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Assay Detail

CHEMBL857544

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

Binding
Inhibition of [3H]Ro-256981 binding to N-methyl-D-aspartate glutamate receptor
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Glutamate [NMDA] receptor (CHEMBL2094124)
Type PROTEIN COMPLEX GROUP
Organism Homo sapiens

Publication

Indole-2-carboxamides as novel NR2B selective NMDA receptor antagonists.
Borza I, Kolok S, Gere A, Agai-Csongor E, Agai B, Tárkányi G, Horváth C, Barta-Szalai G, Bozó E, Kiss C, Bielik A, Nagy J, Farkas S, Domány G.
Bioorg Med Chem Lett (2003) 13 : 3859 -3861
PubMed 14552795 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.47 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL219631 BESONPRODIL -1.0 1 8.40
CHEMBL305195 1 8.22
CHEMBL126929 1 8.22
CHEMBL333936 1 7.92
CHEMBL124873 1 7.75
CHEMBL127510 1 7.72
CHEMBL126228 1 7.51
CHEMBL419784 1 7.33
CHEMBL124516 1 6.97
CHEMBL113919 1 6.71
CHEMBL339570 1 6.45
CHEMBL123908 1 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL219631 BESONPRODIL IC50 = 4.0 nM 8.40
CHEMBL305195 IC50 = 6.0 nM 8.22
CHEMBL126929 IC50 = 6.0 nM 8.22
CHEMBL333936 IC50 = 12.0 nM 7.92
CHEMBL124873 IC50 = 18.0 nM 7.75
CHEMBL127510 IC50 = 19.0 nM 7.72
CHEMBL126228 IC50 = 31.0 nM 7.51
CHEMBL419784 IC50 = 47.0 nM 7.33
CHEMBL124516 IC50 = 106.0 nM 6.97
CHEMBL113919 IC50 = 196.0 nM 6.71
CHEMBL339570 IC50 = 359.0 nM 6.45
CHEMBL123908 IC50 = 380.0 nM 6.42