Assay Detail

CHEMBL5159170

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Binding

Inhibition of AAK1 (unknown origin)

ChEMBL ↗

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Target

AP2-associated protein kinase 1 (CHEMBL3830) ↗

Open DB target context

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AP2-associated protein kinase 1 (CHEMBL3830) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target AP2-associated protein kinase 1

CHEMBL3830

Anchored from Assay target.

Protein identity AP2-associated protein kinase 1

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

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

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	1	8.40	8.40

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4439128	—	—	1	8.40

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4439128	—	IC50	=	4.0	nM	8.40