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Assay Detail

CHEMBL3595953

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

Binding
Displacement of [3H]-ifenprodil from rat cortical membranes NMDA receptor by beta counting analysis in absence of 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 4.93 6.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3594017 1 6.39
CHEMBL1169964 1 6.12
CHEMBL3594018 1 6.08
CHEMBL181480 1 5.85
CHEMBL3594016 1 5.83
CHEMBL249456 1 5.40
CHEMBL3594012 1 5.34
CHEMBL1170548 1 5.15
CHEMBL185172 1 5.14
CHEMBL3594080 1 5.04
CHEMBL365916 1 4.97
CHEMBL3594013 1 4.94
CHEMBL1170755 1 4.89
CHEMBL3594011 1 4.78
CHEMBL9126 1 4.77
CHEMBL1170985 1 4.77
CHEMBL3594008 1 4.72
CHEMBL269032 1 4.72
CHEMBL3594010 1 4.69
CHEMBL3594014 1 4.66
CHEMBL102740 ARCAINE 1 4.61
CHEMBL183814 BIS(4-CARBAMIMIDOYLPHENYL)TEREPHTHALATE 1 4.57
CHEMBL3594081 1 4.51
CHEMBL3593840 1 4.49
CHEMBL3594007 1 4.36
CHEMBL1852874 1 4.31
CHEMBL229102 1 4.31
CHEMBL185063 1 4.26
CHEMBL3593841 1 4.20
CHEMBL22629 1 4.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3594017 IC50 = 410.0 nM 6.39
CHEMBL1169964 IC50 = 760.0 nM 6.12
CHEMBL3594018 IC50 = 840.0 nM 6.08
CHEMBL181480 IC50 = 1420.0 nM 5.85
CHEMBL3594016 IC50 = 1470.0 nM 5.83
CHEMBL249456 IC50 = 3970.0 nM 5.40
CHEMBL3594012 IC50 = 4540.0 nM 5.34
CHEMBL1170548 IC50 = 7140.0 nM 5.15
CHEMBL185172 IC50 = 7290.0 nM 5.14
CHEMBL3594080 IC50 = 9160.0 nM 5.04
CHEMBL365916 IC50 = 10800.0 nM 4.97
CHEMBL3594013 IC50 = 11400.0 nM 4.94
CHEMBL1170755 IC50 = 13000.0 nM 4.89
CHEMBL3594011 IC50 = 16600.0 nM 4.78
CHEMBL1170985 IC50 = 16900.0 nM 4.77
CHEMBL9126 IC50 = 17000.0 nM 4.77
CHEMBL3594008 IC50 = 19200.0 nM 4.72
CHEMBL269032 IC50 = 19100.0 nM 4.72
CHEMBL3594010 IC50 = 20600.0 nM 4.69
CHEMBL3594014 IC50 = 21900.0 nM 4.66
CHEMBL102740 ARCAINE IC50 = 24400.0 nM 4.61
CHEMBL183814 BIS(4-CARBAMIMIDOYLPHENYL)TEREPHTHALATE IC50 = 27000.0 nM 4.57
CHEMBL3594081 IC50 = 31200.0 nM 4.51
CHEMBL3593840 IC50 = 32500.0 nM 4.49
CHEMBL3594007 IC50 = 43700.0 nM 4.36
CHEMBL1852874 IC50 = 49400.0 nM 4.31
CHEMBL229102 IC50 = 49300.0 nM 4.31
CHEMBL185063 IC50 = 54500.0 nM 4.26
CHEMBL3593841 IC50 = 63800.0 nM 4.20
CHEMBL22629 IC50 = 77700.0 nM 4.11
CHEMBL1851600 IC50 - -
CHEMBL1851728 IC50 - -
CHEMBL142952 IC50 - -
CHEMBL9391 IC50 - -
CHEMBL1852582 IC50 - -
CHEMBL24057 FURAMIDINE IC50 - -
CHEMBL284933 IC50 - -
CHEMBL279660 IC50 - -
CHEMBL3594195 IC50 - -
CHEMBL165542 IC50 - -
CHEMBL3594197 IC50 - -
CHEMBL1232046 IC50 - -
CHEMBL3594196 IC50 - -
CHEMBL1962539 IC50 - -
CHEMBL1963649 IC50 - -
CHEMBL1963648 IC50 - -
CHEMBL1963636 IC50 - -
CHEMBL1080776 IC50 - -
CHEMBL1081887 IC50 - -
CHEMBL424711 IC50 - -