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Assay Detail

CHEMBL5629494

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

Binding
Binding affinity to human partial length AURKB (D25 to A303 residues) expressed in mammalian system assessed as dissociation constant by DiscoverX kinomescan assay
8
Total Activities
8
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

Aurora kinase B (CHEMBL2185)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and evaluation of dual EGFR/AURKB inhibitors as anticancer agents for non-small cell lung cancer.
Kurup S, Gesinski D, Assaad K, Reynolds A.
Bioorg Med Chem Lett (2024) 100 : 129612 -129612
PubMed 38199330 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 8 5.91 6.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5633661 1 6.62
CHEMBL388978 STAUROSPORINE 1 6.36
CHEMBL5633878 1 6.33
CHEMBL5632112 1 5.82
CHEMBL5181237 1 5.32
CHEMBL5200160 1 5.01
CHEMBL5632436 1 -
CHEMBL202721 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5633661 Kd = 240.0 nM 6.62
CHEMBL388978 STAUROSPORINE Kd = 440.0 nM 6.36
CHEMBL5633878 Kd = 470.0 nM 6.33
CHEMBL5632112 Kd = 1500.0 nM 5.82
CHEMBL5181237 Kd = 4800.0 nM 5.32
CHEMBL5200160 Kd = 9800.0 nM 5.01
CHEMBL5632436 Kd > 30000.0 nM -
CHEMBL202721 Kd - -