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Assay Detail

CHEMBL4253918

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

Binding
Inhibition of human PTP1B using p-nitrophenyl phosphate as substrate preincubated for 10 mins followed by substrate addition measured every minute for 10 mins by UV-VIS spectrophotometric analysis
8
Total Activities
8
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

Naturally occurring Diels-Alder-type adducts from Morus nigra as potent inhibitors of Mycobacterium tuberculosis protein tyrosine phosphatase B.
Mascarello A, Orbem Menegatti AC, Calcaterra A, Martins PGA, Chiaradia-Delatorre LD, D'Acquarica I, Ferrari F, Pau V, Sanna A, De Logu A, Botta M, Botta B, Terenzi H, Mori M.
Eur J Med Chem (2018) 144 : 277 -288
PubMed 29275228 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.25 5.71

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1808155 CHALCOMORACIN 1 5.71
CHEMBL4290098 1 5.59
CHEMBL220746 CUDRAFLAVANONE A 1 5.37
CHEMBL4279417 1 5.34
CHEMBL463145 NORARTOCARPETIN 1 5.29
CHEMBL4291588 1 5.10
CHEMBL464006 MORUSIN 1 4.99
CHEMBL43065 OXYRESVERATROL 1 4.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1808155 CHALCOMORACIN IC50 = 1940.0 nM 5.71
CHEMBL4290098 IC50 = 2540.0 nM 5.59
CHEMBL220746 CUDRAFLAVANONE A IC50 = 4310.0 nM 5.37
CHEMBL4279417 IC50 = 4560.0 nM 5.34
CHEMBL463145 NORARTOCARPETIN IC50 = 5180.0 nM 5.29
CHEMBL4291588 IC50 = 7980.0 nM 5.10
CHEMBL464006 MORUSIN IC50 = 10320.0 nM 4.99
CHEMBL43065 OXYRESVERATROL IC50 = 27130.0 nM 4.57