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Assay Detail

CHEMBL4620114

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

Binding
Negative allosteric modulation of human mGluR2 by FLIPR assay
34
Total Activities
33
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 of 4-arylquinoline-2-carboxamides, highly potent and selective class of mGluR2 negative allosteric modulators: From HTS to activity in animal models.
Shu Y, Diamond TL, Hershey JC, Huang S, Magliaro BC, O'Brien JA, Schlegel KS, Puri V, Uebele VN, Uslaner JM, Wang C, Converso A.
Bioorg Med Chem Lett (2020) 30 : 127066 -127066
PubMed 32173198 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 7.19 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3892073 1 8.05
CHEMBL4637618 1 8.00
CHEMBL4642428 2 7.92
CHEMBL4640203 1 7.89
CHEMBL4642338 1 7.80
CHEMBL4109248 1 7.80
CHEMBL4644424 1 7.72
CHEMBL3973949 1 7.68
CHEMBL4647980 1 7.60
CHEMBL4108213 1 7.44
CHEMBL4640529 1 7.44
CHEMBL3953417 1 7.24
CHEMBL3919306 1 7.21
CHEMBL3974648 1 7.17
CHEMBL4638570 1 7.17
CHEMBL4635528 1 7.04
CHEMBL4643527 1 6.84
CHEMBL3945170 1 6.83
CHEMBL4634754 1 6.62
CHEMBL4636186 1 6.43
CHEMBL4642255 1 6.39
CHEMBL4634600 1 6.39
CHEMBL4634351 1 5.86
CHEMBL4646222 1 5.57
CHEMBL4645156 1 -
CHEMBL4638395 1 -
CHEMBL4632721 1 -
CHEMBL4640683 1 -
CHEMBL4649821 1 -
CHEMBL4646658 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3892073 IC50 = 9.0 nM 8.05
CHEMBL4637618 IC50 = 10.0 nM 8.00
CHEMBL4642428 IC50 = 12.0 nM 7.92
CHEMBL4640203 IC50 = 13.0 nM 7.89
CHEMBL4642338 IC50 = 16.0 nM 7.80
CHEMBL4109248 IC50 = 16.0 nM 7.80
CHEMBL4644424 IC50 = 19.0 nM 7.72
CHEMBL4642428 IC50 = 19.0 nM 7.72
CHEMBL3973949 IC50 = 21.0 nM 7.68
CHEMBL4647980 IC50 = 25.0 nM 7.60
CHEMBL4108213 IC50 = 36.0 nM 7.44
CHEMBL4640529 IC50 = 36.0 nM 7.44
CHEMBL3953417 IC50 = 58.0 nM 7.24
CHEMBL3919306 IC50 = 61.0 nM 7.21
CHEMBL3974648 IC50 = 68.0 nM 7.17
CHEMBL4638570 IC50 = 68.0 nM 7.17
CHEMBL4635528 IC50 = 91.0 nM 7.04
CHEMBL4643527 IC50 = 144.0 nM 6.84
CHEMBL3945170 IC50 = 149.0 nM 6.83
CHEMBL4634754 IC50 = 238.0 nM 6.62
CHEMBL4636186 IC50 = 367.0 nM 6.43
CHEMBL4642255 IC50 = 409.0 nM 6.39
CHEMBL4634600 IC50 = 404.0 nM 6.39
CHEMBL4634351 IC50 = 1378.0 nM 5.86
CHEMBL4646222 IC50 = 2700.0 nM 5.57
CHEMBL4645156 IC50 > 10000.0 nM -
CHEMBL4638395 IC50 > 10000.0 nM -
CHEMBL4632721 IC50 > 10000.0 nM -
CHEMBL4640683 IC50 > 10000.0 nM -
CHEMBL4649821 IC50 > 10000.0 nM -
CHEMBL4646658 IC50 > 10000.0 nM -
CHEMBL4638009 IC50 > 10000.0 nM -
CHEMBL4635360 IC50 > 10000.0 nM -
CHEMBL4642363 IC50 > 10000.0 nM -