancer cells.
Zwergel C, Czepukojc B, Evain-Bana E, Xu Z, Stazi G, Mori M, Patsilinakos A, Mai A, Botta B, Ragno R, Bagrel D, Kirsch G, Meiser P, Jacob C, Montenarh M, Valente S.
Eur J Med Chem (2017) 134 : 316 -333
PubMed 28431339 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 5.57 7.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL429095 1 7.26
CHEMBL4066424 1 5.92
CHEMBL4093222 1 5.82
CHEMBL4097725 1 5.79
CHEMBL4060132 1 5.66
CHEMBL4075821 1 5.59
CHEMBL4094178 1 5.54
CHEMBL4066643 1 5.54
CHEMBL4066281 1 5.54
CHEMBL4104313 1 5.51
CHEMBL4097300 1 5.49
CHEMBL4094844 1 5.47
CHEMBL4085485 1 5.46
CHEMBL4082819 1 5.39
CHEMBL4067408 1 5.36
CHEMBL4098262 1 5.24
CHEMBL4086414 1 5.18
CHEMBL4105005 1 5.11
CHEMBL4087165 1 4.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL429095 IC50 = 55.0 nM 7.26
CHEMBL4066424 IC50 = 1200.0 nM 5.92
CHEMBL4093222 IC50 = 1500.0 nM 5.82
CHEMBL4097725 IC50 = 1610.0 nM 5.79
CHEMBL4060132 IC50 = 2190.0 nM 5.66
CHEMBL4075821 IC50 = 2570.0 nM 5.59
CHEMBL4094178 IC50 = 2900.0 nM 5.54
CHEMBL4066643 IC50 = 2880.0 nM 5.54
CHEMBL4066281 IC50 = 2850.0 nM 5.54
CHEMBL4104313 IC50 = 3110.0 nM 5.51
CHEMBL4097300 IC50 = 3230.0 nM 5.49
CHEMBL4094844 IC50 = 3370.0 nM 5.47
CHEMBL4085485 IC50 = 3500.0 nM 5.46
CHEMBL4082819 IC50 = 4040.0 nM 5.39
CHEMBL4067408 IC50 = 4330.0 nM 5.36
CHEMBL4098262 IC50 = 5800.0 nM 5.24
CHEMBL4086414 IC50 = 6600.0 nM 5.18
CHEMBL4105005 IC50 = 7730.0 nM 5.11
CHEMBL4087165 IC50 = 13000.0 nM 4.89