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Assay Detail

CHEMBL768523

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

Binding
Inhibitory activity against Protein tyrosine phosphatase 1B (PTP1B) over-expressed in intact Sf9 cell assay
23
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type Sf9
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Tyrosine-protein phosphatase non-receptor type 1 (CHEMBL335)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure based design of a series of potent and selective non peptidic PTP-1B inhibitors.
Lau CK, Bayly CI, Gauthier JY, Li CS, Therien M, Asante-Appiah E, Cromlish W, Boie Y, Forghani F, Desmarais S, Wang Q, Skorey K, Waddleton D, Payette P, Ramachandran C, Kennedy BP, Scapin G.
Bioorg Med Chem Lett (2004) 14 : 1043 -1048
PubMed 15013020 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 6.43 7.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL266753 4 7.24
CHEMBL273474 1 7.21
CHEMBL268903 1 7.08
CHEMBL8662 1 7.06
CHEMBL267048 1 6.92
CHEMBL276647 1 6.92
CHEMBL274435 1 6.92
CHEMBL267488 1 6.80
CHEMBL9473 1 6.72
CHEMBL268526 1 6.66
CHEMBL269166 1 6.62
CHEMBL276648 1 6.43
CHEMBL416145 1 6.34
CHEMBL9321 1 6.19
CHEMBL9252 1 6.03
CHEMBL418703 1 5.92
CHEMBL9339 1 5.80
CHEMBL267759 1 5.80
CHEMBL267245 1 5.77
CHEMBL9374 1 5.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL266753 IC50 = 58.0 nM 7.24
CHEMBL273474 IC50 = 62.0 nM 7.21
CHEMBL268903 IC50 = 84.0 nM 7.08
CHEMBL8662 IC50 = 88.0 nM 7.06
CHEMBL266753 IC50 = 100.0 nM 7.00
CHEMBL267048 IC50 = 120.0 nM 6.92
CHEMBL276647 IC50 = 120.0 nM 6.92
CHEMBL274435 IC50 = 120.0 nM 6.92
CHEMBL267488 IC50 = 160.0 nM 6.80
CHEMBL9473 IC50 = 190.0 nM 6.72
CHEMBL268526 IC50 = 220.0 nM 6.66
CHEMBL269166 IC50 = 240.0 nM 6.62
CHEMBL276648 IC50 = 370.0 nM 6.43
CHEMBL416145 IC50 = 460.0 nM 6.34
CHEMBL9321 IC50 = 650.0 nM 6.19
CHEMBL9252 IC50 = 930.0 nM 6.03
CHEMBL418703 IC50 = 1200.0 nM 5.92
CHEMBL9339 IC50 = 1600.0 nM 5.80
CHEMBL267759 IC50 = 1600.0 nM 5.80
CHEMBL267245 IC50 = 1700.0 nM 5.77
CHEMBL266753 IC50 = 1790.0 nM 5.75
CHEMBL9374 IC50 = 4070.0 nM 5.39
CHEMBL266753 IC50 = 5340.0 nM 5.27