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Assay Detail

CHEMBL864940

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

Binding
Inhibition of Akt1 in presence of 10 uM ATP
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Identification of a novel 3,5-disubstituted pyridine as a potent, selective, and orally active inhibitor of Akt1 kinase.
Thomas SA, Li T, Woods KW, Song X, Packard G, Fischer JP, Diebold RB, Liu X, Shi Y, Klinghofer V, Johnson EF, Bouska JJ, Olson A, Guan R, Magnone SR, Marsh K, Luo Y, Rosenberg SH, Giranda VL, Li Q.
Bioorg Med Chem Lett (2006) 16 : 3740 -3744
PubMed 16678413 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 7.37 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL379300 A-443654 1 9.80
CHEMBL210403 1 8.96
CHEMBL383264 1 8.70
CHEMBL208790 1 8.68
CHEMBL210740 1 8.49
CHEMBL211018 1 8.46
CHEMBL263510 1 8.18
CHEMBL211827 1 8.17
CHEMBL210349 1 8.08
CHEMBL207338 1 8.08
CHEMBL379218 1 7.96
CHEMBL208606 1 7.26
CHEMBL211865 1 7.20
CHEMBL211186 1 7.15
CHEMBL437122 1 7.07
CHEMBL210020 1 7.05
CHEMBL379868 1 6.73
CHEMBL212098 1 6.71
CHEMBL378870 1 6.63
CHEMBL378759 1 6.61
CHEMBL211084 1 6.54
CHEMBL212259 1 6.43
CHEMBL207373 1 6.33
CHEMBL212157 1 6.20
CHEMBL209638 1 6.17
CHEMBL209358 1 5.82
CHEMBL208612 1 5.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL379300 A-443654 Ki = 0.16 nM 9.80
CHEMBL210403 Ki = 1.1 nM 8.96
CHEMBL383264 Ki = 2.0 nM 8.70
CHEMBL208790 Ki = 2.1 nM 8.68
CHEMBL210740 Ki = 3.2 nM 8.49
CHEMBL211018 Ki = 3.5 nM 8.46
CHEMBL263510 Ki = 6.6 nM 8.18
CHEMBL211827 Ki = 6.8 nM 8.17
CHEMBL210349 Ki = 8.3 nM 8.08
CHEMBL207338 Ki = 8.3 nM 8.08
CHEMBL379218 Ki = 11.0 nM 7.96
CHEMBL208606 Ki = 54.6 nM 7.26
CHEMBL211865 Ki = 63.7 nM 7.20
CHEMBL211186 Ki = 70.6 nM 7.15
CHEMBL437122 Ki = 85.0 nM 7.07
CHEMBL210020 Ki = 89.6 nM 7.05
CHEMBL379868 Ki = 185.0 nM 6.73
CHEMBL212098 Ki = 197.0 nM 6.71
CHEMBL378870 Ki = 233.0 nM 6.63
CHEMBL378759 Ki = 244.0 nM 6.61
CHEMBL211084 Ki = 289.0 nM 6.54
CHEMBL212259 Ki = 368.0 nM 6.43
CHEMBL207373 Ki = 465.0 nM 6.33
CHEMBL212157 Ki = 626.0 nM 6.20
CHEMBL209638 Ki = 672.0 nM 6.17
CHEMBL209358 Ki = 1525.0 nM 5.82
CHEMBL208612 Ki = 3282.0 nM 5.48