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Assay Detail

CHEMBL1044679

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

Functional
Allosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium flux
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Metabotropic glutamate receptor 4 (CHEMBL2736)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and SAR of a novel positive allosteric modulator (PAM) of the metabotropic glutamate receptor 4 (mGluR4).
Williams R, Johnson KA, Gentry PR, Niswender CM, Weaver CD, Conn PJ, Lindsley CW, Hopkins CR.
Bioorg Med Chem Lett (2009) 19 : 4967 -4970
PubMed 19640716 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 38 5.51 6.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL578988 1 6.13
CHEMBL578358 1 6.02
CHEMBL571063 1 5.70
CHEMBL568240 1 5.70
CHEMBL578129 1 5.57
CHEMBL565748 1 5.51
CHEMBL578793 1 5.48
CHEMBL568252 1 5.02
CHEMBL584413 1 5.00
CHEMBL568440 1 5.00
CHEMBL577918 1 -
CHEMBL584412 1 -
CHEMBL568226 1 -
CHEMBL578381 1 -
CHEMBL568227 1 -
CHEMBL568029 1 -
CHEMBL568441 1 -
CHEMBL568452 1 -
CHEMBL584609 1 -
CHEMBL568253 1 -
CHEMBL584209 1 -
CHEMBL577474 1 -
CHEMBL577542 1 -
CHEMBL568453 1 -
CHEMBL578589 1 -
CHEMBL565947 1 -
CHEMBL568225 1 -
CHEMBL570602 1 -
CHEMBL570838 1 -
CHEMBL577252 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL578988 EC50 = 740.0 nM 6.13
CHEMBL578358 EC50 = 950.0 nM 6.02
CHEMBL568240 EC50 = 2000.0 nM 5.70
CHEMBL571063 EC50 = 2000.0 nM 5.70
CHEMBL578129 EC50 = 2700.0 nM 5.57
CHEMBL565748 EC50 = 3100.0 nM 5.51
CHEMBL578793 EC50 = 3300.0 nM 5.48
CHEMBL568252 EC50 = 9600.0 nM 5.02
CHEMBL584413 EC50 = 10000.0 nM 5.00
CHEMBL568440 EC50 = 10000.0 nM 5.00
CHEMBL568227 EC50 - -
CHEMBL568018 EC50 - -
CHEMBL568029 EC50 - -
CHEMBL568441 EC50 - -
CHEMBL568452 EC50 - -
CHEMBL584609 EC50 - -
CHEMBL568253 EC50 - -
CHEMBL577919 EC50 - -
CHEMBL571062 EC50 - -
CHEMBL584005 EC50 - -
CHEMBL577688 EC50 - -
CHEMBL568659 EC50 > 10000.0 nM -
CHEMBL578593 EC50 - -
CHEMBL568228 EC50 - -
CHEMBL578381 EC50 - -
CHEMBL568226 EC50 - -
CHEMBL584412 EC50 - -
CHEMBL577918 EC50 - -
CHEMBL584209 EC50 > 10000.0 nM -
CHEMBL577474 EC50 - -
CHEMBL577542 EC50 - -
CHEMBL568453 EC50 - -
CHEMBL578589 EC50 - -
CHEMBL565947 EC50 - -
CHEMBL568225 EC50 - -
CHEMBL570602 EC50 - -
CHEMBL570838 EC50 - -
CHEMBL577252 EC50 - -