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Assay Detail

CHEMBL4430369

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

Binding
Inhibition of AURKB (unknown origin)
9
Total Activities
9
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

Design and optimization of (3-aryl-1H-indazol-6-yl)spiro[cyclopropane-1,3'-indolin]-2'-ones as potent PLK4 inhibitors with oral antitumor efficacy.
Li SW, Liu Y, Sampson PB, Patel NK, Forrest BT, Edwards L, Laufer R, Feher M, Ban F, Awrey DE, Hodgson R, Beletskaya I, Mao G, Mason JM, Wei X, Luo X, Kiarash R, Green E, Mak TW, Pan G, Pauls HW.
Bioorg Med Chem Lett (2016) 26 : 4625 -4630
PubMed 27592744 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.70 8.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4448596 1 8.16
CHEMBL4553351 1 8.16
CHEMBL4470693 1 8.15
CHEMBL4440812 1 8.07
CHEMBL4516793 1 8.00
CHEMBL4440053 1 7.89
CHEMBL4434704 1 7.46
CHEMBL4467348 1 5.68
CHEMBL4437913 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4448596 IC50 = 6.9 nM 8.16
CHEMBL4553351 IC50 = 6.9 nM 8.16
CHEMBL4470693 IC50 = 7.0 nM 8.15
CHEMBL4440812 IC50 = 8.5 nM 8.07
CHEMBL4516793 IC50 = 10.0 nM 8.00
CHEMBL4440053 IC50 = 13.0 nM 7.89
CHEMBL4434704 IC50 = 35.0 nM 7.46
CHEMBL4467348 IC50 = 2100.0 nM 5.68
CHEMBL4437913 IC50 - -