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Assay Detail

CHEMBL3871604

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

Binding
Inhibition of GST-tagged Aurora A (123 to 401 residues) (unknown origin) preincubated for 15 mins followed by tetra(LRRWSLG) substrate addition measured for 90 mins by Kinase-Glo luminescence assay
23
Total Activities
23
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 A (CHEMBL4722)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of novel inhibitors of Aurora kinases with indazole scaffold: In silico fragment-based and knowledge-based drug design.
Chang CF, Lin WH, Ke YY, Lin YS, Wang WC, Chen CH, Kuo PC, Hsu JTA, Uang BJ, Hsieh HP.
Eur J Med Chem (2016) 124 : 186 -199
PubMed 27573544 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 6.45 7.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3986609 1 7.58
CHEMBL3946005 1 7.29
CHEMBL3983327 1 7.22
CHEMBL3923159 1 7.18
CHEMBL3975342 1 7.13
CHEMBL3939365 1 7.08
CHEMBL3953964 1 7.07
CHEMBL3922175 1 6.68
CHEMBL3912937 1 6.58
CHEMBL3901797 1 6.58
CHEMBL3974375 1 6.51
CHEMBL3935219 1 6.50
CHEMBL3894492 1 6.32
CHEMBL3954695 1 6.32
CHEMBL3961791 1 6.10
CHEMBL3929110 1 6.10
CHEMBL3909328 1 6.02
CHEMBL3901151 1 5.78
CHEMBL3901743 1 5.54
CHEMBL3972822 1 5.02
CHEMBL3970521 1 4.87
CHEMBL3946537 1 -
CHEMBL3964280 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3986609 IC50 = 26.0 nM 7.58
CHEMBL3946005 IC50 = 51.0 nM 7.29
CHEMBL3983327 IC50 = 60.0 nM 7.22
CHEMBL3923159 IC50 = 66.0 nM 7.18
CHEMBL3975342 IC50 = 74.0 nM 7.13
CHEMBL3939365 IC50 = 83.0 nM 7.08
CHEMBL3953964 IC50 = 85.0 nM 7.07
CHEMBL3922175 IC50 = 208.0 nM 6.68
CHEMBL3912937 IC50 = 260.0 nM 6.58
CHEMBL3901797 IC50 = 260.0 nM 6.58
CHEMBL3974375 IC50 = 310.0 nM 6.51
CHEMBL3935219 IC50 = 314.0 nM 6.50
CHEMBL3894492 IC50 = 480.0 nM 6.32
CHEMBL3954695 IC50 = 480.0 nM 6.32
CHEMBL3961791 IC50 = 790.0 nM 6.10
CHEMBL3929110 IC50 = 790.0 nM 6.10
CHEMBL3909328 IC50 = 950.0 nM 6.02
CHEMBL3901151 IC50 = 1660.0 nM 5.78
CHEMBL3901743 IC50 = 2860.0 nM 5.54
CHEMBL3972822 IC50 = 9610.0 nM 5.02
CHEMBL3970521 IC50 = 13560.0 nM 4.87
CHEMBL3946537 IC50 > 1000.0 nM -
CHEMBL3964280 IC50 > 1000.0 nM -