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Assay Detail

CHEMBL5507790

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Binding
Inhibition of AAK1 (unknown origin)
9
Total Activities
9
Compounds Tested
2
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

Design, synthesis and biological evaluation of novel 1,2,4a,5-tetrahydro-4H-benzo[b][1,4]oxazino[4,3-d][1,4]oxazine-based AAK1 inhibitors with anti-viral property against SARS-CoV-2.
Mao ND, Xu Y, Che H, Yao X, Gao Y, Wang C, Deng H, Hui Z, Zhang H, Ye XY.
Eur J Med Chem (2024) 268 : 116232 -116232
PubMed 38377825 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 8.14 8.92
Ki 1 8.04 8.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5089410 PILAVAPADIN 2.0 1 8.92
CHEMBL4439128 1 8.40
CHEMBL4855590 1 8.32
CHEMBL5202351 1 8.24
CHEMBL4452939 1 8.04
CHEMBL5564665 1 7.95
CHEMBL4872886 1 7.92
CHEMBL516312 1 7.24
CHEMBL4127773 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5089410 PILAVAPADIN IC50 = 1.2 nM 8.92
CHEMBL4439128 IC50 = 4.02 nM 8.40
CHEMBL4855590 IC50 = 4.8 nM 8.32
CHEMBL5202351 IC50 = 5.8 nM 8.24
CHEMBL4452939 Ki = 9.1 nM 8.04
CHEMBL5564665 IC50 = 11.19 nM 7.95
CHEMBL4872886 IC50 = 12.0 nM 7.92
CHEMBL516312 IC50 = 57.81 nM 7.24
CHEMBL4127773 IC50 < 10.0 nM -