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Assay Detail

CHEMBL928488

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

Binding
Inhibition of Akt2 in human C33A cells by immunoprecipitation kinase assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type C-33-A
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

RAC-beta serine/threonine-protein kinase (CHEMBL2431)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of pyridopyrimidines as potent Akt1/2 inhibitors.
Wu Z, Hartnett JC, Neilson LA, Robinson RG, Fu S, Barnett SF, Defeo-Jones D, Jones RE, Kral AM, Huber HE, Hartman GD, Bilodeau MT.
Bioorg Med Chem Lett (2008) 18 : 1274 -1279
PubMed 18249537 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.85 6.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL253458 1 6.33
CHEMBL404555 1 6.23
CHEMBL254099 1 6.23
CHEMBL404554 1 6.20
CHEMBL253693 1 6.08
CHEMBL252857 1 6.05
CHEMBL252856 1 5.95
CHEMBL403356 1 5.80
CHEMBL253457 1 5.74
CHEMBL404347 1 5.64
CHEMBL404556 1 5.43
CHEMBL252652 1 5.28
CHEMBL252457 1 5.03
CHEMBL404553 1 -
CHEMBL252654 1 -
CHEMBL252653 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL253458 IC50 = 468.0 nM 6.33
CHEMBL404555 IC50 = 586.0 nM 6.23
CHEMBL254099 IC50 = 589.0 nM 6.23
CHEMBL404554 IC50 = 635.0 nM 6.20
CHEMBL253693 IC50 = 828.0 nM 6.08
CHEMBL252857 IC50 = 899.0 nM 6.05
CHEMBL252856 IC50 = 1131.0 nM 5.95
CHEMBL403356 IC50 = 1572.0 nM 5.80
CHEMBL253457 IC50 = 1811.0 nM 5.74
CHEMBL404347 IC50 = 2295.0 nM 5.64
CHEMBL404556 IC50 = 3706.0 nM 5.43
CHEMBL252652 IC50 = 5296.0 nM 5.28
CHEMBL252457 IC50 = 9259.0 nM 5.03
CHEMBL404553 IC50 - -
CHEMBL252654 IC50 - -
CHEMBL252653 IC50 - -