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Assay Detail

CHEMBL951580

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Binding
Inhibition of Akt2 phosphorylation in human by C33a cells by IPKA assay
27
Total Activities
27
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type C33a
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

Discovery of potent and cell-active allosteric dual Akt 1 and 2 inhibitors.
Siu T, Liang J, Arruda J, Li Y, Jones RE, Defeo-Jones D, Barnett SF, Robinson RG.
Bioorg Med Chem Lett (2008) 18 : 4186 -4190
PubMed 18539456 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 6.82 7.72
Activity 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL447168 1 7.72
CHEMBL448991 1 7.57
CHEMBL443661 1 7.41
CHEMBL453995 1 7.39
CHEMBL503980 1 7.36
CHEMBL504251 1 7.28
CHEMBL454859 1 7.16
CHEMBL450545 1 7.00
CHEMBL508754 1 6.90
CHEMBL448196 1 6.88
CHEMBL453586 1 6.84
CHEMBL500993 1 6.78
CHEMBL447348 1 6.75
CHEMBL448826 1 6.74
CHEMBL502426 1 6.71
CHEMBL454210 1 6.70
CHEMBL505758 1 6.65
CHEMBL442718 1 6.64
CHEMBL488654 1 6.61
CHEMBL252456 1 6.41
CHEMBL499683 1 6.38
CHEMBL451961 1 6.33
CHEMBL448926 1 6.17
CHEMBL447044 1 6.13
CHEMBL252857 1 6.05
CHEMBL506434 1 -
CHEMBL443633 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL447168 IC50 = 19.0 nM 7.72
CHEMBL448991 IC50 = 27.0 nM 7.57
CHEMBL443661 IC50 = 39.0 nM 7.41
CHEMBL453995 IC50 = 41.0 nM 7.39
CHEMBL503980 IC50 = 44.0 nM 7.36
CHEMBL504251 IC50 = 52.0 nM 7.28
CHEMBL454859 IC50 = 70.0 nM 7.16
CHEMBL450545 IC50 = 101.0 nM 7.00
CHEMBL508754 IC50 = 125.0 nM 6.90
CHEMBL448196 IC50 = 133.0 nM 6.88
CHEMBL453586 IC50 = 145.0 nM 6.84
CHEMBL500993 IC50 = 168.0 nM 6.78
CHEMBL447348 IC50 = 177.0 nM 6.75
CHEMBL448826 IC50 = 184.0 nM 6.74
CHEMBL502426 IC50 = 196.0 nM 6.71
CHEMBL454210 IC50 = 199.0 nM 6.70
CHEMBL505758 IC50 = 223.0 nM 6.65
CHEMBL442718 IC50 = 229.0 nM 6.64
CHEMBL488654 IC50 = 243.0 nM 6.61
CHEMBL252456 IC50 = 388.0 nM 6.41
CHEMBL499683 IC50 = 421.0 nM 6.38
CHEMBL451961 IC50 = 462.0 nM 6.33
CHEMBL448926 IC50 = 684.0 nM 6.17
CHEMBL447044 IC50 = 735.0 nM 6.13
CHEMBL252857 IC50 = 899.0 nM 6.05
CHEMBL506434 Activity - -
CHEMBL443633 Activity - -