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Assay Detail

CHEMBL5239393

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

Binding
Inhibition of LZK (unknown origin)
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Mitogen-activated protein kinase kinase kinase 13 (CHEMBL1163124)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Potent and Selective Dual Leucine Zipper Kinase/Leucine Zipper-Bearing Kinase Inhibitors with Neuroprotective Properties in In Vitro and In Vivo Models of Amyotrophic Lateral Sclerosis.
Craig RA, Fox BM, Hu C, Lexa KW, Osipov M, Thottumkara AP, Larhammar M, Miyamoto T, Rana A, Kane LA, Yulyaningsih E, Solanoy H, Nguyen H, Chau R, Earr T, Kajiwara Y, Fleck D, Lucas A, Haddick PCG, Takahashi RH, Tong V, Wang J, Canet MJ, Poda SB, Scearce-Levie K, Srivastava A, Sweeney ZK, Xu M, Zhang R, He J, Lei Y, Zhuo Z, de Vicente J.
J Med Chem (2022) 65 : 16290 -16312
PubMed 36469401 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.12 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3393333 1 8.52
CHEMBL5287658 1 8.00
CHEMBL3732012 GDC-0134 1.0 1 7.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3393333 IC50 = 3.0 nM 8.52
CHEMBL5287658 IC50 = 10.0 nM 8.00
CHEMBL3732012 GDC-0134 IC50 = 14.0 nM 7.85