Assay Detail

CHEMBL5161264

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Binding

Inhibition of CLK1 (unknown origin)

ChEMBL ↗

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Target

Dual specificity protein kinase CLK1 (CHEMBL4224) ↗

Open DB target context

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Dual specificity protein kinase CLK1 (CHEMBL4224) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Dual specificity protein kinase CLK1

CHEMBL4224

Anchored from Assay target.

Protein identity Dual specificity protein kinase CLK1

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

Dual specificity protein kinase CLK1 (CHEMBL4224) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery and Optimization of Biaryl Alkyl Ethers as a Novel Class of Highly Selective, CNS-Penetrable, and Orally Active Adaptor Protein-2-Associated Kinase 1 (AAK1) Inhibitors for the Potential Treatment of Neuropathic Pain.

Luo G, Chen L, Kostich WA, Hamman B, Allen J, Easton A, Bourin C, Gulianello M, Lippy J, Nara S, Pattipati SN, Dandapani K, Dokania M, Vattikundala P, Sharma V, Elavazhagan S, Verma MK, Lal Das M, Wagh S, Balakrishnan A, Johnson BM, Santone KS, Thalody G, Denton R, Saminathan H, Holenarsipur VK, Kumar A, Rao A, Putlur SP, Sarvasiddhi SK, Shankar G, Louis JV, Ramarao M, Conway CM, Li YW, Pieschl R, Tian Y, Hong Y, Bristow L, Albright CF, Bronson JJ, Macor JE, Dzierba CD.
J Med Chem (2022) 65 : 4534 -4564
PubMed 35261239 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	5.77	5.77

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL5185000	—	—	1	5.77

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL5185000	—	IC50	=	1700.0	nM	5.77