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Assay Detail

CHEMBL3595951

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

Binding
Displacement of [3H]-MK-801 from rat cortical membranes NMDA receptor by beta counting analysis in presence of 30 uM spermine
79
Total Activities
79
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

Pentamidine analogs as inhibitors of [(3)H]MK-801 and [(3)H]ifenprodil binding to rat brain NMDA receptors.
Berger ML, Maciejewska D, Vanden Eynde JJ, Mottamal M, Żabiński J, Kaźmierczak P, Rezler M, Jarak I, Piantanida I, Karminski-Zamola G, Mayence A, Rebernik P, Kumar A, Ismail MA, Boykin DW, Huang TL.
Bioorg Med Chem (2015) 23 : 4489 -4500
PubMed 26117647 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 79 4.64 5.88

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3594017 1 5.88
CHEMBL3594016 1 5.67
CHEMBL181480 1 5.26
CHEMBL269032 1 5.26
CHEMBL3594011 1 5.25
CHEMBL229102 1 5.21
CHEMBL249456 1 5.17
CHEMBL3594195 1 5.17
CHEMBL24057 FURAMIDINE -1.0 1 5.13
CHEMBL3594196 1 4.93
CHEMBL3594014 1 4.90
CHEMBL1232046 1 4.87
CHEMBL3594080 1 4.86
CHEMBL165542 1 4.75
CHEMBL185172 1 4.74
CHEMBL3594012 1 4.68
CHEMBL137195 1 4.62
CHEMBL284933 1 4.62
CHEMBL3594009 1 4.62
CHEMBL3594081 1 4.61
CHEMBL3593840 1 4.60
CHEMBL3594082 1 4.59
CHEMBL365916 1 4.59
CHEMBL1080776 1 4.56
CHEMBL3594018 1 4.54
CHEMBL3594008 1 4.54
CHEMBL3594197 1 4.52
CHEMBL279660 1 4.51
CHEMBL3594083 1 4.51
CHEMBL424711 1 4.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3594017 IC50 = 1320.0 nM 5.88
CHEMBL3594016 IC50 = 2130.0 nM 5.67
CHEMBL269032 IC50 = 5470.0 nM 5.26
CHEMBL181480 IC50 = 5540.0 nM 5.26
CHEMBL3594011 IC50 = 5620.0 nM 5.25
CHEMBL229102 IC50 = 6100.0 nM 5.21
CHEMBL249456 IC50 = 6700.0 nM 5.17
CHEMBL3594195 IC50 = 6760.0 nM 5.17
CHEMBL24057 FURAMIDINE IC50 = 7480.0 nM 5.13
CHEMBL3594196 IC50 = 11700.0 nM 4.93
CHEMBL3594014 IC50 = 12500.0 nM 4.90
CHEMBL1232046 IC50 = 13400.0 nM 4.87
CHEMBL3594080 IC50 = 13800.0 nM 4.86
CHEMBL165542 IC50 = 17700.0 nM 4.75
CHEMBL185172 IC50 = 18400.0 nM 4.74
CHEMBL3594012 IC50 = 20700.0 nM 4.68
CHEMBL137195 IC50 = 23900.0 nM 4.62
CHEMBL284933 IC50 = 24000.0 nM 4.62
CHEMBL3594009 IC50 = 23800.0 nM 4.62
CHEMBL3594081 IC50 = 24700.0 nM 4.61
CHEMBL3593840 IC50 = 24900.0 nM 4.60
CHEMBL3594082 IC50 = 25400.0 nM 4.59
CHEMBL365916 IC50 = 25700.0 nM 4.59
CHEMBL1080776 IC50 = 27700.0 nM 4.56
CHEMBL3594008 IC50 = 29100.0 nM 4.54
CHEMBL3594018 IC50 = 28700.0 nM 4.54
CHEMBL3594197 IC50 = 30000.0 nM 4.52
CHEMBL279660 IC50 = 30700.0 nM 4.51
CHEMBL3594083 IC50 = 31100.0 nM 4.51
CHEMBL424711 IC50 = 34200.0 nM 4.47
CHEMBL9391 IC50 = 36700.0 nM 4.43
CHEMBL3594013 IC50 = 38500.0 nM 4.42
CHEMBL3594010 IC50 = 42300.0 nM 4.37
CHEMBL183814 BIS(4-CARBAMIMIDOYLPHENYL)TEREPHTHALATE IC50 = 46600.0 nM 4.33
CHEMBL1170755 IC50 = 48100.0 nM 4.32
CHEMBL1169964 IC50 = 50700.0 nM 4.29
CHEMBL142952 IC50 = 52900.0 nM 4.28
CHEMBL1170985 IC50 = 54500.0 nM 4.26
CHEMBL1081887 IC50 = 62600.0 nM 4.20
CHEMBL9126 IC50 = 70700.0 nM 4.15
CHEMBL9531 IC50 = 70900.0 nM 4.15
CHEMBL1852874 IC50 = 74900.0 nM 4.13
CHEMBL283745 IC50 = 84200.0 nM 4.08
CHEMBL1170548 IC50 = 85300.0 nM 4.07
CHEMBL88596 IC50 = 85700.0 nM 4.07
CHEMBL9185 IC50 = 92200.0 nM 4.04
CHEMBL586743 IC50 = 466000.0 nM -
CHEMBL8892 IC50 = 106000.0 nM -
CHEMBL535664 IC50 = 159000.0 nM -
CHEMBL535205 IC50 = 139000.0 nM -