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Assay Detail

CHEMBL898093

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

Functional
Activity at rat mGlu5 receptor expressed in CHO cells assessed as inhibition of quisqualate-stimulated calcium mobilization by FLIPR assay
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Metabotropic glutamate receptor 5 (CHEMBL2564)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists.
Milbank JB, Knauer CS, Augelli-Szafran CE, Sakkab-Tan AT, Lin KK, Yamagata K, Hoffman JK, Zhuang N, Thomas J, Galatsis P, Wendt JA, Mickelson JW, Schwarz RD, Kinsora JJ, Lotarski SM, Stakich K, Gillespie KK, Lam WW, Mutlib AE.
Bioorg Med Chem Lett (2007) 17 : 4415 -4418
PubMed 17590335 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 6.70 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL66654 1 9.70
CHEMBL232188 1 9.10
CHEMBL396135 1 8.85
CHEMBL232189 1 8.80
CHEMBL231790 1 8.70
CHEMBL231788 1 8.70
CHEMBL233417 1 8.62
CHEMBL244796 1 8.11
CHEMBL396177 1 7.89
CHEMBL233358 1 7.77
CHEMBL233418 1 7.64
CHEMBL233615 1 7.14
CHEMBL396415 1 7.12
CHEMBL233616 1 7.09
CHEMBL233617 1 6.51
CHEMBL233618 1 6.44
CHEMBL267839 1 6.37
CHEMBL231763 1 6.29
CHEMBL394876 1 6.07
CHEMBL233807 1 5.96
CHEMBL231764 1 5.75
CHEMBL231765 1 5.47
CHEMBL231991 1 5.38
CHEMBL233370 1 5.32
CHEMBL231985 1 5.24
CHEMBL231986 1 5.06
CHEMBL244418 1 5.05
CHEMBL434585 1 5.01
CHEMBL413487 1 4.92
CHEMBL231987 1 4.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL66654 IC50 = 0.2 nM 9.70
CHEMBL232188 IC50 = 0.8 nM 9.10
CHEMBL396135 IC50 = 1.4 nM 8.85
CHEMBL232189 IC50 = 1.6 nM 8.80
CHEMBL231790 IC50 = 2.0 nM 8.70
CHEMBL231788 IC50 = 2.0 nM 8.70
CHEMBL233417 IC50 = 2.4 nM 8.62
CHEMBL244796 IC50 = 7.7 nM 8.11
CHEMBL396177 IC50 = 13.0 nM 7.89
CHEMBL233358 IC50 = 17.0 nM 7.77
CHEMBL233418 IC50 = 23.0 nM 7.64
CHEMBL233615 IC50 = 72.0 nM 7.14
CHEMBL396415 IC50 = 75.0 nM 7.12
CHEMBL233616 IC50 = 82.0 nM 7.09
CHEMBL233617 IC50 = 310.0 nM 6.51
CHEMBL233618 IC50 = 360.0 nM 6.44
CHEMBL267839 IC50 = 430.0 nM 6.37
CHEMBL231763 IC50 = 510.0 nM 6.29
CHEMBL394876 IC50 = 860.0 nM 6.07
CHEMBL233807 IC50 = 1090.0 nM 5.96
CHEMBL231764 IC50 = 1800.0 nM 5.75
CHEMBL231765 IC50 = 3400.0 nM 5.47
CHEMBL231991 IC50 = 4200.0 nM 5.38
CHEMBL233370 IC50 = 4760.0 nM 5.32
CHEMBL231985 IC50 = 5800.0 nM 5.24
CHEMBL231986 IC50 = 8700.0 nM 5.06
CHEMBL244418 IC50 = 9000.0 nM 5.05
CHEMBL434585 IC50 = 9800.0 nM 5.01
CHEMBL413487 IC50 = 12000.0 nM 4.92
CHEMBL231987 IC50 = 14000.0 nM 4.85
CHEMBL396134 IC50 = 16000.0 nM 4.80
CHEMBL231988 IC50 = 19000.0 nM 4.72
CHEMBL395899 IC50 > 10000.0 nM -
CHEMBL232184 IC50 > 10000.0 nM -
CHEMBL231989 IC50 > 10000.0 nM -
CHEMBL232187 IC50 > 10000.0 nM -