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Assay Detail

CHEMBL4413208

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

Binding
Binding affinity to recombinant human His-tagged PDK1 expressed in Escherichia coli by isothermal calorimetry
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

High-throughput screening of novel pyruvate dehydrogenase kinases inhibitors and biological evaluation of their in vitro and in vivo antiproliferative activity.
Wu DM, Wang YJ, Fan SH, Zhang ZF, Shan Q, Lu J, Chen GQ, Zheng YL.
Eur J Med Chem (2019) 164 : 252 -262
PubMed 30597326 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 3 5.78 6.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4476534 1 6.06
CHEMBL4434895 1 5.83
CHEMBL4434775 1 5.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4476534 Kd = 870.0 nM 6.06
CHEMBL4434895 Kd = 1490.0 nM 5.83
CHEMBL4434775 Kd = 3500.0 nM 5.46