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Assay Detail

CHEMBL2330883

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

Binding
Inhibition of Akt in human MDA-MB-468 cells assessed as inhibition of GSK3beta phosphorylation after 2 hrs by laser scanning cytometry
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MDA-MB-468
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of 4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363), an orally bioavailable, potent inhibitor of Akt kinases.
Addie M, Ballard P, Buttar D, Crafter C, Currie G, Davies BR, Debreczeni J, Dry H, Dudley P, Greenwood R, Johnson PD, Kettle JG, Lane C, Lamont G, Leach A, Luke RW, Morris J, Ogilvie D, Page K, Pass M, Pearson S, Ruston L.
J Med Chem (2013) 56 : 2059 -2073
PubMed 23394218 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 6.42 7.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2325728 1 7.37
CHEMBL2325729 1 7.11
CHEMBL2325996 1 7.09
CHEMBL2325741 CAPIVASERTIB 4.0 1 7.05
CHEMBL2325738 1 7.04
CHEMBL2325992 1 7.02
CHEMBL2325727 1 6.96
CHEMBL2325993 1 6.90
CHEMBL2325743 1 6.87
CHEMBL2325739 1 6.86
CHEMBL2325982 1 6.84
CHEMBL2325995 1 6.81
CHEMBL2325997 1 6.71
CHEMBL2325983 1 6.68
CHEMBL2325994 1 6.68
CHEMBL2325740 1 6.52
CHEMBL2325737 1 6.52
CHEMBL598194 1 6.48
CHEMBL2325736 1 6.38
CHEMBL2325733 1 6.31
CHEMBL2325731 1 6.17
CHEMBL2325734 1 6.06
CHEMBL2325735 1 6.00
CHEMBL2325730 1 5.95
CHEMBL2325984 1 5.79
CHEMBL2325985 1 5.78
CHEMBL2325987 1 5.75
CHEMBL2325732 1 5.54
CHEMBL2325742 1 5.34
CHEMBL2325990 1 5.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2325728 IC50 = 43.0 nM 7.37
CHEMBL2325729 IC50 = 78.0 nM 7.11
CHEMBL2325996 IC50 = 81.0 nM 7.09
CHEMBL2325741 CAPIVASERTIB IC50 = 89.0 nM 7.05
CHEMBL2325738 IC50 = 91.0 nM 7.04
CHEMBL2325992 IC50 = 96.0 nM 7.02
CHEMBL2325727 IC50 = 110.0 nM 6.96
CHEMBL2325993 IC50 = 126.0 nM 6.90
CHEMBL2325743 IC50 = 134.0 nM 6.87
CHEMBL2325739 IC50 = 138.0 nM 6.86
CHEMBL2325982 IC50 = 144.0 nM 6.84
CHEMBL2325995 IC50 = 156.0 nM 6.81
CHEMBL2325997 IC50 = 197.0 nM 6.71
CHEMBL2325983 IC50 = 208.0 nM 6.68
CHEMBL2325994 IC50 = 209.0 nM 6.68
CHEMBL2325740 IC50 = 303.0 nM 6.52
CHEMBL2325737 IC50 = 302.0 nM 6.52
CHEMBL598194 IC50 = 328.0 nM 6.48
CHEMBL2325736 IC50 = 414.0 nM 6.38
CHEMBL2325733 IC50 = 489.0 nM 6.31
CHEMBL2325731 IC50 = 681.0 nM 6.17
CHEMBL2325734 IC50 = 874.0 nM 6.06
CHEMBL2325735 IC50 = 995.0 nM 6.00
CHEMBL2325730 IC50 = 1126.0 nM 5.95
CHEMBL2325984 IC50 = 1620.0 nM 5.79
CHEMBL2325985 IC50 = 1650.0 nM 5.78
CHEMBL2325987 IC50 = 1776.0 nM 5.75
CHEMBL2325732 IC50 = 2893.0 nM 5.54
CHEMBL2325742 IC50 = 4594.0 nM 5.34
CHEMBL2325990 IC50 = 5165.0 nM 5.29
CHEMBL2325986 IC50 = 6710.0 nM 5.17
CHEMBL2325989 IC50 > 3250.0 nM -
CHEMBL2325988 IC50 > 30132.0 nM -
CHEMBL2325991 IC50 > 3250.0 nM -