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Assay Detail

CHEMBL5516359

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

Binding
Inhibition of SHP-1 (245 to 543 residues)(unknown origin) expressed in Escherichia coli BL21(DE3) using DiFMUP as substrate incubated for 10 mins by fluorescence based assay
9
Total Activities
9
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

Tyrosine-protein phosphatase non-receptor type 6 (CHEMBL3166)
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 9 4.46 4.81

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5567968 1 4.81
CHEMBL5555119 1 4.64
CHEMBL5559251 1 4.44
CHEMBL5563600 1 4.24
CHEMBL5568311 1 4.19
CHEMBL57974 1 -
CHEMBL5560087 1 -
CHEMBL5556892 1 -
CHEMBL5561438 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5567968 IC50 = 15470.0 nM 4.81
CHEMBL5555119 IC50 = 22700.0 nM 4.64
CHEMBL5559251 IC50 = 36600.0 nM 4.44
CHEMBL5563600 IC50 = 57000.0 nM 4.24
CHEMBL5568311 IC50 = 64700.0 nM 4.19
CHEMBL57974 IC50 = 5730000.0 nM -
CHEMBL5560087 IC50 = 138700.0 nM -
CHEMBL5556892 IC50 = 167300.0 nM -
CHEMBL5561438 IC50 > 500000.0 nM -