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Assay Detail

CHEMBL4119868

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

Binding
Inhibition of doxycycline inducible human DLK transfected in HEK293 cells assessed as JNK phosphorylation after 5.5 hrs by Hoechst-33342 staining-based assay
26
Total Activities
26
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

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
IC50 26 6.35 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4128619 1 7.00
CHEMBL3715238 1 6.84
CHEMBL3718522 1 6.75
CHEMBL3719135 1 6.71
CHEMBL4128477 1 6.70
CHEMBL3714822 1 6.68
CHEMBL4128889 1 6.68
CHEMBL3717481 1 6.60
CHEMBL3716231 1 6.58
CHEMBL4125824 1 6.56
CHEMBL4125721 1 6.52
CHEMBL3718912 1 6.52
CHEMBL3718265 1 6.52
CHEMBL3714987 1 6.48
CHEMBL4129958 1 6.39
CHEMBL3718344 1 6.31
CHEMBL3716456 1 6.24
CHEMBL3717769 1 6.21
CHEMBL4127238 1 6.08
CHEMBL3715469 1 6.06
CHEMBL3717627 1 5.92
CHEMBL4127922 1 5.89
CHEMBL3718750 1 5.77
CHEMBL4126530 1 5.75
CHEMBL3719126 1 5.72
CHEMBL3719209 1 5.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4128619 IC50 = 99.0 nM 7.00
CHEMBL3715238 IC50 = 144.0 nM 6.84
CHEMBL3718522 IC50 = 180.0 nM 6.75
CHEMBL3719135 IC50 = 195.0 nM 6.71
CHEMBL4128477 IC50 = 202.0 nM 6.70
CHEMBL3714822 IC50 = 210.0 nM 6.68
CHEMBL4128889 IC50 = 208.0 nM 6.68
CHEMBL3717481 IC50 = 250.0 nM 6.60
CHEMBL3716231 IC50 = 265.0 nM 6.58
CHEMBL4125824 IC50 = 274.0 nM 6.56
CHEMBL4125721 IC50 = 304.0 nM 6.52
CHEMBL3718912 IC50 = 303.0 nM 6.52
CHEMBL3718265 IC50 = 302.0 nM 6.52
CHEMBL3714987 IC50 = 328.0 nM 6.48
CHEMBL4129958 IC50 = 406.0 nM 6.39
CHEMBL3718344 IC50 = 485.0 nM 6.31
CHEMBL3716456 IC50 = 574.0 nM 6.24
CHEMBL3717769 IC50 = 611.0 nM 6.21
CHEMBL4127238 IC50 = 829.0 nM 6.08
CHEMBL3715469 IC50 = 873.0 nM 6.06
CHEMBL3717627 IC50 = 1200.0 nM 5.92
CHEMBL4127922 IC50 = 1300.0 nM 5.89
CHEMBL3718750 IC50 = 1700.0 nM 5.77
CHEMBL4126530 IC50 = 1800.0 nM 5.75
CHEMBL3719126 IC50 = 1900.0 nM 5.72
CHEMBL3719209 IC50 = 2800.0 nM 5.55