Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4022632

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

Binding
Inhibition of GST-Xa-tagged human AAK1 expressed in bacterial system using fluoresceinated peptide (5 -FAM)-Aha-KEEQSQITSQVTGQIGWR-NH2 and ATP incubated for 3 hrs
8
Total Activities
8
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

Inhibitors of Adaptor-Associated Kinase 1 (AAK1) May Treat Neuropathic Pain, Schizophrenia, Parkinson's Disease, and Other Disorders.
Abdel-Magid AF.
ACS Med Chem Lett (2017) 8 : 595 -597
PubMed 28626516 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 8.55 10.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4085072 1 10.15
CHEMBL4065155 1 9.64
CHEMBL4084103 1 9.49
CHEMBL4062388 1 9.38
CHEMBL4092824 1 9.29
CHEMBL4073745 1 8.52
CHEMBL4066208 1 6.05
CHEMBL4103020 1 5.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4085072 IC50 = 0.07 nM 10.15
CHEMBL4065155 IC50 = 0.23 nM 9.64
CHEMBL4084103 IC50 = 0.32 nM 9.49
CHEMBL4062388 IC50 = 0.42 nM 9.38
CHEMBL4092824 IC50 = 0.51 nM 9.29
CHEMBL4073745 IC50 = 3.0 nM 8.52
CHEMBL4066208 IC50 = 886.0 nM 6.05
CHEMBL4103020 IC50 = 1400.0 nM 5.85