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Assay Detail

CHEMBL1687390

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

Binding
Displacement of biotinylated phosphatidylinositol-3,4,5-phosphate from mouse AKT1 PH domain by surface plasmon resonance competitive binding assay
49
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

RAC-alpha serine/threonine-protein kinase (CHEMBL5859)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Development of sulfonamide AKT PH domain inhibitors.
Ahad AM, Zuohe S, Du-Cuny L, Moses SA, Zhou LL, Zhang S, Powis G, Meuillet EJ, Mash EA.
Bioorg Med Chem (2011) 19 : 2046 -2054
PubMed 21353784 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 49 5.07 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1685065 PHOSPHATIDYLINOSITOL-TRISPHOSPHATE 1 6.30
CHEMBL1685066 1 5.80
CHEMBL595583 1 5.62
CHEMBL1685055 1 5.37
CHEMBL1681823 1 5.30
CHEMBL1685049 1 5.25
CHEMBL1685058 1 5.22
CHEMBL1685053 1 5.16
CHEMBL1685050 1 5.12
CHEMBL1685057 1 5.12
CHEMBL1685064 1 5.10
CHEMBL1685039 1 5.10
CHEMBL1685042 1 5.05
CHEMBL1685043 1 5.05
CHEMBL1685041 1 5.00
CHEMBL1685038 1 4.96
CHEMBL1685044 1 4.96
CHEMBL1685051 1 4.92
CHEMBL1685040 1 4.92
CHEMBL1685060 1 4.77
CHEMBL1685063 1 4.75
CHEMBL1685056 1 4.72
CHEMBL1685059 1 4.72
CHEMBL595582 1 4.66
CHEMBL1685061 1 4.40
CHEMBL611216 1 4.39
CHEMBL1685052 1 -
CHEMBL1685054 1 -
CHEMBL1685062 1 -
CHEMBL1685045 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1685065 PHOSPHATIDYLINOSITOL-TRISPHOSPHATE Ki = 500.0 nM 6.30
CHEMBL1685066 Ki = 1600.0 nM 5.80
CHEMBL595583 Ki = 2400.0 nM 5.62
CHEMBL1685055 Ki = 4300.0 nM 5.37
CHEMBL1681823 Ki = 5000.0 nM 5.30
CHEMBL1685049 Ki = 5600.0 nM 5.25
CHEMBL1685058 Ki = 6000.0 nM 5.22
CHEMBL1685053 Ki = 7000.0 nM 5.16
CHEMBL1685050 Ki = 7600.0 nM 5.12
CHEMBL1685057 Ki = 7500.0 nM 5.12
CHEMBL1685064 Ki = 8000.0 nM 5.10
CHEMBL1685039 Ki = 8000.0 nM 5.10
CHEMBL1685043 Ki = 9000.0 nM 5.05
CHEMBL1685042 Ki = 9000.0 nM 5.05
CHEMBL1685041 Ki = 10000.0 nM 5.00
CHEMBL1685038 Ki = 11000.0 nM 4.96
CHEMBL1685044 Ki = 11000.0 nM 4.96
CHEMBL1685051 Ki = 12000.0 nM 4.92
CHEMBL1685040 Ki = 12000.0 nM 4.92
CHEMBL1685060 Ki = 17000.0 nM 4.77
CHEMBL1685063 Ki = 18000.0 nM 4.75
CHEMBL1685056 Ki = 19000.0 nM 4.72
CHEMBL1685059 Ki = 19000.0 nM 4.72
CHEMBL595582 Ki = 22000.0 nM 4.66
CHEMBL1685061 Ki = 40000.0 nM 4.40
CHEMBL611216 Ki = 41000.0 nM 4.39
CHEMBL593946 Ki > 50000.0 nM -
CHEMBL1685047 Ki > 50000.0 nM -
CHEMBL1685046 Ki > 50000.0 nM -
CHEMBL286737 Ki > 50000.0 nM -
CHEMBL282021 Ki - -
CHEMBL1685037 Ki - -
CHEMBL1685036 Ki - -
CHEMBL1685035 Ki - -
CHEMBL1685034 Ki - -
CHEMBL1685048 Ki > 50000.0 nM -
CHEMBL1685033 Ki - -
CHEMBL1685032 Ki - -
CHEMBL268439 Ki - -
CHEMBL1685031 Ki - -
CHEMBL1685030 Ki - -
CHEMBL94087 GLYBUTHIAZOL Ki - -
CHEMBL1355299 SULFAETHIDOLE Ki - -
CHEMBL1191 SULFAMETHIZOLE Ki - -
CHEMBL1480108 Ki - -
CHEMBL1685045 Ki > 50000.0 nM -
CHEMBL1685062 Ki > 50000.0 nM -
CHEMBL1685054 Ki > 50000.0 nM -
CHEMBL1685052 Ki > 50000.0 nM -