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Assay Detail

CHEMBL5044759

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

Binding
Agonist activity at PPARdelta (unknown origin)
47
Total Activities
47
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

Peroxisome proliferator-activated receptor delta (CHEMBL3979)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, Synthesis, and Biological Evaluation of Triazolone Derivatives as Potent PPARα/δ Dual Agonists for the Treatment of Nonalcoholic Steatohepatitis.
Feng Z, Xiang J, Liu H, Li J, Xu X, Sun G, Zheng R, Zhang S, Liu J, Yang S, Xu Q, Wen X, Yuan H, Sun H, Dai L.
J Med Chem (2022) 65 : 2571 -2592
PubMed 35060744 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 47 6.96 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38943 GW501516 2.0 1 9.30
CHEMBL5081996 1 8.85
CHEMBL5078556 1 8.77
CHEMBL5094105 1 8.25
CHEMBL5084377 1 8.08
CHEMBL5075951 1 7.83
CHEMBL5081988 1 7.67
CHEMBL4470753 1 7.62
CHEMBL5085927 1 7.54
CHEMBL5085903 1 7.42
CHEMBL5089733 1 7.41
CHEMBL5077367 1 7.38
CHEMBL5089010 1 7.38
CHEMBL5085496 1 7.33
CHEMBL5082783 1 7.25
CHEMBL5072619 1 7.17
CHEMBL5070178 1 7.09
CHEMBL5076090 1 7.06
CHEMBL5084763 1 7.04
CHEMBL5077842 1 6.91
CHEMBL5090142 1 6.88
CHEMBL5087638 1 6.87
CHEMBL5075917 1 6.76
CHEMBL5081430 1 6.74
CHEMBL5094903 1 6.67
CHEMBL5082865 1 6.65
CHEMBL5079871 1 6.64
CHEMBL5084019 1 6.61
CHEMBL5092961 1 6.56
CHEMBL5086358 1 6.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38943 GW501516 EC50 = 0.5 nM 9.30
CHEMBL5081996 EC50 = 1.4 nM 8.85
CHEMBL5078556 EC50 = 1.7 nM 8.77
CHEMBL5094105 EC50 = 5.6 nM 8.25
CHEMBL5084377 EC50 = 8.4 nM 8.08
CHEMBL5075951 EC50 = 14.7 nM 7.83
CHEMBL5081988 EC50 = 21.6 nM 7.67
CHEMBL4470753 EC50 = 24.2 nM 7.62
CHEMBL5085927 EC50 = 28.5 nM 7.54
CHEMBL5085903 EC50 = 38.1 nM 7.42
CHEMBL5089733 EC50 = 38.6 nM 7.41
CHEMBL5077367 EC50 = 42.0 nM 7.38
CHEMBL5089010 EC50 = 42.1 nM 7.38
CHEMBL5085496 EC50 = 46.6 nM 7.33
CHEMBL5082783 EC50 = 55.6 nM 7.25
CHEMBL5072619 EC50 = 66.9 nM 7.17
CHEMBL5070178 EC50 = 81.3 nM 7.09
CHEMBL5076090 EC50 = 87.1 nM 7.06
CHEMBL5084763 EC50 = 90.7 nM 7.04
CHEMBL5077842 EC50 = 123.8 nM 6.91
CHEMBL5090142 EC50 = 132.0 nM 6.88
CHEMBL5087638 EC50 = 134.6 nM 6.87
CHEMBL5075917 EC50 = 175.0 nM 6.76
CHEMBL5081430 EC50 = 181.3 nM 6.74
CHEMBL5094903 EC50 = 211.6 nM 6.67
CHEMBL5082865 EC50 = 225.1 nM 6.65
CHEMBL5079871 EC50 = 229.3 nM 6.64
CHEMBL5084019 EC50 = 247.7 nM 6.61
CHEMBL5092961 EC50 = 278.0 nM 6.56
CHEMBL5086358 EC50 = 278.1 nM 6.56
CHEMBL5087115 EC50 = 323.3 nM 6.49
CHEMBL5089520 EC50 = 388.8 nM 6.41
CHEMBL5084826 EC50 = 480.7 nM 6.32
CHEMBL5076583 EC50 = 585.7 nM 6.23
CHEMBL5076063 EC50 = 619.6 nM 6.21
CHEMBL5087157 EC50 = 647.0 nM 6.19
CHEMBL5075465 EC50 = 663.7 nM 6.18
CHEMBL3707395 ELAFIBRANOR EC50 = 842.9 nM 6.07
CHEMBL5088968 EC50 = 914.1 nM 6.04
CHEMBL5087349 EC50 = 1367.0 nM 5.86
CHEMBL5088489 EC50 = 1519.0 nM 5.82
CHEMBL5091032 EC50 = 1675.0 nM 5.78
CHEMBL4091374 LANIFIBRANOR EC50 = 2962.0 nM 5.53
CHEMBL5084631 EC50 > 5000.0 nM -
CHEMBL5073521 EC50 > 5000.0 nM -
CHEMBL5080431 EC50 > 5000.0 nM -
CHEMBL5077836 EC50 > 5000.0 nM -