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Assay Detail

CHEMBL680160

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Binding
Binding affinity for Group II Metabotropic glutamate receptor was measured using [3H]glutamate in rat forebrain membranes
ChEMBL ↗
60
Total Activities
58
Compounds Tested
2
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

2-substituted (2SR)-2-amino-2-((1SR,2SR)-2-carboxycycloprop-1-yl)glycines as potent and selective antagonists of group II metabotropic glutamate receptors. 2. Effects of aromatic substitution, pharmacological characterization, and bioavailability.
Ornstein PL, Bleisch TJ, Arnold MB, Kennedy JH, Wright RA, Johnson BG, Tizzano JP, Helton DR, Kallman MJ, Schoepp DD, Hérin M.
J Med Chem (1998) 41 : 358 -378
PubMed 9464367 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 58 6.57 8.54
Displacement 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL432038 — — 1 8.54
CHEMBL124501 — — 1 7.92
CHEMBL122179 — — 1 7.68
CHEMBL338282 — — 1 7.66
CHEMBL124201 — — 1 7.54
CHEMBL124472 — — 1 7.47
CHEMBL124078 — — 1 7.46
CHEMBL124567 — — 1 7.20
CHEMBL331445 — — 1 7.17
CHEMBL332754 — — 1 7.16
CHEMBL2112634 — — 1 7.11
CHEMBL125985 — — 2 7.05
CHEMBL341457 — — 1 7.03
CHEMBL333771 — — 1 7.00
CHEMBL123083 — — 1 6.96
CHEMBL2111822 — — 1 6.96
CHEMBL122133 — — 1 6.89
CHEMBL123847 — — 1 6.85
CHEMBL124483 — — 1 6.82
CHEMBL338032 — — 1 6.80
CHEMBL125121 — — 1 6.77
CHEMBL124590 — — 1 6.77
CHEMBL123842 — — 1 6.70
CHEMBL123032 — — 1 6.66
CHEMBL339542 — — 1 6.66
CHEMBL332526 — — 1 6.66
CHEMBL122905 — — 1 6.58
CHEMBL123790 — — 1 6.54
CHEMBL125545 — — 1 6.52
CHEMBL122555 — — 1 6.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL432038 — IC50 = 2.9 nM 8.54
CHEMBL124501 — IC50 = 12.0 nM 7.92
CHEMBL122179 — IC50 = 21.0 nM 7.68
CHEMBL338282 — IC50 = 22.0 nM 7.66
CHEMBL124201 — IC50 = 29.0 nM 7.54
CHEMBL124472 — IC50 = 34.0 nM 7.47
CHEMBL124078 — IC50 = 35.0 nM 7.46
CHEMBL124567 — IC50 = 63.0 nM 7.20
CHEMBL331445 — IC50 = 67.0 nM 7.17
CHEMBL332754 — IC50 = 69.0 nM 7.16
CHEMBL2112634 — IC50 = 77.0 nM 7.11
CHEMBL125985 — IC50 = 89.0 nM 7.05
CHEMBL341457 — IC50 = 94.0 nM 7.03
CHEMBL333771 — IC50 = 100.0 nM 7.00
CHEMBL2111822 — IC50 = 110.0 nM 6.96
CHEMBL123083 — IC50 = 110.0 nM 6.96
CHEMBL122133 — IC50 = 130.0 nM 6.89
CHEMBL123847 — IC50 = 140.0 nM 6.85
CHEMBL124483 — IC50 = 150.0 nM 6.82
CHEMBL338032 — IC50 = 160.0 nM 6.80
CHEMBL125121 — IC50 = 170.0 nM 6.77
CHEMBL124590 — IC50 = 170.0 nM 6.77
CHEMBL123842 — IC50 = 200.0 nM 6.70
CHEMBL123032 — IC50 = 220.0 nM 6.66
CHEMBL332526 — IC50 = 220.0 nM 6.66
CHEMBL339542 — IC50 = 220.0 nM 6.66
CHEMBL122905 — IC50 = 260.0 nM 6.58
CHEMBL123790 — IC50 = 290.0 nM 6.54
CHEMBL125545 — IC50 = 300.0 nM 6.52
CHEMBL122555 — IC50 = 310.0 nM 6.51
CHEMBL2112582 — IC50 = 320.0 nM 6.50
CHEMBL338874 — IC50 = 360.0 nM 6.44
CHEMBL125927 — IC50 = 370.0 nM 6.43
CHEMBL127903 — IC50 = 370.0 nM 6.43
CHEMBL407750 — IC50 = 410.0 nM 6.39
CHEMBL124604 — IC50 = 410.0 nM 6.39
CHEMBL125265 — IC50 = 460.0 nM 6.34
CHEMBL119635 — IC50 = 470.0 nM 6.33
CHEMBL333275 — IC50 = 480.0 nM 6.32
CHEMBL340905 — IC50 = 510.0 nM 6.29
CHEMBL144151 — IC50 = 530.0 nM 6.28
CHEMBL421620 — IC50 = 570.0 nM 6.24
CHEMBL332130 — IC50 = 570.0 nM 6.24
CHEMBL338341 — IC50 = 590.0 nM 6.23
CHEMBL126123 — IC50 = 680.0 nM 6.17
CHEMBL331156 — IC50 = 710.0 nM 6.15
CHEMBL123376 — IC50 = 860.0 nM 6.07
CHEMBL122033 — IC50 = 1400.0 nM 5.85
CHEMBL340452 — IC50 = 1500.0 nM 5.82
CHEMBL2311086 — IC50 = 2000.0 nM 5.70