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Assay Detail

CHEMBL2161972

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

Binding
Inhibition of HePTP expressed in Escherichia coli BL21 using pNPP substrate
17
Total Activities
17
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 7 (CHEMBL2219)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a novel series of inhibitors of lymphoid tyrosine phosphatase with activity in human T cells.
Stanford SM, Krishnamurthy D, Falk MD, Messina R, Debnath B, Li S, Liu T, Kazemi R, Dahl R, He Y, Yu X, Chan AC, Zhang ZY, Barrios AM, Woods VL, Neamati N, Bottini N.
J Med Chem (2011) 54 : 1640 -1654
PubMed 21341673 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 4.87 5.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2159933 1 5.10
CHEMBL2159726 1 5.10
CHEMBL2159725 1 5.05
CHEMBL1713374 1 5.00
CHEMBL2159929 1 4.92
CHEMBL2159934 1 4.82
CHEMBL2159932 1 4.80
CHEMBL2159928 1 4.75
CHEMBL1721448 1 4.70
CHEMBL2159930 1 4.70
CHEMBL2159931 1 4.66
CHEMBL1710150 1 -
CHEMBL2159937 1 -
CHEMBL2159949 1 -
CHEMBL2158022 1 -
CHEMBL2159948 1 -
CHEMBL2159946 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2159933 IC50 = 8000.0 nM 5.10
CHEMBL2159726 IC50 = 8000.0 nM 5.10
CHEMBL2159725 IC50 = 9000.0 nM 5.05
CHEMBL1713374 IC50 = 10000.0 nM 5.00
CHEMBL2159929 IC50 = 12000.0 nM 4.92
CHEMBL2159934 IC50 = 15000.0 nM 4.82
CHEMBL2159932 IC50 = 16000.0 nM 4.80
CHEMBL2159928 IC50 = 18000.0 nM 4.75
CHEMBL1721448 IC50 = 20000.0 nM 4.70
CHEMBL2159930 IC50 = 20000.0 nM 4.70
CHEMBL2159931 IC50 = 22000.0 nM 4.66
CHEMBL1710150 IC50 > 40000.0 nM -
CHEMBL2159937 IC50 > 75000.0 nM -
CHEMBL2159949 IC50 > 75000.0 nM -
CHEMBL2158022 IC50 > 75000.0 nM -
CHEMBL2159948 IC50 > 75000.0 nM -
CHEMBL2159946 IC50 > 75000.0 nM -