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Assay Detail

CHEMBL769458

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Binding
Inhibition of porcine pyruvate dehydrogenase kinase (PDHK)in a primary enzymatic assay
ChEMBL ↗
90
Total Activities
90
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

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

Publication

Anilides of (R)-trifluoro-2-hydroxy-2-methylpropionic acid as inhibitors of pyruvate dehydrogenase kinase.
Bebernitz GR, Aicher TD, Stanton JL, Gao J, Shetty SS, Knorr DC, Strohschein RJ, Tan J, Brand LJ, Liu C, Wang WH, Vinluan CC, Kaplan EL, Dragland CJ, DelGrande D, Islam A, Lozito RJ, Liu X, Maniara WM, Mann WR.
J Med Chem (2000) 43 : 2248 -2257
PubMed 10841803 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 90 6.29 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL73068 — — 1 8.15
CHEMBL74582 — — 1 8.10
CHEMBL73204 — — 1 8.08
CHEMBL75821 — — 1 8.00
CHEMBL73099 — — 1 7.89
CHEMBL307687 — — 1 7.82
CHEMBL75507 — — 1 7.80
CHEMBL450618 — — 1 7.80
CHEMBL306972 — — 1 7.72
CHEMBL72298 — — 1 7.70
CHEMBL308151 — — 1 7.70
CHEMBL72567 — — 1 7.64
CHEMBL306835 — — 1 7.54
CHEMBL73551 — — 1 7.50
CHEMBL72021 — — 1 7.47
CHEMBL72204 — — 1 7.46
CHEMBL73100 — — 1 7.33
CHEMBL74399 — — 1 7.21
CHEMBL415267 — — 1 7.18
CHEMBL73048 — — 1 7.16
CHEMBL421689 — — 1 7.15
CHEMBL306522 — — 1 7.14
CHEMBL306281 — — 1 7.11
CHEMBL70898 — — 1 7.11
CHEMBL76189 — — 1 7.06
CHEMBL310927 — — 1 7.05
CHEMBL70916 — — 1 7.01
CHEMBL303468 — — 1 6.96
CHEMBL308156 — — 1 6.96
CHEMBL75001 — — 1 6.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL73068 — IC50 = 7.1 nM 8.15
CHEMBL74582 — IC50 = 8.0 nM 8.10
CHEMBL73204 — IC50 = 8.4 nM 8.08
CHEMBL75821 — IC50 = 10.0 nM 8.00
CHEMBL73099 — IC50 = 13.0 nM 7.89
CHEMBL307687 — IC50 = 15.0 nM 7.82
CHEMBL75507 — IC50 = 16.0 nM 7.80
CHEMBL450618 — IC50 = 16.0 nM 7.80
CHEMBL306972 — IC50 = 19.0 nM 7.72
CHEMBL72298 — IC50 = 20.0 nM 7.70
CHEMBL308151 — IC50 = 20.0 nM 7.70
CHEMBL72567 — IC50 = 23.0 nM 7.64
CHEMBL306835 — IC50 = 29.0 nM 7.54
CHEMBL73551 — IC50 = 32.0 nM 7.50
CHEMBL72021 — IC50 = 34.0 nM 7.47
CHEMBL72204 — IC50 = 35.0 nM 7.46
CHEMBL73100 — IC50 = 47.0 nM 7.33
CHEMBL74399 — IC50 = 61.0 nM 7.21
CHEMBL415267 — IC50 = 66.0 nM 7.18
CHEMBL73048 — IC50 = 70.0 nM 7.16
CHEMBL421689 — IC50 = 71.0 nM 7.15
CHEMBL306522 — IC50 = 73.0 nM 7.14
CHEMBL306281 — IC50 = 77.0 nM 7.11
CHEMBL70898 — IC50 = 77.0 nM 7.11
CHEMBL76189 — IC50 = 87.0 nM 7.06
CHEMBL310927 — IC50 = 90.0 nM 7.05
CHEMBL70916 — IC50 = 98.0 nM 7.01
CHEMBL303468 — IC50 = 110.0 nM 6.96
CHEMBL308156 — IC50 = 110.0 nM 6.96
CHEMBL75001 — IC50 = 113.0 nM 6.95
CHEMBL74949 — IC50 = 115.0 nM 6.94
CHEMBL421116 — IC50 = 126.0 nM 6.90
CHEMBL73337 — IC50 = 130.0 nM 6.89
CHEMBL73191 — IC50 = 130.0 nM 6.89
CHEMBL306028 — IC50 = 140.0 nM 6.85
CHEMBL73579 — IC50 = 140.0 nM 6.85
CHEMBL70596 — IC50 = 150.0 nM 6.82
CHEMBL72330 — IC50 = 150.0 nM 6.82
CHEMBL75939 — IC50 = 160.0 nM 6.80
CHEMBL72106 — IC50 = 180.0 nM 6.75
CHEMBL73109 — IC50 = 219.0 nM 6.66
CHEMBL74677 — IC50 = 230.0 nM 6.64
CHEMBL308548 — IC50 = 240.0 nM 6.62
CHEMBL76001 — IC50 = 300.0 nM 6.52
CHEMBL75562 — IC50 = 380.0 nM 6.42
CHEMBL72149 — IC50 = 380.0 nM 6.42
CHEMBL70343 — IC50 = 560.0 nM 6.25
CHEMBL73437 — IC50 = 596.0 nM 6.22
CHEMBL73494 — IC50 = 920.0 nM 6.04
CHEMBL74006 — IC50 = 1000.0 nM 6.00