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Assay Detail

CHEMBL4119876

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

Binding
Inhibition of DLK in CD-1 mouse DRG neuron assessed as axonal protection pre-incubated for 2 hrs before NGF deprivation for 16 to 20 hrs by Campenot chamber based fluorescence assay
4
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Mitogen-activated protein kinase kinase kinase 12 (CHEMBL4295854)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Selective Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12) with Activity in a Model of Alzheimer's Disease.
Patel S, Meilandt WJ, Erickson RI, Chen J, Deshmukh G, Estrada AA, Fuji RN, Gibbons P, Gustafson A, Harris SF, Imperio J, Liu W, Liu X, Liu Y, Lyssikatos JP, Ma C, Yin J, Lewcock JW, Siu M.
J Med Chem (2017) 60 : 8083 -8102
PubMed 28929759 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 6.29 6.34
Activity 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3715238 2 6.34
CHEMBL3719135 2 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3715238 EC50 = 457.0 nM 6.34
CHEMBL3719135 EC50 = 574.0 nM 6.24
CHEMBL3719135 Activity - -
CHEMBL3715238 Activity - -