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Assay Detail

CHEMBL2214497

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

Binding
Inhibition of PTP1B by para-nitrophenyl phosphate release assay
18
Total Activities
18
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 1 (CHEMBL335)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of 4,4-dimethyl lithocholic acid derivatives as novel inhibitors of protein tyrosine phosphatase 1B.
He HB, Gao LX, Deng QF, Ma WP, Tang CL, Qiu WW, Tang J, Li JY, Li J, Yang F.
Bioorg Med Chem Lett (2012) 22 : 7237 -7242
PubMed 23067554 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.04 5.79

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2205895 1 5.79
CHEMBL2205890 1 5.44
CHEMBL129681 1 5.41
CHEMBL2205896 1 5.39
CHEMBL2205886 1 5.25
CHEMBL2205888 1 5.06
CHEMBL2205885 1 5.04
CHEMBL2205894 1 5.04
CHEMBL2205892 1 5.04
CHEMBL2205884 1 5.03
CHEMBL2205893 1 4.93
CHEMBL1478 LITHOCHOLIC ACID 1 4.89
CHEMBL2205898 1 4.88
CHEMBL2205883 1 4.88
CHEMBL2205897 1 4.72
CHEMBL2205889 1 4.55
CHEMBL2205887 1 4.40
CHEMBL2205891 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2205895 IC50 = 1620.0 nM 5.79
CHEMBL2205890 IC50 = 3610.0 nM 5.44
CHEMBL129681 IC50 = 3890.0 nM 5.41
CHEMBL2205896 IC50 = 4110.0 nM 5.39
CHEMBL2205886 IC50 = 5570.0 nM 5.25
CHEMBL2205888 IC50 = 8620.0 nM 5.06
CHEMBL2205885 IC50 = 9040.0 nM 5.04
CHEMBL2205894 IC50 = 9130.0 nM 5.04
CHEMBL2205892 IC50 = 9110.0 nM 5.04
CHEMBL2205884 IC50 = 9270.0 nM 5.03
CHEMBL2205893 IC50 = 11650.0 nM 4.93
CHEMBL1478 LITHOCHOLIC ACID IC50 = 12740.0 nM 4.89
CHEMBL2205898 IC50 = 13210.0 nM 4.88
CHEMBL2205883 IC50 = 13200.0 nM 4.88
CHEMBL2205897 IC50 = 19164.0 nM 4.72
CHEMBL2205889 IC50 = 28220.0 nM 4.55
CHEMBL2205887 IC50 = 39440.0 nM 4.40
CHEMBL2205891 IC50 > 40000.0 nM -