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Assay Detail

CHEMBL2330886

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

Binding
Inhibition of recombinant Akt1 (unknown origin) using 5-FAM-labeled peptide as substrate after 1 hr by caliper off-chip incubation mobility shift assay
34
Total Activities
34
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

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 7.78 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2325992 1 8.70
CHEMBL2325993 1 8.52
CHEMBL2325741 CAPIVASERTIB 4.0 1 8.52
CHEMBL2325727 1 8.52
CHEMBL2325994 1 8.40
CHEMBL2325743 1 8.40
CHEMBL2325728 1 8.40
CHEMBL2325729 1 8.40
CHEMBL2325738 1 8.40
CHEMBL2325983 1 8.30
CHEMBL2325996 1 8.30
CHEMBL2325995 1 8.30
CHEMBL2325734 1 8.22
CHEMBL2325739 1 8.22
CHEMBL2325736 1 8.15
CHEMBL2325737 1 8.15
CHEMBL2325982 1 8.15
CHEMBL2325997 1 8.10
CHEMBL2325987 1 8.05
CHEMBL2325740 1 8.00
CHEMBL2325733 1 7.92
CHEMBL598194 1 7.89
CHEMBL2325735 1 7.80
CHEMBL2325730 1 7.52
CHEMBL2325732 1 7.51
CHEMBL2325985 1 7.51
CHEMBL2325984 1 7.39
CHEMBL2325731 1 7.38
CHEMBL2325986 1 6.83
CHEMBL2325990 1 6.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2325992 IC50 = 2.0 nM 8.70
CHEMBL2325993 IC50 = 3.0 nM 8.52
CHEMBL2325727 IC50 = 3.0 nM 8.52
CHEMBL2325741 CAPIVASERTIB IC50 = 3.0 nM 8.52
CHEMBL2325994 IC50 = 4.0 nM 8.40
CHEMBL2325743 IC50 = 4.0 nM 8.40
CHEMBL2325728 IC50 = 4.0 nM 8.40
CHEMBL2325729 IC50 = 4.0 nM 8.40
CHEMBL2325738 IC50 = 4.0 nM 8.40
CHEMBL2325983 IC50 = 5.0 nM 8.30
CHEMBL2325996 IC50 = 5.0 nM 8.30
CHEMBL2325995 IC50 = 5.0 nM 8.30
CHEMBL2325734 IC50 = 6.0 nM 8.22
CHEMBL2325739 IC50 = 6.0 nM 8.22
CHEMBL2325982 IC50 = 7.0 nM 8.15
CHEMBL2325736 IC50 = 7.0 nM 8.15
CHEMBL2325737 IC50 = 7.0 nM 8.15
CHEMBL2325997 IC50 = 8.0 nM 8.10
CHEMBL2325987 IC50 = 9.0 nM 8.05
CHEMBL2325740 IC50 = 10.0 nM 8.00
CHEMBL2325733 IC50 = 12.0 nM 7.92
CHEMBL598194 IC50 = 13.0 nM 7.89
CHEMBL2325735 IC50 = 16.0 nM 7.80
CHEMBL2325730 IC50 = 30.0 nM 7.52
CHEMBL2325732 IC50 = 31.0 nM 7.51
CHEMBL2325985 IC50 = 31.0 nM 7.51
CHEMBL2325984 IC50 = 41.0 nM 7.39
CHEMBL2325731 IC50 = 42.0 nM 7.38
CHEMBL2325986 IC50 = 149.0 nM 6.83
CHEMBL2325990 IC50 = 183.0 nM 6.74
CHEMBL2325742 IC50 = 276.0 nM 6.56
CHEMBL2325991 IC50 = 1192.0 nM 5.92
CHEMBL2325988 IC50 = 1313.0 nM 5.88
CHEMBL2325989 IC50 = 2753.0 nM 5.56