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Assay Detail

CHEMBL768521

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Binding
In vitro inhibitory activity against protein tyrosine phosphatase 1B (PTP1B) was determined in fluorescein diphosphate (FDP) assay
16
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

The development of potent non-peptidic PTP-1B inhibitors.
Dufresne C, Roy P, Wang Z, Asante-Appiah E, Cromlish W, Boie Y, Forghani F, Desmarais S, Wang Q, Skorey K, Waddleton D, Ramachandran C, Kennedy BP, Xu L, Gordon R, Chan CC, Leblanc Y.
Bioorg Med Chem Lett (2004) 14 : 1039 -1042
PubMed 15013019 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.58 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL9046 1 7.40
CHEMBL267954 1 7.22
CHEMBL266056 2 7.22
CHEMBL263348 1 7.05
CHEMBL8767 1 6.96
CHEMBL8758 1 6.92
CHEMBL276376 1 6.80
CHEMBL8725 1 6.72
CHEMBL9087 1 6.72
CHEMBL428651 1 6.44
CHEMBL9070 1 6.41
CHEMBL8660 1 6.10
CHEMBL267981 1 6.03
CHEMBL267022 1 5.70
CHEMBL9047 1 4.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL9046 IC50 = 40.0 nM 7.40
CHEMBL267954 IC50 = 60.0 nM 7.22
CHEMBL266056 IC50 = 60.0 nM 7.22
CHEMBL263348 IC50 = 90.0 nM 7.05
CHEMBL8767 IC50 = 110.0 nM 6.96
CHEMBL8758 IC50 = 120.0 nM 6.92
CHEMBL276376 IC50 = 160.0 nM 6.80
CHEMBL8725 IC50 = 190.0 nM 6.72
CHEMBL9087 IC50 = 190.0 nM 6.72
CHEMBL266056 IC50 = 190.0 nM 6.72
CHEMBL428651 IC50 = 360.0 nM 6.44
CHEMBL9070 IC50 = 390.0 nM 6.41
CHEMBL8660 IC50 = 800.0 nM 6.10
CHEMBL267981 IC50 = 940.0 nM 6.03
CHEMBL267022 IC50 = 2000.0 nM 5.70
CHEMBL9047 IC50 = 16000.0 nM 4.80