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Assay Detail

CHEMBL4831260

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

Binding
Inhibition of recombinant full length GST-tagged human Aurora B (1 to 344 residues) co-expressed with N-terminal His-tagged human recombinant INCENP (803 to 918 residues) in baculovirus infected Sf21 cells incubated for 90 mins by mobility shift assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf21
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Aurora kinase B/Inner centromere protein (CHEMBL3430907)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Identification of Clinical Candidate M2698, a Dual p70S6K and Akt Inhibitor, for Treatment of PAM Pathway-Altered Cancers.
DeSelm L, Huck B, Lan R, Neagu C, Potnick J, Xiao Y, Chen X, Jones R, Richardson TE, Heasley BH, Haxell T, Moore J, Tian H, Georgi K, Rohdich F, Sutton A, Johnson T, Mochalkin I, Jackson J, Lin J, Crowley L, Machl A, Clark A, Wilker E, Sherer B, Goutopoulos A.
J Med Chem (2021) 64 : 14603 -14619
PubMed 34596404 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.32 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3685329 1 8.40
CHEMBL4854144 1 8.22
CHEMBL3675415 1 8.05
CHEMBL4875416 1 7.39
CHEMBL4851020 1 7.35
CHEMBL4857965 1 7.35
CHEMBL4855657 1 7.33
CHEMBL4869229 1 7.29
CHEMBL4860970 1 7.25
CHEMBL4856439 1 7.12
CHEMBL4871106 RUPITASERTIB 2.0 1 6.77
CHEMBL4876446 1 6.75
CHEMBL4846712 1 6.63
CHEMBL4871853 1 6.58
CHEMBL4853030 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3685329 IC50 = 4.0 nM 8.40
CHEMBL4854144 IC50 = 6.0 nM 8.22
CHEMBL3675415 IC50 = 9.0 nM 8.05
CHEMBL4875416 IC50 = 41.0 nM 7.39
CHEMBL4851020 IC50 = 45.0 nM 7.35
CHEMBL4857965 IC50 = 45.0 nM 7.35
CHEMBL4855657 IC50 = 47.0 nM 7.33
CHEMBL4869229 IC50 = 51.0 nM 7.29
CHEMBL4860970 IC50 = 56.0 nM 7.25
CHEMBL4856439 IC50 = 75.0 nM 7.12
CHEMBL4871106 RUPITASERTIB IC50 = 170.0 nM 6.77
CHEMBL4876446 IC50 = 180.0 nM 6.75
CHEMBL4846712 IC50 = 233.0 nM 6.63
CHEMBL4871853 IC50 = 260.0 nM 6.58
CHEMBL4853030 IC50 > 1000.0 nM -