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Assay Detail

CHEMBL863344

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

Functional
Inhibition of NMDA-evoked intracellular calcium increase in rat cortical cells
16
Total Activities
16
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

Indole-2-carboxamidines as novel NR2B selective NMDA receptor antagonists.
Borza I, Kolok S, Ignácz-Szendrei G, Greiner I, Tárkányi G, Galgóczy K, Horváth C, Farkas S, Domány G.
Bioorg Med Chem Lett (2005) 15 : 5439 -5441
PubMed 16213709 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.30 8.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL534486 1 8.27
CHEMBL158737 1 8.18
CHEMBL538825 1 7.77
CHEMBL333936 1 7.75
CHEMBL538081 1 7.72
CHEMBL558984 1 7.58
CHEMBL537860 1 7.48
CHEMBL557803 1 7.46
CHEMBL534485 1 7.19
CHEMBL537192 1 7.16
CHEMBL113919 1 6.88
CHEMBL535826 1 6.84
CHEMBL535828 1 6.80
CHEMBL537418 1 6.77
CHEMBL537417 1 6.63
CHEMBL113830 (S,R)-IFENPRODIL 1 6.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL534486 IC50 = 5.4 nM 8.27
CHEMBL158737 IC50 = 6.6 nM 8.18
CHEMBL538825 IC50 = 17.0 nM 7.77
CHEMBL333936 IC50 = 18.0 nM 7.75
CHEMBL538081 IC50 = 19.0 nM 7.72
CHEMBL558984 IC50 = 26.0 nM 7.58
CHEMBL537860 IC50 = 33.0 nM 7.48
CHEMBL557803 IC50 = 35.0 nM 7.46
CHEMBL534485 IC50 = 64.0 nM 7.19
CHEMBL537192 IC50 = 69.0 nM 7.16
CHEMBL113919 IC50 = 131.0 nM 6.88
CHEMBL535826 IC50 = 143.0 nM 6.84
CHEMBL535828 IC50 = 159.0 nM 6.80
CHEMBL537418 IC50 = 170.0 nM 6.77
CHEMBL537417 IC50 = 232.0 nM 6.63
CHEMBL113830 (S,R)-IFENPRODIL IC50 = 470.0 nM 6.33