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Assay Detail

CHEMBL888369

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Functional
Agonist activity at human recombinant PPARgamma by GAL4 transactivation assay
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Peroxisome proliferator-activated receptor gamma (CHEMBL235)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of highly potent and selective human peroxisome proliferator-activated receptor alpha agonists.
Yamazaki Y, Abe K, Toma T, Nishikawa M, Ozawa H, Okuda A, Araki T, Oda S, Inoue K, Shibuya K, Staels B, Fruchart JC.
Bioorg Med Chem Lett (2007) 17 : 4689 -4693
PubMed 17553678 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 36 6.01 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL395924 1 7.00
CHEMBL427701 1 6.89
CHEMBL246070 1 6.68
CHEMBL245464 1 6.40
CHEMBL398118 1 6.28
CHEMBL246281 1 6.12
CHEMBL394296 1 6.06
CHEMBL391622 1 6.04
CHEMBL247748 1 6.03
CHEMBL398117 1 6.00
CHEMBL248117 1 5.96
CHEMBL248527 1 5.96
CHEMBL247951 PEMAFIBRATE 4.0 1 5.96
CHEMBL247749 1 5.92
CHEMBL248324 1 5.92
CHEMBL247952 1 5.88
CHEMBL246510 1 5.85
CHEMBL248526 1 5.82
CHEMBL428574 1 5.80
CHEMBL248326 1 5.75
CHEMBL429824 1 5.75
CHEMBL391620 1 5.75
CHEMBL392810 1 5.70
CHEMBL247919 1 5.68
CHEMBL246282 1 5.68
CHEMBL248118 1 5.30
CHEMBL245465 1 -
CHEMBL245664 1 -
CHEMBL245865 1 -
CHEMBL245866 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL395924 EC50 = 100.0 nM 7.00
CHEMBL427701 EC50 = 130.0 nM 6.89
CHEMBL246070 EC50 = 210.0 nM 6.68
CHEMBL245464 EC50 = 400.0 nM 6.40
CHEMBL398118 EC50 = 530.0 nM 6.28
CHEMBL246281 EC50 = 750.0 nM 6.12
CHEMBL394296 EC50 = 870.0 nM 6.06
CHEMBL391622 EC50 = 910.0 nM 6.04
CHEMBL247748 EC50 = 940.0 nM 6.03
CHEMBL398117 EC50 = 1000.0 nM 6.00
CHEMBL248117 EC50 = 1100.0 nM 5.96
CHEMBL247951 PEMAFIBRATE EC50 = 1100.0 nM 5.96
CHEMBL248527 EC50 = 1100.0 nM 5.96
CHEMBL247749 EC50 = 1190.0 nM 5.92
CHEMBL248324 EC50 = 1200.0 nM 5.92
CHEMBL247952 EC50 = 1310.0 nM 5.88
CHEMBL246510 EC50 = 1400.0 nM 5.85
CHEMBL248526 EC50 = 1500.0 nM 5.82
CHEMBL428574 EC50 = 1600.0 nM 5.80
CHEMBL429824 EC50 = 1800.0 nM 5.75
CHEMBL391620 EC50 = 1800.0 nM 5.75
CHEMBL248326 EC50 = 1800.0 nM 5.75
CHEMBL392810 EC50 = 2000.0 nM 5.70
CHEMBL247919 EC50 = 2100.0 nM 5.68
CHEMBL246282 EC50 = 2100.0 nM 5.68
CHEMBL248118 EC50 = 5000.0 nM 5.30
CHEMBL247917 EC50 - -
CHEMBL247918 EC50 - -
CHEMBL248119 EC50 - -
CHEMBL248325 EC50 > 10000.0 nM -
CHEMBL392811 EC50 > 10000.0 nM -
CHEMBL246069 EC50 > 10000.0 nM -
CHEMBL245866 EC50 > 10000.0 nM -
CHEMBL245865 EC50 > 10000.0 nM -
CHEMBL245664 EC50 > 10000.0 nM -
CHEMBL245465 EC50 > 10000.0 nM -