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Assay Detail

CHEMBL3608122

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

Binding
Inhibition of human NR1-1a/NR2B expressed in mouse L13-E6 cells assessed as inhibition of glutamate-induced excitotoxicity incubated for 16 hrs by LDH release assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type L13-E6
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Glutamate NMDA receptor; GRIN1/GRIN2B (CHEMBL1907603)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Evaluation of Homobivalent Carbolines as Designed Multiple Ligands for the Treatment of Neurodegenerative Disorders.
Otto R, Penzis R, Gaube F, Adolph O, Föhr KJ, Warncke P, Robaa D, Appenroth D, Fleck C, Enzensperger C, Lehmann J, Winckler T.
J Med Chem (2015) 58 : 6710 -6715
PubMed 26278660 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 5.34 6.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3605361 1 6.11
CHEMBL3605360 1 5.82
CHEMBL3605365 1 5.70
CHEMBL3605363 1 5.58
CHEMBL3605364 1 5.55
CHEMBL1198953 1 5.54
CHEMBL807 MEMANTINE 4.0 1 5.28
CHEMBL3605359 1 5.14
CHEMBL3605362 1 5.13
CHEMBL3605358 1 4.51
CHEMBL95 TACRINE 4.0 1 4.36
CHEMBL3605355 1 -
CHEMBL3605354 1 -
CHEMBL3605353 1 -
CHEMBL1087459 1 -
CHEMBL1098471 1 -
CHEMBL3605366 1 -
CHEMBL3605367 1 -
CHEMBL3605368 1 -
CHEMBL3605369 1 -
CHEMBL3605370 1 -
CHEMBL8706 CLORGILINE 2.0 1 -
CHEMBL972 SELEGILINE 4.0 1 -
CHEMBL3605356 1 -
CHEMBL3605357 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3605361 IC50 = 780.0 nM 6.11
CHEMBL3605360 IC50 = 1500.0 nM 5.82
CHEMBL3605365 IC50 = 2000.0 nM 5.70
CHEMBL3605363 IC50 = 2600.0 nM 5.58
CHEMBL3605364 IC50 = 2800.0 nM 5.55
CHEMBL1198953 IC50 = 2900.0 nM 5.54
CHEMBL807 MEMANTINE IC50 = 5200.0 nM 5.28
CHEMBL3605359 IC50 = 7200.0 nM 5.14
CHEMBL3605362 IC50 = 7400.0 nM 5.13
CHEMBL3605358 IC50 = 30800.0 nM 4.51
CHEMBL95 TACRINE IC50 = 44000.0 nM 4.36
CHEMBL3605355 IC50 - -
CHEMBL3605354 IC50 - -
CHEMBL3605353 IC50 - -
CHEMBL1087459 IC50 - -
CHEMBL1098471 IC50 - -
CHEMBL3605366 IC50 - -
CHEMBL3605367 IC50 - -
CHEMBL3605368 IC50 - -
CHEMBL3605369 IC50 - -
CHEMBL3605370 IC50 - -
CHEMBL8706 CLORGILINE IC50 - -
CHEMBL972 SELEGILINE IC50 - -
CHEMBL3605356 IC50 - -
CHEMBL3605357 IC50 - -