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Assay Detail

CHEMBL719076

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

Functional
Agonist potency against cloned human metabotropic glutamate receptor 1
52
Total Activities
52
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 1 (CHEMBL3772)
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 52 5.09 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38499 1 6.82
CHEMBL92162 1 6.46
CHEMBL279956 QUISQUALATE 1 5.96
CHEMBL90501 1 5.80
CHEMBL92118 1 5.24
CHEMBL313124 1 5.22
CHEMBL39221 1 5.18
CHEMBL432038 1 5.17
CHEMBL315591 1 5.06
CHEMBL327783 1 5.00
CHEMBL575060 GLUTAMIC ACID 3.0 1 5.00
CHEMBL41221 1 5.00
CHEMBL43412 1 4.60
CHEMBL66654 1 4.52
CHEMBL444589 1 4.52
CHEMBL34453 1 4.38
CHEMBL284895 1 4.37
CHEMBL280563 1 4.30
CHEMBL94990 1 4.08
CHEMBL40123 1 -
CHEMBL313938 1 -
CHEMBL89293 1 -
CHEMBL126608 1 -
CHEMBL40086 1 -
CHEMBL297150 1 -
CHEMBL315268 1 -
CHEMBL299683 1 -
CHEMBL315663 1 -
CHEMBL88184 1 -
CHEMBL277475 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38499 Ki = 150.0 nM 6.82
CHEMBL92162 Ki = 350.0 nM 6.46
CHEMBL279956 QUISQUALATE Ki = 1100.0 nM 5.96
CHEMBL90501 Ki = 1600.0 nM 5.80
CHEMBL92118 Ki = 5700.0 nM 5.24
CHEMBL313124 Ki = 6000.0 nM 5.22
CHEMBL39221 Ki = 6600.0 nM 5.18
CHEMBL432038 Ki = 6800.0 nM 5.17
CHEMBL315591 Ki = 8800.0 nM 5.06
CHEMBL327783 Ki = 9900.0 nM 5.00
CHEMBL575060 GLUTAMIC ACID Ki = 10000.0 nM 5.00
CHEMBL41221 Ki = 10000.0 nM 5.00
CHEMBL43412 Ki = 25000.0 nM 4.60
CHEMBL66654 Ki = 30000.0 nM 4.52
CHEMBL444589 Ki = 30000.0 nM 4.52
CHEMBL34453 Ki = 42000.0 nM 4.38
CHEMBL284895 Ki = 43000.0 nM 4.37
CHEMBL280563 Ki = 50000.0 nM 4.30
CHEMBL94990 Ki = 84000.0 nM 4.08
CHEMBL88999 Ki > 100000.0 nM -
CHEMBL33567 Ki > 1000000.0 nM -
CHEMBL88804 (S)-2-AMINOADIPIC ACID Ki > 1000000.0 nM -
CHEMBL39338 Ki > 300000.0 nM -
CHEMBL313713 Ki = 500000.0 nM -
CHEMBL305406 Ki > 100000.0 nM -
CHEMBL330097 Ki > 100000.0 nM -
CHEMBL2021372 Ki = 232000.0 nM -
CHEMBL8759 EGLUMETAD Ki > 100000.0 nM -
CHEMBL313394 Ki > 1000000.0 nM -
CHEMBL60238 Ki > 1000000.0 nM -
CHEMBL315032 Ki > 1000000.0 nM -
CHEMBL277961 Ki > 1000000.0 nM -
CHEMBL86508 Ki > 1000000.0 nM -
CHEMBL88553 Ki > 100000.0 nM -
CHEMBL89001 Ki = - nM -
CHEMBL71898 Ki > 1000000.0 nM -
CHEMBL275079 LY-379268 Ki > 100000.0 nM -
CHEMBL88612 Ki > 100000.0 nM -
CHEMBL329236 Ki > 1000000.0 nM -
CHEMBL277475 Ki > 500000.0 nM -
CHEMBL88184 Ki = 250000.0 nM -
CHEMBL315663 Ki = 110000.0 nM -
CHEMBL299683 Ki = 540000.0 nM -
CHEMBL315268 Ki > 1000000.0 nM -
CHEMBL297150 Ki > 1000000.0 nM -
CHEMBL40086 Ki > 100000.0 nM -
CHEMBL126608 Ki = 184000.0 nM -
CHEMBL89293 Ki > 100000.0 nM -
CHEMBL313938 Ki = 214000.0 nM -
CHEMBL40123 Ki > 300000.0 nM -