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Assay Detail

CHEMBL3395585

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

Binding
Inhibition of DLK (unknown origin)
33
Total Activities
33
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 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
Ki 33 7.69 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3393337 1 9.70
CHEMBL3393334 1 9.15
CHEMBL3393329 1 9.05
CHEMBL3393340 1 9.00
CHEMBL3393327 1 9.00
CHEMBL3393322 1 8.70
CHEMBL3393314 1 8.40
CHEMBL3393332 1 8.30
CHEMBL3393330 1 8.30
CHEMBL3393321 1 8.15
CHEMBL3393320 1 8.15
CHEMBL3393336 1 8.10
CHEMBL3393335 1 8.10
CHEMBL3393331 1 7.85
CHEMBL3393339 1 7.75
CHEMBL3393315 1 7.75
CHEMBL3393312 1 7.62
CHEMBL3393328 1 7.60
CHEMBL3393324 1 7.48
CHEMBL3393308 1 7.46
CHEMBL3393323 1 7.39
CHEMBL3393318 1 7.24
CHEMBL3393310 1 7.07
CHEMBL3393317 1 7.05
CHEMBL3393338 1 7.03
CHEMBL3393325 1 6.78
CHEMBL3393313 1 6.71
CHEMBL3393309 1 6.40
CHEMBL3393326 1 6.37
CHEMBL3393311 1 6.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3393337 Ki = 0.2 nM 9.70
CHEMBL3393334 Ki = 0.7 nM 9.15
CHEMBL3393329 Ki = 0.9 nM 9.05
CHEMBL3393340 Ki = 1.0 nM 9.00
CHEMBL3393327 Ki = 1.0 nM 9.00
CHEMBL3393322 Ki = 2.0 nM 8.70
CHEMBL3393314 Ki = 4.0 nM 8.40
CHEMBL3393332 Ki = 5.0 nM 8.30
CHEMBL3393330 Ki = 5.0 nM 8.30
CHEMBL3393321 Ki = 7.0 nM 8.15
CHEMBL3393320 Ki = 7.0 nM 8.15
CHEMBL3393336 Ki = 8.0 nM 8.10
CHEMBL3393335 Ki = 8.0 nM 8.10
CHEMBL3393331 Ki = 14.0 nM 7.85
CHEMBL3393315 Ki = 18.0 nM 7.75
CHEMBL3393339 Ki = 18.0 nM 7.75
CHEMBL3393312 Ki = 24.0 nM 7.62
CHEMBL3393328 Ki = 25.0 nM 7.60
CHEMBL3393324 Ki = 33.0 nM 7.48
CHEMBL3393308 Ki = 35.0 nM 7.46
CHEMBL3393323 Ki = 41.0 nM 7.39
CHEMBL3393318 Ki = 57.0 nM 7.24
CHEMBL3393310 Ki = 85.0 nM 7.07
CHEMBL3393317 Ki = 90.0 nM 7.05
CHEMBL3393338 Ki = 93.0 nM 7.03
CHEMBL3393325 Ki = 166.0 nM 6.78
CHEMBL3393313 Ki = 195.0 nM 6.71
CHEMBL3393309 Ki = 401.0 nM 6.40
CHEMBL3393326 Ki = 431.0 nM 6.37
CHEMBL3393311 Ki = 691.0 nM 6.16
CHEMBL3393319 Ki = 725.0 nM 6.14
CHEMBL3393316 Ki = 942.0 nM 6.03
CHEMBL3393333 Ki < 0.5 nM -