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Assay Detail

CHEMBL5161147

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Binding
Inhibition of full length human AAK1 expressed in HEK293F cells assessed as suppression of AP2 phosphorylation measured after 3 hrs by Western blot analysis based cellular assay
ChEMBL ↗
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293F
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

AP2-associated protein kinase 1 (CHEMBL3830) ↗
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 39 8.80 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5186783 — — 1 9.70
CHEMBL5202896 — — 1 9.70
CHEMBL5178245 — — 1 9.40
CHEMBL5183016 — — 1 9.40
CHEMBL5179172 — — 1 9.35
CHEMBL4534648 — — 1 9.30
CHEMBL5199698 — — 1 9.30
CHEMBL5204340 — — 1 9.30
CHEMBL5202370 — — 1 9.22
CHEMBL5189920 — — 1 9.22
CHEMBL5185616 — — 1 9.12
CHEMBL5174967 — — 1 9.10
CHEMBL5198877 — — 1 9.10
CHEMBL4092824 — — 1 9.05
CHEMBL4084103 — — 1 9.00
CHEMBL4062388 — — 1 8.96
CHEMBL5205578 — — 1 8.92
CHEMBL5177318 — — 1 8.92
CHEMBL5187778 — — 1 8.85
CHEMBL5178261 — — 1 8.82
CHEMBL5198578 — — 1 8.80
CHEMBL5177574 — — 1 8.80
CHEMBL5204513 — — 1 8.72
CHEMBL5089410 PILAVAPADIN 2.0 1 8.70
CHEMBL5170576 — — 1 8.62
CHEMBL5194667 — — 1 8.57
CHEMBL5184381 — — 1 8.47
CHEMBL5189987 — — 1 8.43
CHEMBL4073745 — — 1 8.42
CHEMBL5195859 — — 1 8.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5186783 — IC50 = 0.2 nM 9.70
CHEMBL5202896 — IC50 = 0.2 nM 9.70
CHEMBL5183016 — IC50 = 0.4 nM 9.40
CHEMBL5178245 — IC50 = 0.4 nM 9.40
CHEMBL5179172 — IC50 = 0.45 nM 9.35
CHEMBL4534648 — IC50 = 0.5 nM 9.30
CHEMBL5199698 — IC50 = 0.5 nM 9.30
CHEMBL5204340 — IC50 = 0.5 nM 9.30
CHEMBL5202370 — IC50 = 0.6 nM 9.22
CHEMBL5189920 — IC50 = 0.6 nM 9.22
CHEMBL5185616 — IC50 = 0.75 nM 9.12
CHEMBL5174967 — IC50 = 0.8 nM 9.10
CHEMBL5198877 — IC50 = 0.8 nM 9.10
CHEMBL4092824 — IC50 = 0.9 nM 9.05
CHEMBL4084103 — IC50 = 1.0 nM 9.00
CHEMBL4062388 — IC50 = 1.1 nM 8.96
CHEMBL5205578 — IC50 = 1.2 nM 8.92
CHEMBL5177318 — IC50 = 1.2 nM 8.92
CHEMBL5187778 — IC50 = 1.4 nM 8.85
CHEMBL5178261 — IC50 = 1.5 nM 8.82
CHEMBL5177574 — IC50 = 1.6 nM 8.80
CHEMBL5198578 — IC50 = 1.6 nM 8.80
CHEMBL5204513 — IC50 = 1.9 nM 8.72
CHEMBL5089410 PILAVAPADIN IC50 = 2.0 nM 8.70
CHEMBL5170576 — IC50 = 2.4 nM 8.62
CHEMBL5194667 — IC50 = 2.7 nM 8.57
CHEMBL5184381 — IC50 = 3.4 nM 8.47
CHEMBL5189987 — IC50 = 3.7 nM 8.43
CHEMBL4073745 — IC50 = 3.8 nM 8.42
CHEMBL5195859 — IC50 = 3.9 nM 8.41
CHEMBL5179243 — IC50 = 4.1 nM 8.39
CHEMBL5188433 — IC50 = 4.2 nM 8.38
CHEMBL5172656 — IC50 = 4.8 nM 8.32
CHEMBL5189450 — IC50 = 6.7 nM 8.17
CHEMBL5191442 — IC50 = 6.8 nM 8.17
CHEMBL5193012 — IC50 = 8.1 nM 8.09
CHEMBL5180992 — IC50 = 9.7 nM 8.01
CHEMBL5195653 — IC50 = 12.0 nM 7.92
CHEMBL5194195 — IC50 = 12.0 nM 7.92