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Assay Detail

CHEMBL717238

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

Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
21
Total Activities
21
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 3 (CHEMBL2888)
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 21 6.24 8.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL275079 LY-379268 1 8.34
CHEMBL88999 1 8.12
CHEMBL432038 1 7.85
CHEMBL8759 EGLUMETAD 2.0 1 7.42
CHEMBL330097 1 7.00
CHEMBL90675 1 6.70
CHEMBL40086 1 6.39
CHEMBL280563 1 6.36
CHEMBL90501 1 5.66
CHEMBL40123 1 5.21
CHEMBL575060 GLUTAMIC ACID 3.0 1 5.05
CHEMBL39338 1 4.52
CHEMBL279956 QUISQUALATE 1 4.40
CHEMBL297150 1 4.28
CHEMBL33567 1 -
CHEMBL305406 1 -
CHEMBL66654 1 -
CHEMBL88553 1 -
CHEMBL315268 1 -
CHEMBL277475 1 -
CHEMBL88612 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL275079 LY-379268 Ki = 4.6 nM 8.34
CHEMBL88999 Ki = 7.6 nM 8.12
CHEMBL432038 Ki = 14.0 nM 7.85
CHEMBL8759 EGLUMETAD Ki = 38.0 nM 7.42
CHEMBL330097 Ki = 100.0 nM 7.00
CHEMBL90675 Ki = 200.0 nM 6.70
CHEMBL40086 Ki = 410.0 nM 6.39
CHEMBL280563 Ki = 440.0 nM 6.36
CHEMBL90501 Ki = 2200.0 nM 5.66
CHEMBL40123 Ki = 6100.0 nM 5.21
CHEMBL575060 GLUTAMIC ACID Ki = 9000.0 nM 5.05
CHEMBL39338 Ki = 30000.0 nM 4.52
CHEMBL279956 QUISQUALATE Ki = 40000.0 nM 4.40
CHEMBL297150 Ki = 52000.0 nM 4.28
CHEMBL33567 Ki > 1000000.0 nM -
CHEMBL305406 Ki > 100000.0 nM -
CHEMBL66654 Ki > 100000.0 nM -
CHEMBL88553 Ki > 100000.0 nM -
CHEMBL315268 Ki > 1000000.0 nM -
CHEMBL277475 Ki > 200000.0 nM -
CHEMBL88612 Ki > 100000.0 nM -