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Assay Detail

CHEMBL2024777

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

Binding
Inhibition of Aurora B using 1 mM ATP by HTRF assay
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.
Curtin ML, Frey RR, Heyman HR, Soni NB, Marcotte PA, Pease LJ, Glaser KB, Magoc TJ, Tapang P, Albert DH, Osterling DJ, Olson AM, Bouska JJ, Guan Z, Preusser LC, Polakowski JS, Stewart KD, Tse C, Davidsen SK, Michaelides MR.
Bioorg Med Chem Lett (2012) 22 : 3208 -3212
PubMed 22465635 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 7.52 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2022856 1 9.00
CHEMBL2022857 1 8.70
CHEMBL2022855 1 8.30
CHEMBL2023226 1 8.22
CHEMBL1980297 ILORASERTIB 2.0 1 8.15
CHEMBL2022854 1 8.10
CHEMBL2023225 1 8.10
CHEMBL1969102 1 8.10
CHEMBL1970317 1 8.05
CHEMBL1979883 1 7.96
CHEMBL2022853 1 7.96
CHEMBL2023221 1 7.89
CHEMBL1967116 1 7.80
CHEMBL2023232 1 7.77
CHEMBL2023227 1 7.75
CHEMBL2022850 1 7.64
CHEMBL1993941 1 7.51
CHEMBL2023229 1 7.32
CHEMBL1982466 1 7.30
CHEMBL2023230 1 7.28
CHEMBL2023224 1 7.18
CHEMBL2021941 1 7.17
CHEMBL2023228 1 7.16
CHEMBL2023220 1 7.10
CHEMBL2023222 1 7.00
CHEMBL2023231 1 6.94
CHEMBL2023223 1 6.75
CHEMBL2022851 1 6.75
CHEMBL394619 1 6.31
CHEMBL2022852 1 6.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2022856 IC50 = 1.0 nM 9.00
CHEMBL2022857 IC50 = 2.0 nM 8.70
CHEMBL2022855 IC50 = 5.0 nM 8.30
CHEMBL2023226 IC50 = 6.0 nM 8.22
CHEMBL1980297 ILORASERTIB IC50 = 7.0 nM 8.15
CHEMBL2022854 IC50 = 8.0 nM 8.10
CHEMBL2023225 IC50 = 8.0 nM 8.10
CHEMBL1969102 IC50 = 8.0 nM 8.10
CHEMBL1970317 IC50 = 9.0 nM 8.05
CHEMBL1979883 IC50 = 11.0 nM 7.96
CHEMBL2022853 IC50 = 11.0 nM 7.96
CHEMBL2023221 IC50 = 13.0 nM 7.89
CHEMBL1967116 IC50 = 16.0 nM 7.80
CHEMBL2023232 IC50 = 17.0 nM 7.77
CHEMBL2023227 IC50 = 18.0 nM 7.75
CHEMBL2022850 IC50 = 23.0 nM 7.64
CHEMBL1993941 IC50 = 31.0 nM 7.51
CHEMBL2023229 IC50 = 48.0 nM 7.32
CHEMBL1982466 IC50 = 50.0 nM 7.30
CHEMBL2023230 IC50 = 52.0 nM 7.28
CHEMBL2023224 IC50 = 66.0 nM 7.18
CHEMBL2021941 IC50 = 68.0 nM 7.17
CHEMBL2023228 IC50 = 70.0 nM 7.16
CHEMBL2023220 IC50 = 80.0 nM 7.10
CHEMBL2023222 IC50 = 100.0 nM 7.00
CHEMBL2023231 IC50 = 114.0 nM 6.94
CHEMBL2023223 IC50 = 179.0 nM 6.75
CHEMBL2022851 IC50 = 177.0 nM 6.75
CHEMBL394619 IC50 = 487.0 nM 6.31
CHEMBL2022852 IC50 = 529.0 nM 6.28
CHEMBL231511 IC50 = 3280.0 nM 5.48