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Assay Detail

CHEMBL5159134

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

Binding
Inhibition of full length human AAK1 expressed in HEK293F incubated for 3 hrs by Western blot analysis
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293F
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

AP2-associated protein kinase 1 (CHEMBL3830)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Bicyclic Heterocyclic Replacement of an Aryl Amide Leading to Potent and Kinase-Selective Adaptor Protein 2-Associated Kinase 1 Inhibitors.
Hartz RA, Ahuja VT, Nara SJ, Kumar CMV, Manepalli RKVLP, Sarvasiddhi SK, Honkhambe S, Patankar V, Dasgupta B, Rajamani R, Muckelbauer JK, Camac DM, Ghosh K, Pokross M, Kiefer SE, Brown JM, Hunihan L, Gulianello M, Lewis M, Lippy JS, Surti N, Hamman BD, Allen J, Kostich WA, Bronson JJ, Macor JE, Dzierba CD.
J Med Chem (2022) 65 : 4121 -4155
PubMed 35171586 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.38 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5202351 1 7.72
CHEMBL5194899 1 7.50
CHEMBL5201888 1 7.47
CHEMBL5208293 1 7.31
CHEMBL4872886 1 7.29
CHEMBL5182431 1 6.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5202351 IC50 = 19.0 nM 7.72
CHEMBL5194899 IC50 = 32.0 nM 7.50
CHEMBL5201888 IC50 = 34.0 nM 7.47
CHEMBL5208293 IC50 = 49.0 nM 7.31
CHEMBL4872886 IC50 = 51.0 nM 7.29
CHEMBL5182431 IC50 = 108.0 nM 6.97