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Assay Detail

CHEMBL2175186

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Binding
Inhibition of STAT3 SH2 domain assessed as inhibition of STAT3 SH2-phosphotyrosine interaction after 15 mins by fluorescence polarization assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Signal transducer and activator of transcription 3 (CHEMBL4026)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Small molecule inhibitors of signal transducer and activator of transcription 3 (Stat3) protein.
Debnath B, Xu S, Neamati N.
J Med Chem (2012) 55 : 6645 -6668
PubMed 22650325 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 4.57 4.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1829786 1 4.82
CHEMBL2023986 1 4.78
CHEMBL2172014 1 4.73
CHEMBL2023987 1 4.67
CHEMBL2172013 1 4.30
CHEMBL477936 1 4.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1829786 Ki = 15000.0 nM 4.82
CHEMBL2023986 Ki = 16700.0 nM 4.78
CHEMBL2172014 Ki = 18700.0 nM 4.73
CHEMBL2023987 Ki = 21500.0 nM 4.67
CHEMBL2172013 Ki = 50000.0 nM 4.30
CHEMBL477936 Ki = 80000.0 nM 4.10