Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3721114

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

Binding
Inhibition of pyruvate dehydrogenase kinase (unknown origin) assessed as reduction in E1 phosphorylation incubated for 1 hr by DELFIA method
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Pyruvate dehydrogenase kinase (CHEMBL2096665)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Tetrahydroisoquinoline compounds and their use as pyruvate dehydrogenase kinase inhibitors
(2015)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.50 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3715674 1 8.00
CHEMBL3716865 1 8.00
CHEMBL3714823 1 8.00
CHEMBL3717530 1 8.00
CHEMBL3718330 1 7.00
CHEMBL3717671 1 7.00
CHEMBL3717438 1 7.00
CHEMBL3718579 1 7.00
CHEMBL3717827 1 -
CHEMBL3717940 1 -
CHEMBL3714889 1 -
CHEMBL3717609 1 -
CHEMBL3717986 1 -
CHEMBL3717799 1 -
CHEMBL3714905 1 -
CHEMBL3719348 1 -
CHEMBL3719035 1 -
CHEMBL3718896 1 -
CHEMBL3715964 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3715674 IC50 = 10.0 nM 8.00
CHEMBL3716865 IC50 = 10.0 nM 8.00
CHEMBL3714823 IC50 = 10.0 nM 8.00
CHEMBL3717530 IC50 = 10.0 nM 8.00
CHEMBL3718330 IC50 = 100.0 nM 7.00
CHEMBL3717671 IC50 = 100.0 nM 7.00
CHEMBL3717438 IC50 = 100.0 nM 7.00
CHEMBL3718579 IC50 = 100.0 nM 7.00
CHEMBL3717827 IC50 - -
CHEMBL3717940 IC50 - -
CHEMBL3714889 IC50 - -
CHEMBL3717609 IC50 - -
CHEMBL3717986 IC50 - -
CHEMBL3717799 IC50 - -
CHEMBL3714905 IC50 - -
CHEMBL3719348 IC50 - -
CHEMBL3719035 IC50 - -
CHEMBL3718896 IC50 - -
CHEMBL3715964 IC50 - -