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Assay Detail

CHEMBL5161146

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

Binding
Displacement of 3H-LP-927443 from AAK1 in C57BL6 mouse brain homogenate assessed as inhibition constant incubated for 1 hr by liquid scintillation counter analysis
ChEMBL ↗
47
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Tissue Brain
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

AP2-associated protein kinase 1 (CHEMBL5169154) ↗
Type SINGLE PROTEIN
Organism Mus musculus

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
Ki 47 9.55 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5185616 — — 1 10.40
CHEMBL5179172 — — 1 10.40
CHEMBL5202896 — — 1 10.40
CHEMBL5202370 — — 1 10.40
CHEMBL5183016 — — 1 10.40
CHEMBL4534648 — — 1 10.40
CHEMBL5178261 — — 1 10.30
CHEMBL5204340 — — 1 10.30
CHEMBL4084103 — — 1 10.30
CHEMBL5199698 — — 1 10.30
CHEMBL5186783 — — 1 10.22
CHEMBL5204210 — — 1 10.15
CHEMBL5202142 — — 1 10.15
CHEMBL5174967 — — 1 10.15
CHEMBL5177574 — — 1 10.15
CHEMBL5198877 — — 1 10.10
CHEMBL4062388 — — 1 10.10
CHEMBL5179243 — — 1 10.10
CHEMBL5189920 — — 1 10.05
CHEMBL5187778 — — 1 10.05
CHEMBL5188433 — — 1 9.96
CHEMBL5177255 — — 1 9.96
CHEMBL5185000 — — 1 9.82
CHEMBL5205578 — — 1 9.77
CHEMBL4092824 — — 1 9.74
CHEMBL5177318 — — 1 9.70
CHEMBL5184381 — — 1 9.68
CHEMBL5189987 — — 1 9.62
CHEMBL5180992 — — 1 9.59
CHEMBL5170576 — — 1 9.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5185616 — Ki = 0.04 nM 10.40
CHEMBL4534648 — Ki = 0.04 nM 10.40
CHEMBL5183016 — Ki = 0.04 nM 10.40
CHEMBL5202370 — Ki = 0.04 nM 10.40
CHEMBL5179172 — Ki = 0.04 nM 10.40
CHEMBL5202896 — Ki = 0.04 nM 10.40
CHEMBL5199698 — Ki = 0.05 nM 10.30
CHEMBL4084103 — Ki = 0.05 nM 10.30
CHEMBL5178261 — Ki = 0.05 nM 10.30
CHEMBL5204340 — Ki = 0.05 nM 10.30
CHEMBL5186783 — Ki = 0.06 nM 10.22
CHEMBL5177574 — Ki = 0.07 nM 10.15
CHEMBL5174967 — Ki = 0.07 nM 10.15
CHEMBL5202142 — Ki = 0.07 nM 10.15
CHEMBL5204210 — Ki = 0.07 nM 10.15
CHEMBL5198877 — Ki = 0.08 nM 10.10
CHEMBL5179243 — Ki = 0.08 nM 10.10
CHEMBL4062388 — Ki = 0.08 nM 10.10
CHEMBL5189920 — Ki = 0.09 nM 10.05
CHEMBL5187778 — Ki = 0.09 nM 10.05
CHEMBL5188433 — Ki = 0.11 nM 9.96
CHEMBL5177255 — Ki = 0.11 nM 9.96
CHEMBL5185000 — Ki = 0.15 nM 9.82
CHEMBL5205578 — Ki = 0.17 nM 9.77
CHEMBL4092824 — Ki = 0.18 nM 9.74
CHEMBL5177318 — Ki = 0.2 nM 9.70
CHEMBL5184381 — Ki = 0.21 nM 9.68
CHEMBL5189987 — Ki = 0.24 nM 9.62
CHEMBL5180992 — Ki = 0.26 nM 9.59
CHEMBL5170576 — Ki = 0.29 nM 9.54
CHEMBL5194195 — Ki = 0.3 nM 9.52
CHEMBL5198578 — Ki = 0.52 nM 9.28
CHEMBL5189450 — Ki = 0.6 nM 9.22
CHEMBL5195859 — Ki = 0.63 nM 9.20
CHEMBL5204513 — Ki = 0.7 nM 9.15
CHEMBL5193012 — Ki = 0.9 nM 9.05
CHEMBL4073745 — Ki = 0.96 nM 9.02
CHEMBL5195653 — Ki = 1.4 nM 8.85
CHEMBL5172656 — Ki = 1.5 nM 8.82
CHEMBL5191442 — Ki = 2.5 nM 8.60
CHEMBL5171363 — Ki = 2.5 nM 8.60
CHEMBL5180606 — Ki = 4.7 nM 8.33
CHEMBL5198829 — Ki = 4.9 nM 8.31
CHEMBL5193138 — Ki = 13.0 nM 7.89
CHEMBL5169857 — Ki = 18.0 nM 7.75
CHEMBL5194947 — Ki = 27.0 nM 7.57
CHEMBL5180776 — Ki = 41.0 nM 7.39