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Assay Detail

CHEMBL712473

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

Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
18
Total Activities
18
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 8 (CHEMBL3228)
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 18 5.62 7.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL33567 1 7.21
CHEMBL432038 1 6.77
CHEMBL277475 1 6.68
CHEMBL275079 LY-379268 1 5.77
CHEMBL280563 1 5.47
CHEMBL88999 1 5.14
CHEMBL575060 GLUTAMIC ACID 3.0 1 5.02
CHEMBL8759 EGLUMETAD 2.0 1 4.92
CHEMBL330097 1 4.82
CHEMBL34453 1 4.35
CHEMBL40123 1 -
CHEMBL327783 1 -
CHEMBL88612 1 -
CHEMBL40086 1 -
CHEMBL39338 1 -
CHEMBL39221 1 -
CHEMBL66654 1 -
CHEMBL88553 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL33567 Ki = 61.0 nM 7.21
CHEMBL432038 Ki = 170.0 nM 6.77
CHEMBL277475 Ki = 210.0 nM 6.68
CHEMBL275079 LY-379268 Ki = 1700.0 nM 5.77
CHEMBL280563 Ki = 3400.0 nM 5.47
CHEMBL88999 Ki = 7300.0 nM 5.14
CHEMBL575060 GLUTAMIC ACID Ki = 9500.0 nM 5.02
CHEMBL8759 EGLUMETAD Ki = 12000.0 nM 4.92
CHEMBL330097 Ki = 15000.0 nM 4.82
CHEMBL34453 Ki = 45000.0 nM 4.35
CHEMBL40123 Ki > 300000.0 nM -
CHEMBL327783 Ki > 100000.0 nM -
CHEMBL88612 Ki > 100000.0 nM -
CHEMBL40086 Ki > 100000.0 nM -
CHEMBL39338 Ki > 300000.0 nM -
CHEMBL39221 Ki > 1000000.0 nM -
CHEMBL66654 Ki > 100000.0 nM -
CHEMBL88553 Ki > 100000.0 nM -