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Assay Detail

CHEMBL896127

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Binding
Inhibition of human recombinant TCPTP
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structure-based optimization of protein tyrosine phosphatase 1B inhibitors: from the active site to the second phosphotyrosine binding site.
Wilson DP, Wan ZK, Xu WX, Kirincich SJ, Follows BC, Joseph-McCarthy D, Foreman K, Moretto A, Wu J, Zhu M, Binnun E, Zhang YL, Tam M, Erbe DV, Tobin J, Xu X, Leung L, Shilling A, Tam SY, Mansour TS, Lee J.
J Med Chem (2007) 50 : 4681 -4698
PubMed 17705360 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 8.13 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL230862 1 8.70
CHEMBL230860 1 8.70
CHEMBL230751 1 8.70
CHEMBL395722 1 8.70
CHEMBL230645 1 8.40
CHEMBL541214 1 8.30
CHEMBL397415 1 8.30
CHEMBL243267 1 8.30
CHEMBL387614 1 8.22
CHEMBL390245 1 8.22
CHEMBL230752 1 8.10
CHEMBL243268 1 8.05
CHEMBL390244 1 8.05
CHEMBL230643 1 8.00
CHEMBL397903 1 7.92
CHEMBL243942 1 7.58
CHEMBL213758 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL230862 Ki = 2.0 nM 8.70
CHEMBL230860 Ki = 2.0 nM 8.70
CHEMBL230751 Ki = 2.0 nM 8.70
CHEMBL395722 Ki = 2.0 nM 8.70
CHEMBL230645 Ki = 4.0 nM 8.40
CHEMBL541214 Ki = 5.0 nM 8.30
CHEMBL397415 Ki = 5.0 nM 8.30
CHEMBL243267 Ki = 5.0 nM 8.30
CHEMBL387614 Ki = 6.0 nM 8.22
CHEMBL390245 Ki = 6.0 nM 8.22
CHEMBL230752 Ki = 8.0 nM 8.10
CHEMBL243268 Ki = 9.0 nM 8.05
CHEMBL390244 Ki = 9.0 nM 8.05
CHEMBL230643 Ki = 10.0 nM 8.00
CHEMBL397903 Ki = 12.0 nM 7.92
CHEMBL243942 Ki = 26.0 nM 7.58
CHEMBL213758 Ki = 1300.0 nM 5.89