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Assay Detail

CHEMBL5048422

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

Binding
Inhibition of Aurora A (unknown origin) using 5-FAM- peptide as substrate preincubated for 1 hr followed by substrate addition in presence of ATP by microfluidics assay
1
Total Activities
1
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 A (CHEMBL4722)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of N-Trisubstituted Pyrimidine Derivatives as Type I RET and RET Gatekeeper Mutant Inhibitors with a Novel Kinase Binding Pose.
Zhang L, Moccia M, Briggs DC, Bharate JB, Lakkaniga NR, Knowles P, Yan W, Tran P, Kharbanda A, Wang X, Leung YK, Frett B, Santoro M, McDonald NQ, Carlomagno F, Li HY.
J Med Chem (2022) 65 : 1536 -1551
PubMed 35081714 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.02 7.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5070593 1 7.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5070593 IC50 = 96.38 nM 7.02