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Assay Detail

CHEMBL3707758

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Binding
Enzyme Assay: The Aurora assays described here are performed on two Caliper Life Sciences systems: the LC3000 and the Desktop Profiler. These provide data on enzyme activity via measurement of the relative amounts of phosphorylated or unphosphorylated fluorescently labelled substrate peptide at the end of an enzymatic reaction. These different states of peptide are resolved by applying a potential difference across the sample. The presence of the charged phosphate group on the product (as opposed to the substrate) causes a different peptide mobility between the two peptides. This is visualized by excitation of the fluorescent label on the substrate and product peptides and represented as peaks within the analysis software.
251
Total Activities
251
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

Amino azaheterocyclic carboxamides
(2014)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 251 8.43 10.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3680444 1 10.38
CHEMBL3680508 1 10.35
CHEMBL3680447 1 10.34
CHEMBL3680552 1 10.22
CHEMBL3685243 1 10.21
CHEMBL3685277 1 10.05
CHEMBL3675525 1 9.77
CHEMBL3685262 1 9.74
CHEMBL3680596 1 9.74
CHEMBL3639841 1 9.70
CHEMBL3685245 1 9.68
CHEMBL3685306 1 9.66
CHEMBL3670499 1 9.62
CHEMBL3675441 1 9.60
CHEMBL3680500 1 9.59
CHEMBL3680420 1 9.57
CHEMBL3680554 1 9.52
CHEMBL3680403 1 9.52
CHEMBL3685257 1 9.51
CHEMBL3675501 1 9.49
CHEMBL3685237 1 9.48
CHEMBL3675459 1 9.46
CHEMBL3675446 1 9.46
CHEMBL3670467 1 9.46
CHEMBL3685250 1 9.42
CHEMBL3685252 1 9.42
CHEMBL3680550 1 9.42
CHEMBL3680572 1 9.41
CHEMBL3675444 1 9.40
CHEMBL3675493 1 9.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3680444 IC50 = 0.042 nM 10.38
CHEMBL3680508 IC50 = 0.045 nM 10.35
CHEMBL3680447 IC50 = 0.046 nM 10.34
CHEMBL3680552 IC50 = 0.06 nM 10.22
CHEMBL3685243 IC50 = 0.061 nM 10.21
CHEMBL3685277 IC50 = 0.089 nM 10.05
CHEMBL3675525 IC50 = 0.17 nM 9.77
CHEMBL3680596 IC50 = 0.18 nM 9.74
CHEMBL3685262 IC50 = 0.18 nM 9.74
CHEMBL3639841 IC50 = 0.2 nM 9.70
CHEMBL3685245 IC50 = 0.21 nM 9.68
CHEMBL3685306 IC50 = 0.22 nM 9.66
CHEMBL3670499 IC50 = 0.24 nM 9.62
CHEMBL3675441 IC50 = 0.25 nM 9.60
CHEMBL3680500 IC50 = 0.26 nM 9.59
CHEMBL3680420 IC50 = 0.27 nM 9.57
CHEMBL3680403 IC50 = 0.3 nM 9.52
CHEMBL3680554 IC50 = 0.3 nM 9.52
CHEMBL3685257 IC50 = 0.31 nM 9.51
CHEMBL3675501 IC50 = 0.32 nM 9.49
CHEMBL3685237 IC50 = 0.33 nM 9.48
CHEMBL3670467 IC50 = 0.35 nM 9.46
CHEMBL3675446 IC50 = 0.35 nM 9.46
CHEMBL3675459 IC50 = 0.35 nM 9.46
CHEMBL3680550 IC50 = 0.38 nM 9.42
CHEMBL3685250 IC50 = 0.38 nM 9.42
CHEMBL3685252 IC50 = 0.38 nM 9.42
CHEMBL3680572 IC50 = 0.39 nM 9.41
CHEMBL3675444 IC50 = 0.4 nM 9.40
CHEMBL3675493 IC50 = 0.4 nM 9.40
CHEMBL3680460 IC50 = 0.41 nM 9.39
CHEMBL3675438 IC50 = 0.43 nM 9.37
CHEMBL3670485 IC50 = 0.46 nM 9.34
CHEMBL3680417 IC50 = 0.46 nM 9.34
CHEMBL3675510 IC50 = 0.47 nM 9.33
CHEMBL3680522 IC50 = 0.5 nM 9.30
CHEMBL3685249 IC50 = 0.5 nM 9.30
CHEMBL3680587 IC50 = 0.5 nM 9.30
CHEMBL3680588 IC50 = 0.5 nM 9.30
CHEMBL3680455 IC50 = 0.51 nM 9.29
CHEMBL3685272 IC50 = 0.52 nM 9.28
CHEMBL3670470 IC50 = 0.52 nM 9.28
CHEMBL3680599 IC50 = 0.54 nM 9.27
CHEMBL3680421 IC50 = 0.58 nM 9.24
CHEMBL3680467 IC50 = 0.58 nM 9.24
CHEMBL3680446 IC50 = 0.57 nM 9.24
CHEMBL3639742 IC50 = 0.59 nM 9.23
CHEMBL3685307 IC50 = 0.6 nM 9.22
CHEMBL3685268 IC50 = 0.62 nM 9.21
CHEMBL3675466 IC50 = 0.66 nM 9.18