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Assay Detail

CHEMBL3734253

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

Binding
Inhibition of pyruvate dehydrogenase kinase 1 (unknown origin) assessed as reduction in E1alpha phosphorylation incubated for 1 hr by DELFIA method
ChEMBL ↗
105
Total Activities
105
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

Target

[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial (CHEMBL4766) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Resorcinol n-aryl amide compounds, for use as pyruvate dehydrogenase kinase inhibitors
(2015)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 105 6.92 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3729515 — — 1 8.00
CHEMBL3727595 — — 1 8.00
CHEMBL3730756 — — 1 8.00
CHEMBL3732196 — — 1 8.00
CHEMBL3728145 — — 1 8.00
CHEMBL3730985 — — 1 8.00
CHEMBL3731973 — — 1 8.00
CHEMBL3729380 — — 1 8.00
CHEMBL3727499 — — 1 8.00
CHEMBL3728184 — — 1 8.00
CHEMBL3729957 — — 1 8.00
CHEMBL3733181 — — 1 8.00
CHEMBL3732330 — — 1 8.00
CHEMBL3732329 — — 1 8.00
CHEMBL3730908 — — 1 8.00
CHEMBL3727731 — — 1 8.00
CHEMBL3730344 — — 1 8.00
CHEMBL3731590 — — 1 8.00
CHEMBL3729400 — — 1 8.00
CHEMBL3732302 — — 1 8.00
CHEMBL3731468 — — 1 8.00
CHEMBL3727487 — — 1 8.00
CHEMBL3727577 — — 1 8.00
CHEMBL3733014 — — 1 8.00
CHEMBL3732285 — — 1 8.00
CHEMBL3732144 — — 1 8.00
CHEMBL3732532 — — 1 8.00
CHEMBL3730002 — — 1 7.00
CHEMBL3727617 — — 1 7.00
CHEMBL3732766 — — 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3727595 — IC50 = 10.0 nM 8.00
CHEMBL3732285 — IC50 = 10.0 nM 8.00
CHEMBL3733014 — IC50 = 10.0 nM 8.00
CHEMBL3727577 — IC50 = 10.0 nM 8.00
CHEMBL3730985 — IC50 = 10.0 nM 8.00
CHEMBL3732144 — IC50 = 10.0 nM 8.00
CHEMBL3729515 — IC50 = 10.0 nM 8.00
CHEMBL3727487 — IC50 = 10.0 nM 8.00
CHEMBL3731468 — IC50 = 10.0 nM 8.00
CHEMBL3731973 — IC50 = 10.0 nM 8.00
CHEMBL3732532 — IC50 = 10.0 nM 8.00
CHEMBL3729380 — IC50 = 10.0 nM 8.00
CHEMBL3732302 — IC50 = 10.0 nM 8.00
CHEMBL3729400 — IC50 = 10.0 nM 8.00
CHEMBL3731590 — IC50 = 10.0 nM 8.00
CHEMBL3728145 — IC50 = 10.0 nM 8.00
CHEMBL3728184 — IC50 = 10.0 nM 8.00
CHEMBL3730756 — IC50 = 10.0 nM 8.00
CHEMBL3729957 — IC50 = 10.0 nM 8.00
CHEMBL3733181 — IC50 = 10.0 nM 8.00
CHEMBL3732330 — IC50 = 10.0 nM 8.00
CHEMBL3727499 — IC50 = 10.0 nM 8.00
CHEMBL3730908 — IC50 = 10.0 nM 8.00
CHEMBL3727731 — IC50 = 10.0 nM 8.00
CHEMBL3730344 — IC50 = 10.0 nM 8.00
CHEMBL3732196 — IC50 = 10.0 nM 8.00
CHEMBL3732329 — IC50 = 10.0 nM 8.00
CHEMBL3727473 — IC50 = 100.0 nM 7.00
CHEMBL3727925 — IC50 = 100.0 nM 7.00
CHEMBL3727864 — IC50 = 100.0 nM 7.00
CHEMBL3731065 — IC50 = 100.0 nM 7.00
CHEMBL3731057 — IC50 = 100.0 nM 7.00
CHEMBL3730285 — IC50 = 100.0 nM 7.00
CHEMBL3727594 — IC50 = 100.0 nM 7.00
CHEMBL3733286 — IC50 = 100.0 nM 7.00
CHEMBL3732093 — IC50 = 100.0 nM 7.00
CHEMBL3730977 — IC50 = 100.0 nM 7.00
CHEMBL3729659 — IC50 = 100.0 nM 7.00
CHEMBL3730054 — IC50 = 100.0 nM 7.00
CHEMBL3732781 — IC50 = 100.0 nM 7.00
CHEMBL3730414 — IC50 = 100.0 nM 7.00
CHEMBL3728220 — IC50 = 100.0 nM 7.00
CHEMBL3731029 — IC50 = 100.0 nM 7.00
CHEMBL3732739 — IC50 = 100.0 nM 7.00
CHEMBL3732524 — IC50 = 100.0 nM 7.00
CHEMBL3729882 — IC50 = 100.0 nM 7.00
CHEMBL3730103 — IC50 = 100.0 nM 7.00
CHEMBL3732374 — IC50 = 100.0 nM 7.00
CHEMBL3730188 — IC50 = 100.0 nM 7.00
CHEMBL3732826 — IC50 = 100.0 nM 7.00