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Assay Detail

CHEMBL928491

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

Binding
Inhibition of Akt1
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Development of pyridopyrimidines as potent Akt1/2 inhibitors.
Wu Z, Hartnett JC, Neilson LA, Robinson RG, Fu S, Barnett SF, Defeo-Jones D, Jones RE, Kral AM, Huber HE, Hartman GD, Bilodeau MT.
Bioorg Med Chem Lett (2008) 18 : 1274 -1279
PubMed 18249537 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 7.36 8.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL254099 1 8.42
CHEMBL253693 1 8.40
CHEMBL404554 1 8.35
CHEMBL252857 1 8.22
CHEMBL404556 1 8.21
CHEMBL403356 1 8.07
CHEMBL252856 1 8.01
CHEMBL253458 1 7.85
CHEMBL252456 1 7.82
CHEMBL253457 1 7.75
CHEMBL404347 1 7.63
CHEMBL404555 1 7.62
CHEMBL252457 1 7.54
CHEMBL252455 1 7.34
CHEMBL252261 1 7.20
CHEMBL404553 1 7.19
CHEMBL252652 1 7.09
CHEMBL403354 1 7.05
CHEMBL252653 1 7.04
CHEMBL252054 1 7.00
CHEMBL252259 1 6.86
CHEMBL252055 1 6.86
CHEMBL403355 1 6.79
CHEMBL252056 1 6.70
CHEMBL276130 1 6.65
CHEMBL252654 1 6.54
CHEMBL251860 1 6.12
CHEMBL252260 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL254099 IC50 = 3.8 nM 8.42
CHEMBL253693 IC50 = 4.0 nM 8.40
CHEMBL404554 IC50 = 4.5 nM 8.35
CHEMBL252857 IC50 = 6.0 nM 8.22
CHEMBL404556 IC50 = 6.2 nM 8.21
CHEMBL403356 IC50 = 8.5 nM 8.07
CHEMBL252856 IC50 = 9.7 nM 8.01
CHEMBL253458 IC50 = 14.0 nM 7.85
CHEMBL252456 IC50 = 15.0 nM 7.82
CHEMBL253457 IC50 = 18.0 nM 7.75
CHEMBL404347 IC50 = 23.6 nM 7.63
CHEMBL404555 IC50 = 24.0 nM 7.62
CHEMBL252457 IC50 = 29.0 nM 7.54
CHEMBL252455 IC50 = 46.0 nM 7.34
CHEMBL252261 IC50 = 63.0 nM 7.20
CHEMBL404553 IC50 = 64.0 nM 7.19
CHEMBL252652 IC50 = 81.0 nM 7.09
CHEMBL403354 IC50 = 90.0 nM 7.05
CHEMBL252653 IC50 = 91.0 nM 7.04
CHEMBL252054 IC50 = 99.0 nM 7.00
CHEMBL252259 IC50 = 137.0 nM 6.86
CHEMBL252055 IC50 = 139.0 nM 6.86
CHEMBL403355 IC50 = 162.0 nM 6.79
CHEMBL252056 IC50 = 198.0 nM 6.70
CHEMBL276130 IC50 = 226.0 nM 6.65
CHEMBL252654 IC50 = 286.0 nM 6.54
CHEMBL251860 IC50 = 765.0 nM 6.12
CHEMBL252260 IC50 = 1521.0 nM 5.82