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Assay Detail

CHEMBL3429158

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

Binding
Inhibition of His6-tagged human recombinant Cdc25B catalytic domain (350 to 566 residues) expressed in Escherichia coli BL21 (D3) using OMFP substrate after 30 mins by spectrophotometry
26
Total Activities
26
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 2 (CHEMBL4804)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of 3-aminoisoquinolin-1(2H)-one based inhibitors of the dual-specificity phosphatase Cdc25B.
George Rosenker KM, Paquette WD, Johnston PA, Sharlow ER, Vogt A, Bakan A, Lazo JS, Wipf P.
Bioorg Med Chem (2015) 23 : 2810 -2818
PubMed 25703307 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 5.63 6.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3426986 1 6.19
CHEMBL1715541 1 6.11
CHEMBL3426981 1 6.11
CHEMBL1522941 1 6.08
CHEMBL3426980 1 6.07
CHEMBL1453503 1 5.94
CHEMBL3426978 1 5.92
CHEMBL3426982 1 5.81
CHEMBL3426988 1 5.75
CHEMBL3426976 1 5.73
CHEMBL3426989 1 5.70
CHEMBL3426985 1 5.64
CHEMBL3426987 1 5.61
CHEMBL3426979 1 5.59
CHEMBL3426990 1 5.50
CHEMBL3426991 1 5.50
CHEMBL1611833 1 5.48
CHEMBL1712864 1 5.47
CHEMBL3426983 1 5.42
CHEMBL1719459 1 5.38
CHEMBL3426984 1 5.35
CHEMBL1707033 1 5.28
CHEMBL470594 1 5.28
CHEMBL1596475 1 4.97
CHEMBL3426977 1 4.87
CHEMBL1876186 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3426986 IC50 = 640.0 nM 6.19
CHEMBL1715541 IC50 = 770.0 nM 6.11
CHEMBL3426981 IC50 = 770.0 nM 6.11
CHEMBL1522941 IC50 = 830.0 nM 6.08
CHEMBL3426980 IC50 = 850.0 nM 6.07
CHEMBL1453503 IC50 = 1160.0 nM 5.94
CHEMBL3426978 IC50 = 1210.0 nM 5.92
CHEMBL3426982 IC50 = 1550.0 nM 5.81
CHEMBL3426988 IC50 = 1770.0 nM 5.75
CHEMBL3426976 IC50 = 1850.0 nM 5.73
CHEMBL3426989 IC50 = 2000.0 nM 5.70
CHEMBL3426985 IC50 = 2310.0 nM 5.64
CHEMBL3426987 IC50 = 2480.0 nM 5.61
CHEMBL3426979 IC50 = 2570.0 nM 5.59
CHEMBL3426990 IC50 = 3190.0 nM 5.50
CHEMBL3426991 IC50 = 3180.0 nM 5.50
CHEMBL1611833 IC50 = 3310.0 nM 5.48
CHEMBL1712864 IC50 = 3370.0 nM 5.47
CHEMBL3426983 IC50 = 3800.0 nM 5.42
CHEMBL1719459 IC50 = 4190.0 nM 5.38
CHEMBL3426984 IC50 = 4480.0 nM 5.35
CHEMBL1707033 IC50 = 5250.0 nM 5.28
CHEMBL470594 IC50 = 5300.0 nM 5.28
CHEMBL1596475 IC50 = 10750.0 nM 4.97
CHEMBL3426977 IC50 = 13630.0 nM 4.87
CHEMBL1876186 IC50 > 50000.0 nM -