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Assay Detail

CHEMBL985339

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

Functional
Antagonist activity at NMDA receptor in cerebellar granule neurons assessed as inhibition of NMDA-induced increase in intracellular calcium concentration by fluorometric assay
34
Total Activities
34
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Glutamate NMDA receptor (CHEMBL1907608)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

Synthesis and pharmacological evaluation of several ring-contracted amantadine analogs.
Camps P, Duque MD, Vázquez S, Naesens L, De Clercq E, Sureda FX, López-Querol M, Camins A, Pallàs M, Prathalingam SR, Kelly JM, Romero V, Ivorra D, Cortés D.
Bioorg Med Chem (2008) 16 : 9925 -9936
PubMed 18954995 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 4.43 5.82
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL807 MEMANTINE 4.0 1 5.82
CHEMBL445026 1 5.15
CHEMBL500090 1 4.77
CHEMBL450375 1 4.64
CHEMBL499125 1 4.60
CHEMBL505620 1 4.46
CHEMBL445861 1 4.44
CHEMBL448464 1 4.43
CHEMBL511702 1 4.35
CHEMBL456731 1 4.33
CHEMBL444922 1 4.19
CHEMBL458485 1 4.16
CHEMBL456513 1 4.15
CHEMBL507149 1 4.10
CHEMBL460176 1 4.06
CHEMBL448878 1 4.04
CHEMBL454536 1 4.04
CHEMBL660 AMANTADINE 4.0 1 4.04
CHEMBL462519 1 -
CHEMBL512222 1 -
CHEMBL501820 1 -
CHEMBL460607 1 -
CHEMBL460390 1 -
CHEMBL506460 1 -
CHEMBL446494 1 -
CHEMBL448793 1 -
CHEMBL461886 1 -
CHEMBL461887 1 -
CHEMBL460760 1 -
CHEMBL462520 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL807 MEMANTINE IC50 = 1500.0 nM 5.82
CHEMBL445026 IC50 = 7100.0 nM 5.15
CHEMBL500090 IC50 = 17000.0 nM 4.77
CHEMBL450375 IC50 = 23000.0 nM 4.64
CHEMBL499125 IC50 = 25000.0 nM 4.60
CHEMBL505620 IC50 = 35000.0 nM 4.46
CHEMBL445861 IC50 = 36000.0 nM 4.44
CHEMBL448464 IC50 = 37000.0 nM 4.43
CHEMBL511702 IC50 = 45000.0 nM 4.35
CHEMBL456731 IC50 = 47000.0 nM 4.33
CHEMBL444922 IC50 = 65000.0 nM 4.19
CHEMBL458485 IC50 = 70000.0 nM 4.16
CHEMBL456513 IC50 = 71000.0 nM 4.15
CHEMBL507149 IC50 = 80000.0 nM 4.10
CHEMBL460176 IC50 = 87000.0 nM 4.06
CHEMBL454536 IC50 = 92000.0 nM 4.04
CHEMBL448878 IC50 = 92000.0 nM 4.04
CHEMBL660 AMANTADINE IC50 = 92000.0 nM 4.04
CHEMBL456398 IC50 > 200000000.0 nM -
CHEMBL458070 IC50 = 160000.0 nM -
CHEMBL508777 IC50 = 128000.0 nM -
CHEMBL501363 IC50 = 153000.0 nM -
CHEMBL462520 IC50 = 178000.0 nM -
CHEMBL460760 IC50 = 173000.0 nM -
CHEMBL461887 Activity - -
CHEMBL461886 IC50 > 200000000.0 nM -
CHEMBL448793 IC50 > 200000000.0 nM -
CHEMBL446494 IC50 > 200000000.0 nM -
CHEMBL506460 IC50 > 200000000.0 nM -
CHEMBL460390 IC50 > 200000000.0 nM -
CHEMBL460607 IC50 > 200000000.0 nM -
CHEMBL501820 IC50 > 200000000.0 nM -
CHEMBL512222 IC50 > 200000000.0 nM -
CHEMBL462519 IC50 = 138000.0 nM -