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Assay Detail

CHEMBL5516360

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

Binding
Inhibition of human CDC14A using DiFMUP as substrate incubated for 10 mins by fluorescence based assay
17
Total Activities
16
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

Dual specificity protein phosphatase CDC14A (CHEMBL1772926)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of Novel Phosphonodifluoromethyl-Containing Phosphotyrosine Mimetics and a First-In-Class, Potent, Selective, and Bioavailable Inhibitor of Human CDC14 Phosphatases.
Dong J, Jassim BA, Milholland KL, Qu Z, Bai Y, Miao Y, Miao J, Ma Y, Lin J, Hall MC, Zhang ZY.
J Med Chem (2024) 67 : 8817 -8835
PubMed 38768084 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 5.62 7.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5567968 2 7.05
CHEMBL5568076 1 5.72
CHEMBL5560702 1 5.70
CHEMBL5568214 1 5.66
CHEMBL5563039 1 5.56
CHEMBL5565218 1 5.56
CHEMBL5556755 1 5.49
CHEMBL5542122 1 5.03
CHEMBL5561438 1 5.01
CHEMBL5568311 1 4.01
CHEMBL57974 1 -
CHEMBL5563600 1 -
CHEMBL5555119 1 -
CHEMBL5559251 1 -
CHEMBL5560087 1 -
CHEMBL5556892 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5567968 IC50 = 90.0 nM 7.05
CHEMBL5567968 IC50 = 93.0 nM 7.03
CHEMBL5568076 IC50 = 1920.0 nM 5.72
CHEMBL5560702 IC50 = 2000.0 nM 5.70
CHEMBL5568214 IC50 = 2170.0 nM 5.66
CHEMBL5565218 IC50 = 2740.0 nM 5.56
CHEMBL5563039 IC50 = 2780.0 nM 5.56
CHEMBL5556755 IC50 = 3210.0 nM 5.49
CHEMBL5542122 IC50 = 9410.0 nM 5.03
CHEMBL5561438 IC50 = 9850.0 nM 5.01
CHEMBL5568311 IC50 = 98700.0 nM 4.01
CHEMBL57974 IC50 = 3269000.0 nM -
CHEMBL5556892 IC50 = 360000.0 nM -
CHEMBL5560087 IC50 = 339000.0 nM -
CHEMBL5559251 IC50 = 273200.0 nM -
CHEMBL5555119 IC50 = 119600.0 nM -
CHEMBL5563600 IC50 = 220600.0 nM -