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Assay Detail

CHEMBL770975

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Binding
Inhibitory activity against Protein-tyrosine phosphatase 1B (PTP 1B) was determined
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Selective protein tyrosine phosphatase 1B inhibitors: targeting the second phosphotyrosine binding site with non-carboxylic acid-containing ligands.
Liu G, Xin Z, Liang H, Abad-Zapatero C, Hajduk PJ, Janowick DA, Szczepankiewicz BG, Pei Z, Hutchins CW, Ballaron SJ, Stashko MA, Lubben TH, Berg CE, Rondinone CM, Trevillyan JM, Jirousek MR.
J Med Chem (2003) 46 : 3437 -3440
PubMed 12877578 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 6.80 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL116605 1 7.75
CHEMBL117496 1 7.40
CHEMBL117699 1 7.38
CHEMBL325029 1 6.92
CHEMBL116692 1 6.89
CHEMBL116901 1 6.43
CHEMBL326830 1 6.41
CHEMBL326829 1 6.25
CHEMBL116744 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL116605 Ki = 18.0 nM 7.75
CHEMBL117496 Ki = 40.0 nM 7.40
CHEMBL117699 Ki = 42.0 nM 7.38
CHEMBL325029 Ki = 120.0 nM 6.92
CHEMBL116692 Ki = 130.0 nM 6.89
CHEMBL116901 Ki = 370.0 nM 6.43
CHEMBL326830 Ki = 390.0 nM 6.41
CHEMBL326829 Ki = 560.0 nM 6.25
CHEMBL116744 Ki = 1600.0 nM 5.80