Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1678441

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

Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
33
Total Activities
33
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 Autocuration

Target

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

Publication

Discovery, synthesis, and structure-activity relationship development of a series of N-(4-acetamido)phenylpicolinamides as positive allosteric modulators of metabotropic glutamate receptor 4 (mGlu(4)) with CNS exposure in rats.
Engers DW, Field JR, Le U, Zhou Y, Bolinger JD, Zamorano R, Blobaum AL, Jones CK, Jadhav S, Weaver CD, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR.
J Med Chem (2011) 54 : 1106 -1110
PubMed 21247167 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 33 5.98 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1672234 1 7.00
CHEMBL1672245 1 6.94
CHEMBL1672244 1 6.44
CHEMBL1909434 1 6.39
CHEMBL1672243 1 6.37
CHEMBL1672238 1 6.29
CHEMBL1672241 1 6.25
CHEMBL1672232 1 6.20
CHEMBL1672233 1 6.07
CHEMBL1672242 1 6.02
CHEMBL1385271 1 6.01
CHEMBL1909435 1 5.98
CHEMBL1672237 1 5.95
CHEMBL1373422 1 5.93
CHEMBL1672236 1 5.88
CHEMBL1672257 1 5.85
CHEMBL1672256 1 5.85
CHEMBL1509597 1 5.84
CHEMBL1672240 1 5.79
CHEMBL1672235 1 5.75
CHEMBL1672239 1 5.68
CHEMBL1909431 1 5.67
CHEMBL1909433 1 5.66
CHEMBL1672247 1 5.62
CHEMBL1672246 1 5.37
CHEMBL1909436 1 5.33
CHEMBL507522 1 5.32
CHEMBL1672231 1 -
CHEMBL1672230 1 -
CHEMBL1909430 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1672234 EC50 = 99.5 nM 7.00
CHEMBL1672245 EC50 = 114.0 nM 6.94
CHEMBL1672244 EC50 = 361.0 nM 6.44
CHEMBL1909434 EC50 = 403.0 nM 6.39
CHEMBL1672243 EC50 = 426.0 nM 6.37
CHEMBL1672238 EC50 = 517.0 nM 6.29
CHEMBL1672241 EC50 = 556.0 nM 6.25
CHEMBL1672232 EC50 = 627.0 nM 6.20
CHEMBL1672233 EC50 = 845.0 nM 6.07
CHEMBL1672242 EC50 = 958.0 nM 6.02
CHEMBL1385271 EC50 = 977.0 nM 6.01
CHEMBL1909435 EC50 = 1040.0 nM 5.98
CHEMBL1672237 EC50 = 1120.0 nM 5.95
CHEMBL1373422 EC50 = 1170.0 nM 5.93
CHEMBL1672236 EC50 = 1330.0 nM 5.88
CHEMBL1672256 EC50 = 1420.0 nM 5.85
CHEMBL1672257 EC50 = 1410.0 nM 5.85
CHEMBL1509597 EC50 = 1440.0 nM 5.84
CHEMBL1672240 EC50 = 1605.0 nM 5.79
CHEMBL1672235 EC50 = 1780.0 nM 5.75
CHEMBL1672239 EC50 = 2090.0 nM 5.68
CHEMBL1909431 EC50 = 2150.0 nM 5.67
CHEMBL1909433 EC50 = 2180.0 nM 5.66
CHEMBL1672247 EC50 = 2380.0 nM 5.62
CHEMBL1672246 EC50 = 4270.0 nM 5.37
CHEMBL1909436 EC50 = 4720.0 nM 5.33
CHEMBL507522 EC50 = 4740.0 nM 5.32
CHEMBL1672231 EC50 - -
CHEMBL1672230 EC50 - -
CHEMBL1909430 EC50 - -
CHEMBL1909432 EC50 - -
CHEMBL1909437 EC50 - -
CHEMBL1672255 EC50 - -