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Assay Detail

CHEMBL865873

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Binding
Inhibitory activity against recombinant human PTP1B
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

PTP-1B inhibitors: cyclopenta[d][1,2]-oxazine derivatives.
Cho SY, Baek JY, Han SS, Kang SK, Ha JD, Ahn JH, Lee JD, Kim KR, Cheon HG, Rhee SD, Yang SD, Yon GH, Pak CS, Choi JK.
Bioorg Med Chem Lett (2006) 16 : 499 -502
PubMed 16289879 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.67 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL200117 1 6.85
CHEMBL371026 1 6.57
CHEMBL201662 1 6.10
CHEMBL201161 1 5.79
CHEMBL371322 1 5.71
CHEMBL202197 1 5.67
CHEMBL201909 1 5.47
CHEMBL370140 1 5.26
CHEMBL370584 1 5.25
CHEMBL202573 1 5.12
CHEMBL199479 1 5.11
CHEMBL202219 1 5.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL200117 IC50 = 140.0 nM 6.85
CHEMBL371026 IC50 = 270.0 nM 6.57
CHEMBL201662 IC50 = 800.0 nM 6.10
CHEMBL201161 IC50 = 1640.0 nM 5.79
CHEMBL371322 IC50 = 1960.0 nM 5.71
CHEMBL202197 IC50 = 2160.0 nM 5.67
CHEMBL201909 IC50 = 3400.0 nM 5.47
CHEMBL370140 IC50 = 5480.0 nM 5.26
CHEMBL370584 IC50 = 5630.0 nM 5.25
CHEMBL202573 IC50 = 7550.0 nM 5.12
CHEMBL199479 IC50 = 7820.0 nM 5.11
CHEMBL202219 IC50 = 8190.0 nM 5.09