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Assay Detail

CHEMBL904584

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

Binding
Displacement of [3H]MK-801 from NMDA receptor in rat brain in presence of 100 uM spermine
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Glutamate NMDA receptor (CHEMBL1907608)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

New polyamine-sensitive inhibitors of the NMDA receptor: syntheses and pharmacological evaluation.
Pöhler T, Schadt O, Niepel D, Rebernik P, Berger ML, Noe CR.
Eur J Med Chem (2007) 42 : 175 -197
PubMed 17112642 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.32 6.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL229603 1 6.01
CHEMBL228880 1 5.57
CHEMBL229553 1 5.55
CHEMBL425657 1 5.53
CHEMBL229554 1 5.53
CHEMBL228825 1 5.41
CHEMBL229312 1 5.39
CHEMBL229309 1 5.27
CHEMBL229555 1 5.18
CHEMBL229246 1 5.16
CHEMBL229455 1 5.12
CHEMBL229552 1 5.11
CHEMBL229310 1 5.10
CHEMBL229279 1 5.07
CHEMBL229102 1 5.05
CHEMBL229221 1 5.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL229603 IC50 = 980.0 nM 6.01
CHEMBL228880 IC50 = 2670.0 nM 5.57
CHEMBL229553 IC50 = 2790.0 nM 5.55
CHEMBL425657 IC50 = 2960.0 nM 5.53
CHEMBL229554 IC50 = 2980.0 nM 5.53
CHEMBL228825 IC50 = 3900.0 nM 5.41
CHEMBL229312 IC50 = 4070.0 nM 5.39
CHEMBL229309 IC50 = 5380.0 nM 5.27
CHEMBL229555 IC50 = 6570.0 nM 5.18
CHEMBL229246 IC50 = 6940.0 nM 5.16
CHEMBL229455 IC50 = 7670.0 nM 5.12
CHEMBL229552 IC50 = 7700.0 nM 5.11
CHEMBL229310 IC50 = 7950.0 nM 5.10
CHEMBL229279 IC50 = 8580.0 nM 5.07
CHEMBL229102 IC50 = 8840.0 nM 5.05
CHEMBL229221 IC50 = 9070.0 nM 5.04