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Assay Detail

CHEMBL718218

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

Functional
Antagonist potency against cloned Metabotropic glutamate receptor 2
24
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 24 5.50 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL432038 1 7.68
CHEMBL90675 1 7.12
CHEMBL305406 1 6.96
CHEMBL330097 1 6.96
CHEMBL89293 1 6.00
CHEMBL86508 1 4.96
CHEMBL40123 1 4.75
CHEMBL277961 1 4.52
CHEMBL313713 1 4.40
CHEMBL39338 1 4.30
CHEMBL299683 2 4.29
CHEMBL41013 1 4.08
CHEMBL60238 1 -
CHEMBL327783 1 -
CHEMBL66654 1 -
CHEMBL88553 1 -
CHEMBL279838 1 -
CHEMBL43412 1 -
CHEMBL88612 1 -
CHEMBL88184 1 -
CHEMBL315663 1 -
CHEMBL313938 1 -
CHEMBL71898 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL432038 Ki = 21.0 nM 7.68
CHEMBL90675 Ki = 75.0 nM 7.12
CHEMBL305406 Ki = 110.0 nM 6.96
CHEMBL330097 Ki = 110.0 nM 6.96
CHEMBL89293 Ki = 1000.0 nM 6.00
CHEMBL86508 Ki = 11000.0 nM 4.96
CHEMBL40123 Ki = 18000.0 nM 4.75
CHEMBL277961 Ki = 30000.0 nM 4.52
CHEMBL313713 Ki = 40000.0 nM 4.40
CHEMBL39338 Ki = 50000.0 nM 4.30
CHEMBL299683 Ki = 51000.0 nM 4.29
CHEMBL41013 Ki = 84000.0 nM 4.08
CHEMBL71898 Ki = 205000.0 nM -
CHEMBL313938 Ki > 1000000.0 nM -
CHEMBL315663 Ki > 1000000.0 nM -
CHEMBL88184 Ki > 1000000.0 nM -
CHEMBL88612 Ki > 100000.0 nM -
CHEMBL43412 Ki > 300000.0 nM -
CHEMBL299683 Ki = 340000.0 nM -
CHEMBL279838 Ki = 447000.0 nM -
CHEMBL88553 Ki > 100000.0 nM -
CHEMBL66654 Ki > 100000.0 nM -
CHEMBL327783 Ki > 100000.0 nM -
CHEMBL60238 Ki = 200000.0 nM -