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Assay Detail

CHEMBL3887148

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

Binding
Fluorescence Polarization Assays: In another embodiment, Fluorescence Polarization ("FP") based assays may be used to detect and monitor ligand binding. Fluorescence polarization is a versatile laboratory technique for measuring equilibrium binding, nucleic acid hybridization, and enzymatic activity. Fluorescence polarization assays are homogeneous in that they do not require a separation step such as centrifugation, filtration, chromatography, precipitation, or electrophoresis. These assays are done in real time, directly in solution and do not require an immobilized phase. Polarization values can be measured repeatedly and after the addition of reagents since measuring the polarization is rapid and does not destroy the sample. Generally, this technique can be used to measure polarization values of fluorophores from low picomolar to micromolar levels.
149
Total Activities
116
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Taste receptor type 2 member 14 (CHEMBL3309105)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
(2016)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 149 5.68 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3895068 1 7.85
CHEMBL3909546 1 7.44
CHEMBL3907785 1 7.27
CHEMBL3930803 1 7.08
CHEMBL3905445 1 7.04
CHEMBL3904387 1 6.96
CHEMBL3901989 1 6.73
CHEMBL3092287 2 6.70
CHEMBL3946036 1 6.62
CHEMBL1401915 1 6.58
CHEMBL3962122 1 6.54
CHEMBL3917592 1 6.48
CHEMBL3972175 1 6.47
CHEMBL3954153 2 6.46
CHEMBL1082389 1 6.41
CHEMBL3892321 2 6.39
CHEMBL3907807 2 6.37
CHEMBL3976457 1 6.34
CHEMBL3982886 1 6.30
CHEMBL3908011 1 6.30
CHEMBL3894540 1 6.23
CHEMBL3978302 1 6.17
CHEMBL1356858 1 6.17
CHEMBL3945665 1 6.15
CHEMBL3965603 1 6.15
CHEMBL1499181 1 6.14
CHEMBL1711155 1 6.12
CHEMBL3976205 1 6.08
CHEMBL3953366 1 6.07
CHEMBL3916808 2 6.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3895068 IC50 = 14.0 nM 7.85
CHEMBL3909546 IC50 = 36.0 nM 7.44
CHEMBL3907785 IC50 = 54.0 nM 7.27
CHEMBL3930803 IC50 = 83.0 nM 7.08
CHEMBL3905445 IC50 = 92.0 nM 7.04
CHEMBL3904387 IC50 = 109.0 nM 6.96
CHEMBL3901989 IC50 = 188.0 nM 6.73
CHEMBL3092287 IC50 = 200.0 nM 6.70
CHEMBL3092287 IC50 = 220.0 nM 6.66
CHEMBL3946036 IC50 = 240.0 nM 6.62
CHEMBL1401915 IC50 = 264.0 nM 6.58
CHEMBL3962122 IC50 = 292.0 nM 6.54
CHEMBL3917592 IC50 = 334.0 nM 6.48
CHEMBL3972175 IC50 = 342.0 nM 6.47
CHEMBL3954153 IC50 = 345.0 nM 6.46
CHEMBL3954153 IC50 = 345.0 nM 6.46
CHEMBL1082389 IC50 = 394.0 nM 6.41
CHEMBL3892321 IC50 = 406.0 nM 6.39
CHEMBL3892321 IC50 = 406.0 nM 6.39
CHEMBL3907807 IC50 = 429.0 nM 6.37
CHEMBL3907807 IC50 = 429.0 nM 6.37
CHEMBL3976457 IC50 = 459.0 nM 6.34
CHEMBL3982886 IC50 = 499.0 nM 6.30
CHEMBL3908011 IC50 = 499.0 nM 6.30
CHEMBL3894540 IC50 = 590.0 nM 6.23
CHEMBL1356858 IC50 = 672.0 nM 6.17
CHEMBL3978302 IC50 = 678.0 nM 6.17
CHEMBL3945665 IC50 = 706.0 nM 6.15
CHEMBL3965603 IC50 = 710.0 nM 6.15
CHEMBL1499181 IC50 = 721.0 nM 6.14
CHEMBL1711155 IC50 = 763.0 nM 6.12
CHEMBL3976205 IC50 = 842.0 nM 6.08
CHEMBL3953366 IC50 = 861.0 nM 6.07
CHEMBL1419634 IC50 = 935.0 nM 6.03
CHEMBL3916808 IC50 = 935.0 nM 6.03
CHEMBL3916808 IC50 = 935.0 nM 6.03
CHEMBL1419634 IC50 = 935.0 nM 6.03
CHEMBL1366449 IC50 = 1006.0 nM 6.00
CHEMBL3983085 IC50 = 1110.0 nM 5.96
CHEMBL3940903 IC50 = 1255.0 nM 5.90
CHEMBL3982834 IC50 = 1294.0 nM 5.89
CHEMBL3982834 IC50 = 1294.0 nM 5.89
CHEMBL3977716 IC50 = 1397.0 nM 5.86
CHEMBL3977716 IC50 = 1397.0 nM 5.86
CHEMBL3916784 IC50 = 1470.0 nM 5.83
CHEMBL3921682 IC50 = 1619.0 nM 5.79
CHEMBL3946037 IC50 = 1650.0 nM 5.78
CHEMBL3907800 IC50 = 1651.0 nM 5.78
CHEMBL3935097 IC50 = 1726.0 nM 5.76
CHEMBL3935097 IC50 = 1726.0 nM 5.76