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Assay Detail

CHEMBL751238

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

Binding
Displacement of [3H]MK-801 from rat brain membrane N-methyl-D-aspartate glutamate receptor
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

Synthesis and pharmacological evaluation of N,N'-diarylguanidines as potent sodium channel blockers and anticonvulsant agents.
Reddy NL, Fan W, Magar SS, Perlman ME, Yost E, Zhang L, Berlove D, Fischer JB, Burke-Howie K, Wolcott T, Durant GJ.
J Med Chem (1998) 41 : 3298 -3302
PubMed 9703475 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.26 5.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL112806 1 5.66
CHEMBL28853 1 5.60
CHEMBL109210 1 5.48
CHEMBL326502 1 5.46
CHEMBL112132 1 5.40
CHEMBL326741 1 5.11
CHEMBL78083 1 5.10
CHEMBL110909 1 5.00
CHEMBL81602 1 4.99
CHEMBL81626 1 4.75
CHEMBL320340 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL112806 IC50 = 2190.0 nM 5.66
CHEMBL28853 IC50 = 2490.0 nM 5.60
CHEMBL109210 IC50 = 3320.0 nM 5.48
CHEMBL326502 IC50 = 3480.0 nM 5.46
CHEMBL112132 IC50 = 4010.0 nM 5.40
CHEMBL326741 IC50 = 7790.0 nM 5.11
CHEMBL78083 IC50 = 7910.0 nM 5.10
CHEMBL110909 IC50 = 10100.0 nM 5.00
CHEMBL81602 IC50 = 10200.0 nM 4.99
CHEMBL81626 IC50 = 17900.0 nM 4.75
CHEMBL320340 IC50 > 7700.0 nM -