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Assay Detail

CHEMBL4040508

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

Functional
Positive allosteric modulation of human metabotropic glutamate receptor 2 expressed in CHOK1 cell membranes assessed as increase in glutamate-induced [35S]GTPgammaS binding preincubated for 30 mins followed by [35S]GTPgammaS addition measured after 30 mins by Topcount scintillation counting method
ChEMBL ↗
48
Total Activities
45
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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
EC50 45 7.37 8.95
EC80 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4063313 — — 2 8.95
CHEMBL4101354 — — 1 8.54
CHEMBL4091370 — — 1 8.23
CHEMBL4073628 — — 1 8.11
CHEMBL4080973 — — 1 8.06
CHEMBL4104081 — — 1 8.03
CHEMBL4074664 — — 1 7.91
CHEMBL4093657 — — 1 7.82
CHEMBL4067421 — — 1 7.76
CHEMBL4066051 — — 1 7.76
CHEMBL4072262 — — 1 7.73
CHEMBL4064589 — — 2 7.73
CHEMBL4077609 — — 1 7.60
CHEMBL4075697 — — 1 7.55
CHEMBL4093792 — — 1 7.53
CHEMBL4067298 — — 1 7.53
CHEMBL4060306 — — 1 7.53
CHEMBL4087196 — — 1 7.52
CHEMBL4074421 — — 1 7.48
CHEMBL4067290 — — 2 7.42
CHEMBL4075258 — — 1 7.39
CHEMBL4075537 — — 1 7.39
CHEMBL4075762 — — 1 7.38
CHEMBL4076639 — — 1 7.38
CHEMBL4103808 — — 1 7.25
CHEMBL4076786 — — 1 7.24
CHEMBL4089416 — — 1 7.20
CHEMBL4089955 — — 1 7.19
CHEMBL4089612 — — 1 7.13
CHEMBL4075417 — — 1 7.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4063313 — EC50 = 1.122 nM 8.95
CHEMBL4101354 — EC50 = 2.884 nM 8.54
CHEMBL4091370 — EC50 = 5.888 nM 8.23
CHEMBL4073628 — EC50 = 7.762 nM 8.11
CHEMBL4080973 — EC50 = 8.71 nM 8.06
CHEMBL4104081 — EC50 = 9.333 nM 8.03
CHEMBL4074664 — EC50 = 12.3 nM 7.91
CHEMBL4093657 — EC50 = 15.14 nM 7.82
CHEMBL4067421 — EC50 = 17.38 nM 7.76
CHEMBL4066051 — EC50 = 17.38 nM 7.76
CHEMBL4072262 — EC50 = 18.62 nM 7.73
CHEMBL4064589 — EC50 = 18.62 nM 7.73
CHEMBL4077609 — EC50 = 25.12 nM 7.60
CHEMBL4075697 — EC50 = 28.18 nM 7.55
CHEMBL4060306 — EC50 = 29.51 nM 7.53
CHEMBL4067298 — EC50 = 29.51 nM 7.53
CHEMBL4093792 — EC50 = 29.51 nM 7.53
CHEMBL4087196 — EC50 = 30.2 nM 7.52
CHEMBL4074421 — EC50 = 33.11 nM 7.48
CHEMBL4067290 — EC50 = 38.02 nM 7.42
CHEMBL4075258 — EC50 = 40.74 nM 7.39
CHEMBL4075537 — EC50 = 40.74 nM 7.39
CHEMBL4076639 — EC50 = 41.69 nM 7.38
CHEMBL4075762 — EC50 = 41.69 nM 7.38
CHEMBL4103808 — EC50 = 56.23 nM 7.25
CHEMBL4076786 — EC50 = 57.54 nM 7.24
CHEMBL4089416 — EC50 = 63.1 nM 7.20
CHEMBL4089955 — EC50 = 64.57 nM 7.19
CHEMBL4089612 — EC50 = 74.13 nM 7.13
CHEMBL4075417 — EC50 = 77.62 nM 7.11
CHEMBL3337510 — EC50 = 79.43 nM 7.10
CHEMBL4075593 — EC50 = 87.1 nM 7.06
CHEMBL4088239 — EC50 = 93.33 nM 7.03
CHEMBL593013 — EC50 = 93.33 nM 7.03
CHEMBL4100691 — EC50 = 97.72 nM 7.01
CHEMBL4085882 — EC50 = 100.0 nM 7.00
CHEMBL4092105 — EC50 = 107.15 nM 6.97
CHEMBL4092275 — EC50 = 147.91 nM 6.83
CHEMBL4072134 — EC50 = 151.36 nM 6.82
CHEMBL4081244 — EC50 = 158.49 nM 6.80
CHEMBL4088960 — EC50 = 223.87 nM 6.65
CHEMBL4062535 — EC50 = 223.87 nM 6.65
CHEMBL4093620 — EC50 = 251.19 nM 6.60
CHEMBL3937907 — EC50 = 562.34 nM 6.25
CHEMBL4076286 — EC50 = 630.96 nM 6.20
CHEMBL4063313 — EC80 = 60.0 nM -
CHEMBL4064589 — EC80 = 200.0 nM -
CHEMBL4067290 — EC80 = 600.0 nM -