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Assay Detail

CHEMBL877833

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

Binding
Inhibitory activity towards group 2 metabotropic glutamate receptor by displacement of ACPD-sensitive [3H]- glutamate in rat forebrain membrane
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Forebrain
Subcellular Membrane
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

(2S,4S)-amino-4-(2,2-diphenylethyl)pentanedioic acid selective group 2 metabotropic glutamate receptor antagonist.
Escribano A, Ezquerra J, Pedregal C, Rubio A, Yruretagoyena B, Baker SR, Wright RA, Johnson BG, Schoepp DD.
Bioorg Med Chem Lett (1998) 8 : 765 -770
PubMed 9871538 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 5.41 6.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL40123 1 6.42
CHEMBL350704 1 5.94
CHEMBL352773 1 5.85
CHEMBL351653 1 5.74
CHEMBL165500 1 5.60
CHEMBL351946 1 5.50
CHEMBL353121 1 5.50
CHEMBL166309 1 5.48
CHEMBL39338 1 5.47
CHEMBL168017 1 5.47
CHEMBL348985 1 5.34
CHEMBL442712 1 5.33
CHEMBL353124 1 5.33
CHEMBL350497 1 5.11
CHEMBL424016 1 5.05
CHEMBL349277 1 5.05
CHEMBL164132 1 5.03
CHEMBL423104 1 4.84
CHEMBL305387 1 4.68
CHEMBL164614 1 -
CHEMBL165544 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL40123 IC50 = 380.0 nM 6.42
CHEMBL350704 IC50 = 1160.0 nM 5.94
CHEMBL352773 IC50 = 1400.0 nM 5.85
CHEMBL351653 IC50 = 1840.0 nM 5.74
CHEMBL165500 IC50 = 2490.0 nM 5.60
CHEMBL351946 IC50 = 3160.0 nM 5.50
CHEMBL353121 IC50 = 3200.0 nM 5.50
CHEMBL166309 IC50 = 3330.0 nM 5.48
CHEMBL39338 IC50 = 3380.0 nM 5.47
CHEMBL168017 IC50 = 3400.0 nM 5.47
CHEMBL348985 IC50 = 4600.0 nM 5.34
CHEMBL442712 IC50 = 4650.0 nM 5.33
CHEMBL353124 IC50 = 4690.0 nM 5.33
CHEMBL350497 IC50 = 7850.0 nM 5.11
CHEMBL424016 IC50 = 8990.0 nM 5.05
CHEMBL349277 IC50 = 8820.0 nM 5.05
CHEMBL164132 IC50 = 9280.0 nM 5.03
CHEMBL423104 IC50 = 14500.0 nM 4.84
CHEMBL305387 IC50 = 21100.0 nM 4.68
CHEMBL164614 IC50 > 100000.0 nM -
CHEMBL165544 IC50 > 100000.0 nM -