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Assay Detail

CHEMBL711712

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

Functional
Agonist potency against cloned metabotropic glutamate receptor 5
45
Total Activities
45
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 5 (CHEMBL3227)
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 45 5.61 7.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL66654 1 7.44
CHEMBL279956 QUISQUALATE 1 7.26
CHEMBL88612 1 6.54
CHEMBL88553 1 6.43
CHEMBL92162 1 6.33
CHEMBL90501 1 6.14
CHEMBL39221 1 5.72
CHEMBL280563 1 5.51
CHEMBL92118 1 5.47
CHEMBL432038 1 5.09
CHEMBL575060 GLUTAMIC ACID 3.0 1 4.94
CHEMBL88124 1 4.85
CHEMBL34453 1 4.82
CHEMBL284895 1 4.77
CHEMBL126608 1 4.44
CHEMBL315663 1 4.01
CHEMBL277475 1 -
CHEMBL297150 1 -
CHEMBL40086 1 -
CHEMBL315268 1 -
CHEMBL313124 1 -
CHEMBL299683 1 -
CHEMBL43412 1 -
CHEMBL33567 1 -
CHEMBL94990 1 -
CHEMBL315591 1 -
CHEMBL88184 1 -
CHEMBL313938 1 -
CHEMBL40123 1 -
CHEMBL2021372 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL66654 Ki = 36.0 nM 7.44
CHEMBL279956 QUISQUALATE Ki = 55.0 nM 7.26
CHEMBL88612 Ki = 290.0 nM 6.54
CHEMBL88553 Ki = 370.0 nM 6.43
CHEMBL92162 Ki = 470.0 nM 6.33
CHEMBL90501 Ki = 720.0 nM 6.14
CHEMBL39221 Ki = 1900.0 nM 5.72
CHEMBL280563 Ki = 3100.0 nM 5.51
CHEMBL92118 Ki = 3400.0 nM 5.47
CHEMBL432038 Ki = 8200.0 nM 5.09
CHEMBL575060 GLUTAMIC ACID Ki = 11400.0 nM 4.94
CHEMBL88124 Ki = 14000.0 nM 4.85
CHEMBL34453 Ki = 15000.0 nM 4.82
CHEMBL284895 Ki = 17000.0 nM 4.77
CHEMBL126608 Ki = 36000.0 nM 4.44
CHEMBL315663 Ki = 97000.0 nM 4.01
CHEMBL327783 Ki > 100000.0 nM -
CHEMBL71898 Ki > 1000000.0 nM -
CHEMBL86508 Ki > 1000000.0 nM -
CHEMBL277961 Ki > 1000000.0 nM -
CHEMBL60238 Ki = 600000.0 nM -
CHEMBL313394 Ki > 1000000.0 nM -
CHEMBL8759 EGLUMETAD Ki > 100000.0 nM -
CHEMBL275079 LY-379268 Ki > 100000.0 nM -
CHEMBL330097 Ki > 100000.0 nM -
CHEMBL305406 Ki > 100000.0 nM -
CHEMBL313713 Ki = 1000000.0 nM -
CHEMBL39338 Ki > 300000.0 nM -
CHEMBL88804 (S)-2-AMINOADIPIC ACID Ki > 1000000.0 nM -
CHEMBL88999 Ki > 100000.0 nM -
CHEMBL316451 Ki > 10000000.0 nM -
CHEMBL2021372 Ki > 1000000.0 nM -
CHEMBL40123 Ki > 300000.0 nM -
CHEMBL313938 Ki > 1000000.0 nM -
CHEMBL88184 Ki = 490000.0 nM -
CHEMBL315591 Ki > 100000.0 nM -
CHEMBL94990 Ki > 2000000.0 nM -
CHEMBL33567 Ki > 1000000.0 nM -
CHEMBL43412 Ki = 103000.0 nM -
CHEMBL299683 Ki > 2000000.0 nM -
CHEMBL313124 Ki > 100000.0 nM -
CHEMBL315268 Ki > 1000000.0 nM -
CHEMBL40086 Ki > 100000.0 nM -
CHEMBL297150 Ki > 1000000.0 nM -
CHEMBL277475 Ki > 500000.0 nM -