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Assay Detail

CHEMBL5135563

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

Binding
Inhibition of PKL (unknown origin) for 30 mins by Kinase-Glo Max reagent based luminescence assay
40
Total Activities
40
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 kinase PKLR (CHEMBL1075126)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Anthraquinone derivatives as ADP-competitive inhibitors of liver pyruvate kinase.
Nain-Perez A, Foller Füchtbauer A, Håversen L, Lulla A, Gao C, Matic J, Monjas L, Rodríguez A, Brear P, Kim W, Hyvönen M, Borén J, Mardinoglu A, Uhlen M, Grøtli M.
Eur J Med Chem (2022) 234 : 114270 -114270
PubMed 35290845 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 40 5.91 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5204170 1 6.82
CHEMBL5209097 1 6.80
CHEMBL175336 Alizarin Red S 1 6.70
CHEMBL5176753 1 6.70
CHEMBL5208105 1 6.70
CHEMBL5176181 1 6.54
CHEMBL5181251 1 6.52
CHEMBL5204537 1 6.26
CHEMBL5188496 1 6.16
CHEMBL5183208 1 6.05
CHEMBL5186564 1 5.92
CHEMBL5206382 1 5.89
CHEMBL5195754 1 5.89
CHEMBL5186706 1 5.85
CHEMBL5181273 1 5.85
CHEMBL5200212 1 5.77
CHEMBL5198643 1 5.72
CHEMBL5177546 1 5.60
CHEMBL5170574 1 5.47
CHEMBL5169856 1 5.42
CHEMBL5172724 1 5.39
CHEMBL5170819 1 5.32
CHEMBL5172682 1 5.24
CHEMBL5193313 1 5.14
CHEMBL5209293 1 5.12
CHEMBL5188932 1 4.72
CHEMBL5195101 1 -
CHEMBL5204502 1 -
CHEMBL5181117 1 -
CHEMBL5198598 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5204170 IC50 = 150.0 nM 6.82
CHEMBL5209097 IC50 = 160.0 nM 6.80
CHEMBL5176753 IC50 = 200.0 nM 6.70
CHEMBL5208105 IC50 = 200.0 nM 6.70
CHEMBL175336 Alizarin Red S IC50 = 200.0 nM 6.70
CHEMBL5176181 IC50 = 290.0 nM 6.54
CHEMBL5181251 IC50 = 300.0 nM 6.52
CHEMBL5204537 IC50 = 550.0 nM 6.26
CHEMBL5188496 IC50 = 700.0 nM 6.16
CHEMBL5183208 IC50 = 900.0 nM 6.05
CHEMBL5186564 IC50 = 1200.0 nM 5.92
CHEMBL5206382 IC50 = 1300.0 nM 5.89
CHEMBL5195754 IC50 = 1300.0 nM 5.89
CHEMBL5186706 IC50 = 1400.0 nM 5.85
CHEMBL5181273 IC50 = 1400.0 nM 5.85
CHEMBL5200212 IC50 = 1700.0 nM 5.77
CHEMBL5198643 IC50 = 1900.0 nM 5.72
CHEMBL5177546 IC50 = 2500.0 nM 5.60
CHEMBL5170574 IC50 = 3400.0 nM 5.47
CHEMBL5169856 IC50 = 3800.0 nM 5.42
CHEMBL5172724 IC50 = 4100.0 nM 5.39
CHEMBL5170819 IC50 = 4800.0 nM 5.32
CHEMBL5172682 IC50 = 5800.0 nM 5.24
CHEMBL5193313 IC50 = 7300.0 nM 5.14
CHEMBL5209293 IC50 = 7500.0 nM 5.12
CHEMBL5188932 IC50 = 19000.0 nM 4.72
CHEMBL3184279 IC50 - -
CHEMBL55814 ATHRAQUINONES A IC50 - -
CHEMBL5203032 IC50 - -
CHEMBL5171288 IC50 - -
CHEMBL5200574 IC50 - -
CHEMBL5180931 IC50 - -
CHEMBL5176055 IC50 - -
CHEMBL5177528 IC50 - -
CHEMBL5184973 IC50 - -
CHEMBL5175459 IC50 - -
CHEMBL5198598 IC50 - -
CHEMBL5181117 IC50 - -
CHEMBL5204502 IC50 - -
CHEMBL5195101 IC50 - -