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Assay Detail

CHEMBL805109

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

Binding
Inhibition of T cell protein tyrosine phosphatase (TC-PTP) at pH 7.0
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Tyrosine-protein phosphatase non-receptor type 2 (CHEMBL3807)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and SAR of a novel selective and orally bioavailable nonpeptide classical competitive inhibitor class of protein-tyrosine phosphatase 1B.
Andersen HS, Olsen OH, Iversen LF, Sørensen AL, Mortensen SB, Christensen MS, Branner S, Hansen TK, Lau JF, Jeppesen L, Moran EJ, Su J, Bakir F, Judge L, Shahbaz M, Collins T, Vo T, Newman MJ, Ripka WC, Møller NP.
J Med Chem (2002) 45 : 4443 -4459
PubMed 12238924 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 4.81 5.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL139393 1 5.03
CHEMBL138461 1 5.00
CHEMBL139074 1 4.96
CHEMBL341947 1 4.92
CHEMBL139196 1 4.92
CHEMBL424652 1 4.92
CHEMBL342603 1 4.89
CHEMBL344368 1 4.77
CHEMBL136867 1 4.72
CHEMBL136044 1 4.66
CHEMBL138951 1 4.62
CHEMBL138277 1 4.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL139393 Ki = 9400.0 nM 5.03
CHEMBL138461 Ki = 10000.0 nM 5.00
CHEMBL139074 Ki = 11000.0 nM 4.96
CHEMBL341947 Ki = 12000.0 nM 4.92
CHEMBL139196 Ki = 12000.0 nM 4.92
CHEMBL424652 Ki = 12000.0 nM 4.92
CHEMBL342603 Ki = 13000.0 nM 4.89
CHEMBL344368 Ki = 17000.0 nM 4.77
CHEMBL136867 Ki = 19000.0 nM 4.72
CHEMBL136044 Ki = 22000.0 nM 4.66
CHEMBL138951 Ki = 24000.0 nM 4.62
CHEMBL138277 Ki = 48000.0 nM 4.32