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Assay Detail

CHEMBL3371692

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

Binding
Inhibition of purified human GST-tagged PTP-1B using p-nitrophenylphosphate as substrate by spectrophotometry
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 1 (CHEMBL335)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of oleanolic acid derivatives: In vitro, in vivo and in silico studies for PTP-1B inhibition.
Ramírez-Espinosa JJ, Rios MY, Paoli P, Flores-Morales V, Camici G, de la Rosa-Lugo V, Hidalgo-Figueroa S, Navarrete-Vázquez G, Estrada-Soto S.
Eur J Med Chem (2014) 87 : 316 -327
PubMed 25264584 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 4.92 5.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3343064 1 5.28
CHEMBL3343062 1 5.21
CHEMBL3343063 1 5.07
CHEMBL168 OLEANOLIC_ACID 1 5.02
CHEMBL400074 ERYTHRODIOL 1 5.02
CHEMBL3126477 1 4.79
CHEMBL3343061 1 4.75
CHEMBL486822 ACETYL OLEANOLIC ACID 1 4.67
CHEMBL3343065 1 4.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3343064 IC50 = 5300.0 nM 5.28
CHEMBL3343062 IC50 = 6100.0 nM 5.21
CHEMBL3343063 IC50 = 8600.0 nM 5.07
CHEMBL168 OLEANOLIC_ACID IC50 = 9500.0 nM 5.02
CHEMBL400074 ERYTHRODIOL IC50 = 9600.0 nM 5.02
CHEMBL3126477 IC50 = 16200.0 nM 4.79
CHEMBL3343061 IC50 = 17800.0 nM 4.75
CHEMBL486822 ACETYL OLEANOLIC ACID IC50 = 21500.0 nM 4.67
CHEMBL3343065 IC50 = 36500.0 nM 4.44