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Assay Detail

CHEMBL4040507

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

Binding
Binding affinity to human metabotropic glutamate receptor 2 expressed in CHOK1 cell membranes by scintillation proximity assay
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Metabotropic glutamate receptor 2 (CHEMBL5137)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and Kinetic Profiling of 7-Aryl-1,2,4-triazolo[4,3-a]pyridines: Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 2.
Doornbos MLJ, Cid JM, Haubrich J, Nunes A, van de Sande JW, Vermond SC, Mulder-Krieger T, Trabanco AA, Ahnaou A, Drinkenburg WH, Lavreysen H, Heitman LH, IJzerman AP, Tresadern G.
J Med Chem (2017) 60 : 6704 -6720
PubMed 28704052 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 45 8.00 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4074664 1 9.00
CHEMBL4087196 1 8.96
CHEMBL4073628 1 8.92
CHEMBL4063313 1 8.82
CHEMBL4093657 1 8.70
CHEMBL4067298 1 8.68
CHEMBL4088239 1 8.66
CHEMBL4080973 1 8.60
CHEMBL4091370 1 8.54
CHEMBL4077609 1 8.52
CHEMBL4104081 1 8.52
CHEMBL4093792 1 8.48
CHEMBL4067421 1 8.47
CHEMBL4064589 1 8.42
CHEMBL4060306 1 8.21
CHEMBL4101354 1 8.14
CHEMBL4100691 1 8.09
CHEMBL4072262 1 8.07
CHEMBL4076786 1 8.06
CHEMBL4103808 1 8.04
CHEMBL4075417 1 8.00
CHEMBL4076639 1 7.99
CHEMBL4075697 1 7.97
CHEMBL4075762 1 7.97
CHEMBL4089955 1 7.94
CHEMBL4067290 1 7.91
CHEMBL4074421 1 7.90
CHEMBL4089416 1 7.90
CHEMBL4075258 1 7.82
CHEMBL4072134 1 7.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4074664 Kd = 1.0 nM 9.00
CHEMBL4087196 Kd = 1.1 nM 8.96
CHEMBL4073628 Kd = 1.2 nM 8.92
CHEMBL4063313 Kd = 1.5 nM 8.82
CHEMBL4093657 Kd = 2.0 nM 8.70
CHEMBL4067298 Kd = 2.1 nM 8.68
CHEMBL4088239 Kd = 2.2 nM 8.66
CHEMBL4080973 Kd = 2.5 nM 8.60
CHEMBL4091370 Kd = 2.9 nM 8.54
CHEMBL4077609 Kd = 3.0 nM 8.52
CHEMBL4104081 Kd = 3.0 nM 8.52
CHEMBL4093792 Kd = 3.3 nM 8.48
CHEMBL4067421 Kd = 3.4 nM 8.47
CHEMBL4064589 Kd = 3.8 nM 8.42
CHEMBL4060306 Kd = 6.1 nM 8.21
CHEMBL4101354 Kd = 7.3 nM 8.14
CHEMBL4100691 Kd = 8.1 nM 8.09
CHEMBL4072262 Kd = 8.6 nM 8.07
CHEMBL4076786 Kd = 8.7 nM 8.06
CHEMBL4103808 Kd = 9.2 nM 8.04
CHEMBL4075417 Kd = 10.0 nM 8.00
CHEMBL4076639 Kd = 10.3 nM 7.99
CHEMBL4075697 Kd = 10.7 nM 7.97
CHEMBL4075762 Kd = 10.8 nM 7.97
CHEMBL4089955 Kd = 11.5 nM 7.94
CHEMBL4067290 Kd = 12.3 nM 7.91
CHEMBL4074421 Kd = 12.7 nM 7.90
CHEMBL4089416 Kd = 12.7 nM 7.90
CHEMBL4075258 Kd = 15.3 nM 7.82
CHEMBL4072134 Kd = 15.6 nM 7.81
CHEMBL4075537 Kd = 16.0 nM 7.80
CHEMBL4081244 Kd = 16.6 nM 7.78
CHEMBL4066051 Kd = 17.4 nM 7.76
CHEMBL4092275 Kd = 19.5 nM 7.71
CHEMBL4062535 Kd = 20.3 nM 7.69
CHEMBL4085882 Kd = 23.3 nM 7.63
CHEMBL4089612 Kd = 25.2 nM 7.60
CHEMBL4088960 Kd = 28.1 nM 7.55
CHEMBL4093620 Kd = 37.6 nM 7.42
CHEMBL4075593 Kd = 42.7 nM 7.37
CHEMBL3337510 Kd = 51.0 nM 7.29
CHEMBL4076286 Kd = 54.0 nM 7.27
CHEMBL4092105 Kd = 100.0 nM 7.00
CHEMBL593013 Kd = 190.0 nM 6.72
CHEMBL3937907 Kd = 600.0 nM 6.22