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Assay Detail

CHEMBL951085

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

Binding
Inhibition of human recombinant Akt1
19
Total Activities
19
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

RAC-alpha serine/threonine-protein kinase (CHEMBL4282)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Rapid assembly of diverse and potent allosteric Akt inhibitors.
Wu Z, Robinson RG, Fu S, Barnett SF, Defeo-Jones D, Jones RE, Kral AM, Huber HE, Kohl NE, Hartman GD, Bilodeau MT.
Bioorg Med Chem Lett (2008) 18 : 2211 -2214
PubMed 18296048 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.74 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL253458 1 7.85
CHEMBL253457 1 7.75
CHEMBL255348 1 7.68
CHEMBL255835 1 7.68
CHEMBL258844 1 7.24
CHEMBL402579 1 7.16
CHEMBL402199 1 7.09
CHEMBL270157 1 7.07
CHEMBL401999 1 6.97
CHEMBL401622 1 6.92
CHEMBL255360 1 6.89
CHEMBL255559 1 6.88
CHEMBL270815 1 6.61
CHEMBL270388 1 6.60
CHEMBL429576 1 6.30
CHEMBL255772 1 5.65
CHEMBL362455 1 5.47
CHEMBL402355 1 5.26
CHEMBL257441 1 5.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL253458 IC50 = 14.0 nM 7.85
CHEMBL253457 IC50 = 18.0 nM 7.75
CHEMBL255348 IC50 = 21.0 nM 7.68
CHEMBL255835 IC50 = 21.0 nM 7.68
CHEMBL258844 IC50 = 58.0 nM 7.24
CHEMBL402579 IC50 = 69.0 nM 7.16
CHEMBL402199 IC50 = 81.0 nM 7.09
CHEMBL270157 IC50 = 86.0 nM 7.07
CHEMBL401999 IC50 = 107.0 nM 6.97
CHEMBL401622 IC50 = 121.0 nM 6.92
CHEMBL255360 IC50 = 129.0 nM 6.89
CHEMBL255559 IC50 = 131.0 nM 6.88
CHEMBL270815 IC50 = 244.0 nM 6.61
CHEMBL270388 IC50 = 253.0 nM 6.60
CHEMBL429576 IC50 = 495.0 nM 6.30
CHEMBL255772 IC50 = 2249.0 nM 5.65
CHEMBL362455 IC50 = 3400.0 nM 5.47
CHEMBL402355 IC50 = 5548.0 nM 5.26
CHEMBL257441 IC50 = 8457.0 nM 5.07