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Assay Detail

CHEMBL1646368

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

Binding
Inhibition of recombinant SHP1
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Tyrosine-protein phosphatase non-receptor type 6 (CHEMBL3166)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Shp2 protein tyrosine phosphatase inhibitor activity of estramustine phosphate and its triterpenoid analogs.
Scott LM, Chen L, Daniel KG, Brooks WH, Guida WC, Lawrence HR, Sebti SM, Lawrence NJ, Wu J.
Bioorg Med Chem Lett (2011) 21 : 730 -733
PubMed 21193311 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 4.38 4.56

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL301982 CELASTROL 1 4.56
CHEMBL1756 ESTRAMUSTINE PHOSPHATE 4.0 1 4.39
CHEMBL230006 ENOXOLONE 2.0 1 4.18
CHEMBL1642763 ESTRADIOL PHOSPHATE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL301982 CELASTROL IC50 = 27800.0 nM 4.56
CHEMBL1756 ESTRAMUSTINE PHOSPHATE IC50 = 40400.0 nM 4.39
CHEMBL230006 ENOXOLONE IC50 = 65400.0 nM 4.18
CHEMBL1642763 ESTRADIOL PHOSPHATE IC50 > 300000.0 nM -