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Assay Detail

CHEMBL1104014

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

Binding
Activity at recombinant iGluR2 receptor expressed in Xenopus laevis oocytes using holding potential of -15 to -20 mV by TEVC electrophysiology
ChEMBL ↗
12
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type Oocyte
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Glutamate receptor 2 (CHEMBL4016) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

4-hydroxy-1,2,5-oxadiazol-3-yl moiety as bioisoster of the carboxy function. Synthesis, ionization constants, and molecular pharmacological characterization at ionotropic glutamate receptors of compounds related to glutamate and its homologues.
Lolli ML, Giordano C, Pickering DS, Rolando B, Hansen KB, Foti A, Contreras-Sanz A, Amir A, Fruttero R, Gasco A, Nielsen B, Johansen TN.
J Med Chem (2010) 53 : 4110 -4118
PubMed 20408529 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 4.75 5.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1094129 2-AMINO-3-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PROPIONIC ACID (STRUCTURAL MIX) — 4 5.03
CHEMBL575060 GLUTAMIC ACID 3.0 2 4.86
CHEMBL1098101 2-AMINO-4-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)BUTANOIC ACID (STRUCTURAL MIX) — 3 -
CHEMBL1098104 2-AMINO-5-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PENTANOIC ACID (STRUCTURAL MIX) — 3 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1094129 2-AMINO-3-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PROPIONIC ACID (STRUCTURAL MIX) EC50 = 9332.54 nM 5.03
CHEMBL1094129 2-AMINO-3-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PROPIONIC ACID (STRUCTURAL MIX) EC50 = 9400.0 nM 5.03
CHEMBL575060 GLUTAMIC ACID EC50 = 13803.84 nM 4.86
CHEMBL575060 GLUTAMIC ACID EC50 = 14000.0 nM 4.85
CHEMBL1094129 2-AMINO-3-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PROPIONIC ACID (STRUCTURAL MIX) EC50 = 42657.95 nM 4.37
CHEMBL1094129 2-AMINO-3-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PROPIONIC ACID (STRUCTURAL MIX) EC50 = 43000.0 nM 4.37
CHEMBL1098101 2-AMINO-4-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)BUTANOIC ACID (STRUCTURAL MIX) EC50 = 489000.0 nM -
CHEMBL1098104 2-AMINO-5-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PENTANOIC ACID (STRUCTURAL MIX) EC50 = 491000.0 nM -
CHEMBL1098101 2-AMINO-4-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)BUTANOIC ACID (STRUCTURAL MIX) EC50 = 489778.82 nM -
CHEMBL1098101 2-AMINO-4-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)BUTANOIC ACID (STRUCTURAL MIX) EC50 - — -
CHEMBL1098104 2-AMINO-5-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PENTANOIC ACID (STRUCTURAL MIX) EC50 = 489778.82 nM -
CHEMBL1098104 2-AMINO-5-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PENTANOIC ACID (STRUCTURAL MIX) EC50 - — -