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Assay Detail

CHEMBL749385

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

Binding
Ability to compete with [3H]CCP for rat cortical and hippocampal membrane glutamate binding site.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Hippocampus
Confidence 1 — Organism
Curated By Autocuration

Publication

3-(2-Carboxyindol-3-yl)propionic acid-based antagonists of the N-methyl-D-aspartic acid receptor associated glycine binding site.
Salituro FG, Harrison BL, Baron BM, Nyce PL, Stewart KT, Kehne JH, White HS, McDonald IA.
J Med Chem (1992) 35 : 1791 -1799
PubMed 1534125 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 4.44 4.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL50267 1 4.92
CHEMBL51196 1 4.80
CHEMBL417544 1 4.60
CHEMBL278097 1 4.47
CHEMBL54120 1 4.29
CHEMBL50160 1 4.22
CHEMBL299155 TRANSTORINE 1.0 1 4.15
CHEMBL300949 1 4.06
CHEMBL31344 1 -
CHEMBL295718 1 -
CHEMBL301556 1 -
CHEMBL53744 1 -
CHEMBL298643 1 -
CHEMBL50502 1 -
CHEMBL278390 INDOLE-2-CARBOXYLIC ACID 1 -
CHEMBL50744 1 -
CHEMBL298929 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL50267 IC50 = 12000.0 nM 4.92
CHEMBL51196 IC50 = 16000.0 nM 4.80
CHEMBL417544 IC50 = 25000.0 nM 4.60
CHEMBL278097 IC50 = 34000.0 nM 4.47
CHEMBL54120 IC50 = 51000.0 nM 4.29
CHEMBL50160 IC50 = 60000.0 nM 4.22
CHEMBL299155 TRANSTORINE IC50 = 71000.0 nM 4.15
CHEMBL300949 IC50 = 88000.0 nM 4.06
CHEMBL31344 IC50 = 358000.0 nM -
CHEMBL295718 IC50 = 283000.0 nM -
CHEMBL301556 IC50 > 1000000.0 nM -
CHEMBL53744 IC50 > 1000000.0 nM -
CHEMBL298643 IC50 = 710000.0 nM -
CHEMBL50502 IC50 > 100000.0 nM -
CHEMBL278390 INDOLE-2-CARBOXYLIC ACID IC50 = 4200000.0 nM -
CHEMBL50744 IC50 > 100000.0 nM -
CHEMBL298929 IC50 = 141000.0 nM -