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Assay Detail

CHEMBL869532

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

Binding
Inhibition of ERK2 using 10 uM ATP
2
Total Activities
2
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

Mitogen-activated protein kinase 1 (CHEMBL4040)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of trans-3,4'-bispyridinylethylenes as potent and novel inhibitors of protein kinase B (PKB/Akt) for the treatment of cancer: Synthesis and biological evaluation.
Li Q, Li T, Zhu GD, Gong J, Claibone A, Dalton C, Luo Y, Johnson EF, Shi Y, Liu X, Klinghofer V, Bauch JL, Marsh KC, Bouska JJ, Arries S, De Jong R, Oltersdorf T, Stoll VS, Jakob CG, Rosenberg SH, Giranda VL.
Bioorg Med Chem Lett (2006) 16 : 1679 -1685
PubMed 16403626 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.66 6.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388978 STAUROSPORINE 1 6.43
CHEMBL383541 1 4.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388978 STAUROSPORINE IC50 = 370.0 nM 6.43
CHEMBL383541 IC50 = 12850.0 nM 4.89