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Assay Detail

CHEMBL5251263

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Binding
Agonist activity at human TAS2R14 transfected in HEK293T cells assessed as IP1 accumulation measured after 150 mins by IP1 accumulation assay
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of 2-Aminopyrimidines as Potent Agonists for the Bitter Taste Receptor TAS2R14.
Waterloo L, Hübner H, Fierro F, Pfeiffer T, Brox R, Löber S, Weikert D, Niv MY, Gmeiner P.
J Med Chem (2023) 66 : 3499 -3521
PubMed 36847646 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 32 6.30 7.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5279691 1 7.14
CHEMBL5285591 1 7.01
CHEMBL5273955 1 6.82
CHEMBL5274304 1 6.80
CHEMBL5277615 1 6.77
CHEMBL5280542 1 6.75
CHEMBL3623735 1 6.72
CHEMBL5279381 1 6.72
CHEMBL3088246 1 6.64
CHEMBL5278834 1 6.52
CHEMBL5277281 1 6.52
CHEMBL5278171 1 6.48
CHEMBL5274470 1 6.44
CHEMBL5278477 1 6.42
CHEMBL5275001 1 6.41
CHEMBL5289590 1 6.38
CHEMBL23588 FLUFENAMIC ACID 2.0 1 6.37
CHEMBL5280688 1 6.27
CHEMBL5286379 1 6.19
CHEMBL5268924 1 6.19
CHEMBL5279341 1 6.17
CHEMBL5289980 1 6.12
CHEMBL5276181 1 6.03
CHEMBL22815 1 6.02
CHEMBL5265924 1 5.96
CHEMBL5268477 1 5.92
CHEMBL5280454 1 5.85
CHEMBL5274977 1 5.80
CHEMBL5285283 1 5.75
CHEMBL5288875 1 5.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5279691 EC50 = 72.0 nM 7.14
CHEMBL5285591 EC50 = 98.0 nM 7.01
CHEMBL5273955 EC50 = 150.0 nM 6.82
CHEMBL5274304 EC50 = 160.0 nM 6.80
CHEMBL5277615 EC50 = 170.0 nM 6.77
CHEMBL5280542 EC50 = 180.0 nM 6.75
CHEMBL3623735 EC50 = 190.0 nM 6.72
CHEMBL5279381 EC50 = 190.0 nM 6.72
CHEMBL3088246 EC50 = 230.0 nM 6.64
CHEMBL5278834 EC50 = 300.0 nM 6.52
CHEMBL5277281 EC50 = 300.0 nM 6.52
CHEMBL5278171 EC50 = 330.0 nM 6.48
CHEMBL5274470 EC50 = 360.0 nM 6.44
CHEMBL5278477 EC50 = 380.0 nM 6.42
CHEMBL5275001 EC50 = 390.0 nM 6.41
CHEMBL5289590 EC50 = 420.0 nM 6.38
CHEMBL23588 FLUFENAMIC ACID EC50 = 430.0 nM 6.37
CHEMBL5280688 EC50 = 540.0 nM 6.27
CHEMBL5286379 EC50 = 640.0 nM 6.19
CHEMBL5268924 EC50 = 640.0 nM 6.19
CHEMBL5279341 EC50 = 670.0 nM 6.17
CHEMBL5289980 EC50 = 750.0 nM 6.12
CHEMBL5276181 EC50 = 930.0 nM 6.03
CHEMBL22815 EC50 = 950.0 nM 6.02
CHEMBL5265924 EC50 = 1100.0 nM 5.96
CHEMBL5268477 EC50 = 1200.0 nM 5.92
CHEMBL5280454 EC50 = 1400.0 nM 5.85
CHEMBL5274977 EC50 = 1600.0 nM 5.80
CHEMBL5285283 EC50 = 1800.0 nM 5.75
CHEMBL5288875 EC50 = 2100.0 nM 5.68
CHEMBL5265867 EC50 = 3500.0 nM 5.46
CHEMBL5279932 EC50 = 6800.0 nM 5.17