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Assay Detail

CHEMBL747000

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Functional
Inhibitory activity against NMDA open channel block
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Novel benzo[b]quinolizinium cations as uncompetitive N-methyl-D-aspartic acid (NMDA) antagonists: the relationship between log D and agonist independent (closed) NMDA channel block.
Earley WG, Kumar V, Mallamo JP, Subramanyam C, Dority JA, Miller MS, DeHaven-Hudkins DL, Aimone LD, Kelly MD, Ault B.
J Med Chem (1995) 38 : 3586 -3592
PubMed 7658445 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.39 8.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1202358 1 8.14
CHEMBL1202359 1 8.04
CHEMBL284237 DIZOCILPINE 2.0 1 7.64
CHEMBL419052 1 7.57
CHEMBL329612 1 7.50
CHEMBL275528 PHENCYCLIDINE 2.0 1 6.57
CHEMBL1202354 1 6.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1202358 IC50 = 7.3 nM 8.14
CHEMBL1202359 IC50 = 9.13 nM 8.04
CHEMBL284237 DIZOCILPINE IC50 = 23.0 nM 7.64
CHEMBL419052 IC50 = 27.0 nM 7.57
CHEMBL329612 IC50 = 32.0 nM 7.50
CHEMBL275528 PHENCYCLIDINE IC50 = 270.0 nM 6.57
CHEMBL1202354 IC50 = 557.0 nM 6.25