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Assay Detail

CHEMBL4829129

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

Binding
Inhibition of AAK1 (unknown origin)
4
Total Activities
4
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

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

Publication

Discovery, Structure-Activity Relationships, and In Vivo Evaluation of Novel Aryl Amides as Brain Penetrant Adaptor Protein 2-Associated Kinase 1 (AAK1) Inhibitors for the Treatment of Neuropathic Pain.
Hartz RA, Ahuja VT, Nara SJ, Kumar CMV, Brown JM, Bristow LJ, Rajamani R, Muckelbauer JK, Camac D, Kiefer SE, Hunihan L, Gulianello M, Lewis M, Easton A, Lippy JS, Surti N, Pattipati SN, Dokania M, Elavazhagan S, Dandapani K, Hamman BD, Allen J, Kostich W, Bronson JJ, Macor JE, Dzierba CD.
J Med Chem (2021) 64 : 11090 -11128
PubMed 34270254 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.59 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4857123 1 9.15
CHEMBL4127773 1 8.48
CHEMBL4439128 1 8.40
CHEMBL4855590 1 8.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4857123 IC50 = 0.7 nM 9.15
CHEMBL4127773 IC50 = 3.3 nM 8.48
CHEMBL4439128 IC50 = 4.0 nM 8.40
CHEMBL4855590 IC50 = 4.8 nM 8.32