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Assay Detail

CHEMBL718215

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

Functional
Agonist potency against cloned Metabotropic glutamate receptor 2 (mGluR-2).
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Metabotropic glutamate receptor 2 (CHEMBL5137)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Ligands for glutamate receptors: design and therapeutic prospects.
Bräuner-Osborne H, Egebjerg J, Nielsen EO, Madsen U, Krogsgaard-Larsen P.
J Med Chem (2000) 43 : 2609 -2645
PubMed 10893301 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 6.21 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL275079 LY-379268 1 8.57
CHEMBL88999 1 8.41
CHEMBL8759 EGLUMETAD 2.0 1 7.96
CHEMBL38499 1 6.64
CHEMBL90501 1 6.48
CHEMBL40086 1 6.35
CHEMBL41221 1 5.70
CHEMBL297150 1 5.32
CHEMBL34453 1 5.30
CHEMBL444589 1 4.70
CHEMBL126608 1 4.64
CHEMBL88804 (S)-2-AMINOADIPIC ACID 1 4.46
CHEMBL277475 1 -
CHEMBL315268 1 -
CHEMBL329236 1 -
CHEMBL94990 1 -
CHEMBL279956 QUISQUALATE 1 -
CHEMBL88124 1 -
CHEMBL33567 1 -
CHEMBL284895 1 -
CHEMBL39221 1 -
CHEMBL313394 1 -
CHEMBL89001 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL275079 LY-379268 Ki = 2.7 nM 8.57
CHEMBL88999 Ki = 3.9 nM 8.41
CHEMBL8759 EGLUMETAD Ki = 11.0 nM 7.96
CHEMBL38499 Ki = 230.0 nM 6.64
CHEMBL90501 Ki = 330.0 nM 6.48
CHEMBL40086 Ki = 450.0 nM 6.35
CHEMBL41221 Ki = 2000.0 nM 5.70
CHEMBL297150 Ki = 4800.0 nM 5.32
CHEMBL34453 Ki = 5000.0 nM 5.30
CHEMBL444589 Ki = 20000.0 nM 4.70
CHEMBL126608 Ki = 23000.0 nM 4.64
CHEMBL88804 (S)-2-AMINOADIPIC ACID Ki = 35000.0 nM 4.46
CHEMBL277475 Ki > 300000.0 nM -
CHEMBL315268 Ki > 1000000.0 nM -
CHEMBL329236 Ki > 1000000.0 nM -
CHEMBL94990 Ki = 577000.0 nM -
CHEMBL279956 QUISQUALATE Ki > 1000000.0 nM -
CHEMBL88124 Ki > 1000000.0 nM -
CHEMBL33567 Ki > 1000000.0 nM -
CHEMBL284895 Ki = 110000.0 nM -
CHEMBL39221 Ki > 1000000.0 nM -
CHEMBL313394 Ki > 1000000.0 nM -
CHEMBL89001 Ki = - nM -