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Assay Detail

CHEMBL750405

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

Binding
Binding affinity against NR1A/2B receptor in rat brains by [3H]ifenprodil displacement.
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Glutamate NMDA receptor; Grin1/Grin2b (CHEMBL2096666)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Subtype selective NMDA receptor antagonists: evaluation of some novel alkynyl analogues.
Kornberg BE, Nikam SS, Wright JL, Kesten SR, Meltzer LT, Coughenour L, Barr B, Serpa KA, McCormick J.
Bioorg Med Chem Lett (2004) 14 : 1213 -1216
PubMed 14980668 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 7.51 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL19849 1 8.70
CHEMBL19506 1 8.52
CHEMBL19419 1 8.40
CHEMBL19404 1 8.05
CHEMBL19636 1 7.85
CHEMBL283753 1 7.82
CHEMBL19559 1 7.72
CHEMBL19349 1 7.70
CHEMBL19576 1 7.68
CHEMBL19342 1 7.62
CHEMBL280882 1 7.51
CHEMBL19952 1 7.29
CHEMBL19957 1 7.25
CHEMBL417822 1 7.00
CHEMBL416000 1 6.98
CHEMBL19590 1 6.85
CHEMBL19769 1 6.80
CHEMBL280200 1 6.55
CHEMBL19945 1 6.32
CHEMBL19929 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL19849 IC50 = 2.0 nM 8.70
CHEMBL19506 IC50 = 3.0 nM 8.52
CHEMBL19419 IC50 = 4.0 nM 8.40
CHEMBL19404 IC50 = 9.0 nM 8.05
CHEMBL19636 IC50 = 14.0 nM 7.85
CHEMBL283753 IC50 = 15.0 nM 7.82
CHEMBL19559 IC50 = 19.0 nM 7.72
CHEMBL19349 IC50 = 20.0 nM 7.70
CHEMBL19576 IC50 = 21.0 nM 7.68
CHEMBL19342 IC50 = 24.0 nM 7.62
CHEMBL280882 IC50 = 31.0 nM 7.51
CHEMBL19952 IC50 = 51.0 nM 7.29
CHEMBL19957 IC50 = 56.0 nM 7.25
CHEMBL417822 IC50 = 100.0 nM 7.00
CHEMBL416000 IC50 = 104.0 nM 6.98
CHEMBL19590 IC50 = 142.0 nM 6.85
CHEMBL19769 IC50 = 157.0 nM 6.80
CHEMBL280200 IC50 = 284.0 nM 6.55
CHEMBL19945 IC50 = 481.0 nM 6.32
CHEMBL19929 IC50 > 1000.0 nM -