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Assay Detail

CHEMBL909225

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

Functional
Inhibition of NMDA-evoked increase in intracellular calcium ion in rat cortical cells
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Benzimidazole-2-carboxamides as novel NR2B selective NMDA receptor antagonists.
Borza I, Kolok S, Gere A, Nagy J, Fodor L, Galgóczy K, Fetter J, Bertha F, Agai B, Horváth C, Farkas S, Domány G.
Bioorg Med Chem Lett (2006) 16 : 4638 -4640
PubMed 16782335 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 8.20 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL212990 1 8.96
CHEMBL214758 1 8.92
CHEMBL215372 1 8.89
CHEMBL212484 1 8.77
CHEMBL219634 1 8.66
CHEMBL220266 1 8.62
CHEMBL213172 1 8.60
CHEMBL380179 1 8.54
CHEMBL213256 1 8.52
CHEMBL220319 1 8.22
CHEMBL219631 BESONPRODIL -1.0 1 8.18
CHEMBL436521 1 8.07
CHEMBL219737 1 8.06
CHEMBL214632 1 7.92
CHEMBL333936 1 7.75
CHEMBL215371 1 7.40
CHEMBL305195 1 6.80
CHEMBL113919 1 6.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL212990 IC50 = 1.1 nM 8.96
CHEMBL214758 IC50 = 1.2 nM 8.92
CHEMBL215372 IC50 = 1.3 nM 8.89
CHEMBL212484 IC50 = 1.7 nM 8.77
CHEMBL219634 IC50 = 2.2 nM 8.66
CHEMBL220266 IC50 = 2.4 nM 8.62
CHEMBL213172 IC50 = 2.5 nM 8.60
CHEMBL380179 IC50 = 2.9 nM 8.54
CHEMBL213256 IC50 = 3.0 nM 8.52
CHEMBL220319 IC50 = 6.0 nM 8.22
CHEMBL219631 BESONPRODIL IC50 = 6.6 nM 8.18
CHEMBL436521 IC50 = 8.6 nM 8.07
CHEMBL219737 IC50 = 8.7 nM 8.06
CHEMBL214632 IC50 = 12.0 nM 7.92
CHEMBL333936 IC50 = 18.0 nM 7.75
CHEMBL215371 IC50 = 40.0 nM 7.40
CHEMBL305195 IC50 = 159.0 nM 6.80
CHEMBL113919 IC50 = 191.0 nM 6.72