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Assay Detail

CHEMBL996141

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

Functional
Neuroprotective activity against human SH-SY5Y cells assessed as inhibition of MPP+-induced cell death
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type SH-SY5Y
Confidence 1 — Organism
Curated By Autocuration

Target

SH-SY5Y (CHEMBL614910)
Type CELL-LINE
Organism Homo sapiens

Publication

Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models.
Hudkins RL, Diebold JL, Tao M, Josef KA, Park CH, Angeles TS, Aimone LD, Husten J, Ator MA, Meyer SL, Holskin BP, Durkin JT, Fedorov AA, Fedorov EV, Almo SC, Mathiasen JR, Bozyczko-Coyne D, Saporito MS, Scott RW, Mallamo JP.
J Med Chem (2008) 51 : 5680 -5689
PubMed 18714982 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.72 8.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL290352 CEP-1347 3.0 1 8.28
CHEMBL460989 1 7.50
CHEMBL460990 1 7.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL290352 CEP-1347 IC50 = 5.3 nM 8.28
CHEMBL460989 IC50 = 32.0 nM 7.50
CHEMBL460990 IC50 = 43.0 nM 7.37