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Assay Detail

CHEMBL1009880

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Binding
Inhibition of Aurora A
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Aurora kinase A (CHEMBL4722)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity.
Howard S, Berdini V, Boulstridge JA, Carr MG, Cross DM, Curry J, Devine LA, Early TR, Fazal L, Gill AL, Heathcote M, Maman S, Matthews JE, McMenamin RL, Navarro EF, O'Brien MA, O'Reilly M, Rees DC, Reule M, Tisi D, Williams G, Vinković M, Wyatt PG.
J Med Chem (2009) 52 : 379 -388
PubMed 19143567 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.98 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL572878 TOZASERTIB 2.0 1 8.85
CHEMBL458421 1 8.82
CHEMBL516003 1 8.55
CHEMBL496569 1 8.46
CHEMBL496754 1 8.24
CHEMBL522891 1 8.23
CHEMBL522563 1 8.00
CHEMBL458420 1 7.92
CHEMBL523923 1 7.89
CHEMBL522214 1 7.58
CHEMBL504155 1 7.16
CHEMBL495758 1 6.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL572878 TOZASERTIB IC50 = 1.4 nM 8.85
CHEMBL458421 IC50 = 1.5 nM 8.82
CHEMBL516003 IC50 = 2.8 nM 8.55
CHEMBL496569 IC50 = 3.5 nM 8.46
CHEMBL496754 IC50 = 5.7 nM 8.24
CHEMBL522891 IC50 = 5.9 nM 8.23
CHEMBL522563 IC50 = 10.0 nM 8.00
CHEMBL458420 IC50 = 12.0 nM 7.92
CHEMBL523923 IC50 = 13.0 nM 7.89
CHEMBL522214 IC50 = 26.0 nM 7.58
CHEMBL504155 IC50 = 70.0 nM 7.16
CHEMBL495758 IC50 = 910.0 nM 6.04