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Assay Detail

CHEMBL3395587

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

Functional
Neuroprotective activity in E14.5 rat embryo DRG neurons
11
Total Activities
10
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type DRG neuron
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 10 6.66 7.34
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3393337 1 7.34
CHEMBL3393334 1 7.00
CHEMBL3393333 2 6.97
CHEMBL3393340 1 6.81
CHEMBL3393327 1 6.77
CHEMBL3393328 1 6.75
CHEMBL3393332 1 6.40
CHEMBL3393336 1 6.35
CHEMBL3393335 1 6.16
CHEMBL3393339 1 6.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3393337 IC50 = 46.0 nM 7.34
CHEMBL3393334 IC50 = 99.0 nM 7.00
CHEMBL3393333 IC50 = 107.0 nM 6.97
CHEMBL3393340 IC50 = 155.0 nM 6.81
CHEMBL3393327 IC50 = 171.0 nM 6.77
CHEMBL3393328 IC50 = 180.0 nM 6.75
CHEMBL3393332 IC50 = 401.0 nM 6.40
CHEMBL3393336 IC50 = 448.0 nM 6.35
CHEMBL3393335 IC50 = 697.0 nM 6.16
CHEMBL3393339 IC50 = 916.0 nM 6.04
CHEMBL3393333 Activity - -