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Assay Detail

CHEMBL772648

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

Binding
Inhibition of human recombinant Protein-tyrosine phosphatase 1B.
20
Total Activities
19
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

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 20 4.97 5.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL140120 2 5.50
CHEMBL139393 1 5.33
CHEMBL138106 1 5.23
CHEMBL424652 1 5.14
CHEMBL139196 1 5.10
CHEMBL137989 1 5.08
CHEMBL342603 1 5.06
CHEMBL341947 1 5.05
CHEMBL136044 1 4.96
CHEMBL139074 1 4.96
CHEMBL136867 1 4.92
CHEMBL140757 1 4.92
CHEMBL138240 1 4.92
CHEMBL138951 1 4.85
CHEMBL138461 1 4.82
CHEMBL344368 1 4.80
CHEMBL138277 1 4.64
CHEMBL136316 1 4.54
CHEMBL138995 1 4.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL140120 Ki = 3200.0 nM 5.50
CHEMBL139393 Ki = 4700.0 nM 5.33
CHEMBL138106 Ki = 5900.0 nM 5.23
CHEMBL140120 Ki = 7200.0 nM 5.14
CHEMBL424652 Ki = 7300.0 nM 5.14
CHEMBL139196 Ki = 8000.0 nM 5.10
CHEMBL137989 Ki = 8300.0 nM 5.08
CHEMBL342603 Ki = 8700.0 nM 5.06
CHEMBL341947 Ki = 9000.0 nM 5.05
CHEMBL139074 Ki = 11000.0 nM 4.96
CHEMBL136044 Ki = 11000.0 nM 4.96
CHEMBL140757 Ki = 12000.0 nM 4.92
CHEMBL138240 Ki = 12000.0 nM 4.92
CHEMBL136867 Ki = 12000.0 nM 4.92
CHEMBL138951 Ki = 14000.0 nM 4.85
CHEMBL138461 Ki = 15000.0 nM 4.82
CHEMBL344368 Ki = 16000.0 nM 4.80
CHEMBL138277 Ki = 23000.0 nM 4.64
CHEMBL136316 Ki = 29000.0 nM 4.54
CHEMBL138995 Ki = 42000.0 nM 4.38