Assay Detail
Binding
CHEMBL3595950
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-MK-801 from rat cortical membranes NMDA receptor by beta counting analysis in absence of spermine
81
Total Activities
81
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.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 81 | 5.26 | 6.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3594016 | — | — | 1 | 6.64 |
| CHEMBL3594017 | — | — | 1 | 6.62 |
| CHEMBL269032 | — | — | 1 | 6.60 |
| CHEMBL229102 | — | — | 1 | 6.28 |
| CHEMBL3594011 | — | — | 1 | 6.25 |
| CHEMBL3594014 | — | — | 1 | 6.12 |
| CHEMBL249456 | — | — | 1 | 6.10 |
| CHEMBL3594013 | — | — | 1 | 6.07 |
| CHEMBL3594080 | — | — | 1 | 5.94 |
| CHEMBL3594009 | — | — | 1 | 5.91 |
| CHEMBL181480 | — | — | 1 | 5.84 |
| CHEMBL3594081 | — | — | 1 | 5.74 |
| CHEMBL1169964 | — | — | 1 | 5.70 |
| CHEMBL3594008 | — | — | 1 | 5.66 |
| CHEMBL185172 | — | — | 1 | 5.66 |
| CHEMBL3593840 | — | — | 1 | 5.59 |
| CHEMBL1170755 | — | — | 1 | 5.58 |
| CHEMBL1170985 | — | — | 1 | 5.57 |
| CHEMBL3594012 | — | — | 1 | 5.54 |
| CHEMBL9185 | — | — | 1 | 5.52 |
| CHEMBL9126 | — | — | 1 | 5.51 |
| CHEMBL3594010 | — | — | 1 | 5.51 |
| CHEMBL1170548 | — | — | 1 | 5.50 |
| CHEMBL1232046 | — | — | 1 | 5.49 |
| CHEMBL3593841 | — | — | 1 | 5.47 |
| CHEMBL3594018 | — | — | 1 | 5.42 |
| CHEMBL24057 | FURAMIDINE | -1.0 | 1 | 5.37 |
| CHEMBL137195 | — | — | 1 | 5.36 |
| CHEMBL283745 | — | — | 1 | 5.34 |
| CHEMBL102740 | ARCAINE | — | 1 | 5.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3594016 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL3594017 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL269032 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL229102 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL3594011 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL3594014 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL249456 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL3594013 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL3594080 | — | IC50 | = | 1140.0 | nM | 5.94 |
| CHEMBL3594009 | — | IC50 | = | 1220.0 | nM | 5.91 |
| CHEMBL181480 | — | IC50 | = | 1460.0 | nM | 5.84 |
| CHEMBL3594081 | — | IC50 | = | 1840.0 | nM | 5.74 |
| CHEMBL1169964 | — | IC50 | = | 2010.0 | nM | 5.70 |
| CHEMBL185172 | — | IC50 | = | 2190.0 | nM | 5.66 |
| CHEMBL3594008 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL3593840 | — | IC50 | = | 2590.0 | nM | 5.59 |
| CHEMBL1170755 | — | IC50 | = | 2610.0 | nM | 5.58 |
| CHEMBL1170985 | — | IC50 | = | 2710.0 | nM | 5.57 |
| CHEMBL3594012 | — | IC50 | = | 2880.0 | nM | 5.54 |
| CHEMBL9185 | — | IC50 | = | 3030.0 | nM | 5.52 |
| CHEMBL9126 | — | IC50 | = | 3080.0 | nM | 5.51 |
| CHEMBL3594010 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL1170548 | — | IC50 | = | 3180.0 | nM | 5.50 |
| CHEMBL1232046 | — | IC50 | = | 3210.0 | nM | 5.49 |
| CHEMBL3593841 | — | IC50 | = | 3410.0 | nM | 5.47 |
| CHEMBL3594018 | — | IC50 | = | 3770.0 | nM | 5.42 |
| CHEMBL24057 | FURAMIDINE | IC50 | = | 4230.0 | nM | 5.37 |
| CHEMBL137195 | — | IC50 | = | 4370.0 | nM | 5.36 |
| CHEMBL283745 | — | IC50 | = | 4550.0 | nM | 5.34 |
| CHEMBL102740 | ARCAINE | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL3594082 | — | IC50 | = | 4670.0 | nM | 5.33 |
| CHEMBL3594196 | — | IC50 | = | 5010.0 | nM | 5.30 |
| CHEMBL365916 | — | IC50 | = | 5240.0 | nM | 5.28 |
| CHEMBL3594195 | — | IC50 | = | 5340.0 | nM | 5.27 |
| CHEMBL23013 | PROPAMIDINE | IC50 | = | 5540.0 | nM | 5.26 |
| CHEMBL8892 | — | IC50 | = | 6430.0 | nM | 5.19 |
| CHEMBL165542 | — | IC50 | = | 6680.0 | nM | 5.17 |
| CHEMBL1852874 | — | IC50 | = | 6940.0 | nM | 5.16 |
| CHEMBL284933 | — | IC50 | = | 6970.0 | nM | 5.16 |
| CHEMBL69590 | — | IC50 | = | 7050.0 | nM | 5.15 |
| CHEMBL3594083 | — | IC50 | = | 7260.0 | nM | 5.14 |
| CHEMBL88596 | — | IC50 | = | 8130.0 | nM | 5.09 |
| CHEMBL535664 | — | IC50 | = | 9250.0 | nM | 5.03 |
| CHEMBL9121 | — | IC50 | = | 9440.0 | nM | 5.03 |
| CHEMBL1080776 | — | IC50 | = | 9630.0 | nM | 5.02 |
| CHEMBL22629 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL9053 | — | IC50 | = | 9940.0 | nM | 5.00 |
| CHEMBL424711 | — | IC50 | = | 9900.0 | nM | 5.00 |
| CHEMBL535205 | — | IC50 | = | 10300.0 | nM | 4.99 |
| CHEMBL1851600 | — | IC50 | = | 10600.0 | nM | 4.97 |