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Assay Detail

CHEMBL2073499

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

Binding
Inhibition of Aurora B kinase by HTRF analysis in presence of 1 mM ATP
34
Total Activities
34
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

Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases.
Curtin ML, Heyman HR, Frey RR, Marcotte PA, Glaser KB, Jankowski JR, Magoc TJ, Albert DH, Olson AM, Reuter DR, Bouska JJ, Montgomery DA, Palma JP, Donawho CK, Stewart KD, Tse C, Michaelides MR.
Bioorg Med Chem Lett (2012) 22 : 4750 -4755
PubMed 22695126 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 7.44 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1980297 ILORASERTIB 2.0 1 8.15
CHEMBL2071216 1 8.10
CHEMBL2071210 1 8.10
CHEMBL2071276 1 7.92
CHEMBL2071275 1 7.92
CHEMBL2071217 1 7.92
CHEMBL2071277 1 7.82
CHEMBL2071199 1 7.82
CHEMBL2071209 1 7.80
CHEMBL2071270 1 7.72
CHEMBL2071272 1 7.60
CHEMBL2071273 1 7.58
CHEMBL2071274 1 7.57
CHEMBL2071200 1 7.55
CHEMBL2071194 1 7.54
CHEMBL2071202 1 7.54
CHEMBL2071211 1 7.51
CHEMBL2071271 1 7.50
CHEMBL2071214 1 7.50
CHEMBL2071201 1 7.38
CHEMBL2071205 1 7.37
CHEMBL2071215 1 7.36
CHEMBL2071206 1 7.35
CHEMBL2071207 1 7.29
CHEMBL1614709 1 7.27
CHEMBL2071204 1 7.21
CHEMBL2071203 1 7.18
CHEMBL2071208 1 7.00
CHEMBL2071212 1 6.93
CHEMBL2071213 1 6.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1980297 ILORASERTIB IC50 = 7.0 nM 8.15
CHEMBL2071216 IC50 = 8.0 nM 8.10
CHEMBL2071210 IC50 = 8.0 nM 8.10
CHEMBL2071276 IC50 = 12.0 nM 7.92
CHEMBL2071275 IC50 = 12.0 nM 7.92
CHEMBL2071217 IC50 = 12.0 nM 7.92
CHEMBL2071277 IC50 = 15.0 nM 7.82
CHEMBL2071199 IC50 = 15.0 nM 7.82
CHEMBL2071209 IC50 = 16.0 nM 7.80
CHEMBL2071270 IC50 = 19.0 nM 7.72
CHEMBL2071272 IC50 = 25.0 nM 7.60
CHEMBL2071273 IC50 = 26.0 nM 7.58
CHEMBL2071274 IC50 = 27.0 nM 7.57
CHEMBL2071200 IC50 = 28.0 nM 7.55
CHEMBL2071202 IC50 = 29.0 nM 7.54
CHEMBL2071194 IC50 = 29.0 nM 7.54
CHEMBL2071211 IC50 = 31.0 nM 7.51
CHEMBL2071271 IC50 = 32.0 nM 7.50
CHEMBL2071214 IC50 = 32.0 nM 7.50
CHEMBL2071201 IC50 = 42.0 nM 7.38
CHEMBL2071205 IC50 = 43.0 nM 7.37
CHEMBL2071215 IC50 = 44.0 nM 7.36
CHEMBL2071206 IC50 = 45.0 nM 7.35
CHEMBL2071207 IC50 = 51.0 nM 7.29
CHEMBL1614709 IC50 = 54.0 nM 7.27
CHEMBL2071204 IC50 = 61.0 nM 7.21
CHEMBL2071203 IC50 = 66.0 nM 7.18
CHEMBL2071208 IC50 = 99.0 nM 7.00
CHEMBL2071212 IC50 = 118.0 nM 6.93
CHEMBL2071213 IC50 = 135.0 nM 6.87
CHEMBL2071197 IC50 = 145.0 nM 6.84
CHEMBL2071198 IC50 = 197.0 nM 6.71
CHEMBL2071196 IC50 = 252.0 nM 6.60
CHEMBL2071195 IC50 = 294.0 nM 6.53