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Assay Detail

CHEMBL3243854

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

Binding
Inhibition of Aurora A (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition measured after 60 mins
28
Total Activities
28
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

Design, synthesis and bioevaluation of N-trisubstituted pyrimidine derivatives as potent aurora A kinase inhibitors.
Luo Y, Deng YQ, Wang J, Long ZJ, Tu ZC, Peng W, Zhang JQ, Liu Q, Lu G.
Eur J Med Chem (2014) 78 : 65 -71
PubMed 24681066 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 7.33 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3237167 1 8.30
CHEMBL3237169 1 8.11
CHEMBL3237166 1 8.10
CHEMBL3237187 1 8.00
CHEMBL3237168 1 7.96
CHEMBL3237164 1 7.92
CHEMBL3237188 1 7.89
CHEMBL3237165 1 7.80
CHEMBL3237181 1 7.66
CHEMBL3237184 1 7.66
CHEMBL3237174 1 7.60
CHEMBL3237180 1 7.50
CHEMBL3237176 1 7.47
CHEMBL3237185 1 7.47
CHEMBL3237172 1 7.34
CHEMBL3237179 1 7.14
CHEMBL3237171 1 7.01
CHEMBL3237182 1 7.00
CHEMBL3237190 1 6.95
CHEMBL3237175 1 6.95
CHEMBL3237189 1 6.93
CHEMBL3237170 1 6.90
CHEMBL3237173 1 6.87
CHEMBL3237186 1 6.83
CHEMBL3237183 1 6.70
CHEMBL3237178 1 6.64
CHEMBL3237163 1 6.26
CHEMBL3237177 1 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3237167 IC50 = 5.0 nM 8.30
CHEMBL3237169 IC50 = 7.7 nM 8.11
CHEMBL3237166 IC50 = 8.0 nM 8.10
CHEMBL3237187 IC50 = 10.0 nM 8.00
CHEMBL3237168 IC50 = 11.0 nM 7.96
CHEMBL3237164 IC50 = 12.0 nM 7.92
CHEMBL3237188 IC50 = 13.0 nM 7.89
CHEMBL3237165 IC50 = 16.0 nM 7.80
CHEMBL3237181 IC50 = 22.0 nM 7.66
CHEMBL3237184 IC50 = 22.0 nM 7.66
CHEMBL3237174 IC50 = 25.0 nM 7.60
CHEMBL3237180 IC50 = 32.0 nM 7.50
CHEMBL3237176 IC50 = 34.0 nM 7.47
CHEMBL3237185 IC50 = 34.0 nM 7.47
CHEMBL3237172 IC50 = 46.0 nM 7.34
CHEMBL3237179 IC50 = 72.0 nM 7.14
CHEMBL3237171 IC50 = 97.0 nM 7.01
CHEMBL3237182 IC50 = 101.0 nM 7.00
CHEMBL3237190 IC50 = 112.0 nM 6.95
CHEMBL3237175 IC50 = 113.0 nM 6.95
CHEMBL3237189 IC50 = 118.0 nM 6.93
CHEMBL3237170 IC50 = 127.0 nM 6.90
CHEMBL3237173 IC50 = 135.0 nM 6.87
CHEMBL3237186 IC50 = 147.0 nM 6.83
CHEMBL3237183 IC50 = 200.0 nM 6.70
CHEMBL3237178 IC50 = 228.0 nM 6.64
CHEMBL3237163 IC50 = 549.0 nM 6.26
CHEMBL3237177 IC50 = 573.0 nM 6.24