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Assay Detail

CHEMBL3395586

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

Binding
Inhibition of human DLK transfected in HEK293 cells assessed as JNK phosphorylation after 5.5 hrs by Hoechst-33342 staining-based assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mitogen-activated protein kinase kinase kinase 12 (CHEMBL1908389)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of dual leucine zipper kinase (DLK, MAP3K12) inhibitors with activity in neurodegeneration models.
Patel S, Cohen F, Dean BJ, De La Torre K, Deshmukh G, Estrada AA, Ghosh AS, Gibbons P, Gustafson A, Huestis MP, Le Pichon CE, Lin H, Liu W, Liu X, Liu Y, Ly CQ, Lyssikatos JP, Ma C, Scearce-Levie K, Shin YG, Solanoy H, Stark KL, Wang J, Wang B, Zhao X, Lewcock JW, Siu M.
J Med Chem (2015) 58 : 401 -418
PubMed 25341110 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 6.64 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3393333 1 7.52
CHEMBL3393334 1 7.24
CHEMBL3393340 1 7.21
CHEMBL3393337 1 7.19
CHEMBL3393327 1 7.16
CHEMBL3393329 1 7.16
CHEMBL3393330 1 7.10
CHEMBL3393320 1 6.96
CHEMBL3393332 1 6.90
CHEMBL3393336 1 6.85
CHEMBL3393331 1 6.71
CHEMBL3393339 1 6.67
CHEMBL3393312 1 6.64
CHEMBL3393335 1 6.63
CHEMBL3393324 1 6.52
CHEMBL3393322 1 6.39
CHEMBL3393321 1 6.39
CHEMBL3393323 1 6.36
CHEMBL3393315 1 6.31
CHEMBL3393308 1 6.19
CHEMBL3393310 1 6.12
CHEMBL3393318 1 6.00
CHEMBL3393317 1 6.00
CHEMBL3393314 1 5.89
CHEMBL3393338 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3393333 IC50 = 30.0 nM 7.52
CHEMBL3393334 IC50 = 57.0 nM 7.24
CHEMBL3393340 IC50 = 62.0 nM 7.21
CHEMBL3393337 IC50 = 64.0 nM 7.19
CHEMBL3393327 IC50 = 69.0 nM 7.16
CHEMBL3393329 IC50 = 70.0 nM 7.16
CHEMBL3393330 IC50 = 79.0 nM 7.10
CHEMBL3393320 IC50 = 109.0 nM 6.96
CHEMBL3393332 IC50 = 125.0 nM 6.90
CHEMBL3393336 IC50 = 141.0 nM 6.85
CHEMBL3393331 IC50 = 193.0 nM 6.71
CHEMBL3393339 IC50 = 213.0 nM 6.67
CHEMBL3393312 IC50 = 229.0 nM 6.64
CHEMBL3393335 IC50 = 233.0 nM 6.63
CHEMBL3393324 IC50 = 300.0 nM 6.52
CHEMBL3393322 IC50 = 410.0 nM 6.39
CHEMBL3393321 IC50 = 408.0 nM 6.39
CHEMBL3393323 IC50 = 440.0 nM 6.36
CHEMBL3393315 IC50 = 486.0 nM 6.31
CHEMBL3393308 IC50 = 641.0 nM 6.19
CHEMBL3393310 IC50 = 767.0 nM 6.12
CHEMBL3393318 IC50 = 1000.0 nM 6.00
CHEMBL3393317 IC50 = 1000.0 nM 6.00
CHEMBL3393314 IC50 = 1300.0 nM 5.89
CHEMBL3393338 IC50 = 1600.0 nM 5.80