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Assay Detail

CHEMBL882884

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Functional
Effective agonist concentration for human PPAR gamma Gal4 construct in transactivation assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and biological activities of novel aryl indole-2-carboxylic acid analogs as PPARgamma partial agonists.
Dropinski JF, Akiyama T, Einstein M, Habulihaz B, Doebber T, Berger JP, Meinke PT, Shi GQ.
Bioorg Med Chem Lett (2005) 15 : 5035 -5038
PubMed 16153845 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 20 7.07 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL199244 1 8.70
CHEMBL370443 1 8.22
CHEMBL373237 1 7.89
CHEMBL121 ROSIGLITAZONE 4.0 1 7.66
CHEMBL426105 1 7.47
CHEMBL198266 1 7.47
CHEMBL370152 1 7.26
CHEMBL198091 1 7.04
CHEMBL198365 1 7.02
CHEMBL381865 1 6.97
CHEMBL198269 1 6.90
CHEMBL198207 1 6.87
CHEMBL426294 1 6.79
CHEMBL198623 1 6.75
CHEMBL372107 1 6.63
CHEMBL372091 1 6.52
CHEMBL198605 1 6.48
CHEMBL381889 1 6.39
CHEMBL197848 1 6.33
CHEMBL198493 1 6.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL199244 EC50 = 2.0 nM 8.70
CHEMBL370443 EC50 = 6.0 nM 8.22
CHEMBL373237 EC50 = 13.0 nM 7.89
CHEMBL121 ROSIGLITAZONE EC50 = 22.0 nM 7.66
CHEMBL426105 EC50 = 34.0 nM 7.47
CHEMBL198266 EC50 = 34.0 nM 7.47
CHEMBL370152 EC50 = 55.0 nM 7.26
CHEMBL198091 EC50 = 91.0 nM 7.04
CHEMBL198365 EC50 = 95.0 nM 7.02
CHEMBL381865 EC50 = 106.0 nM 6.97
CHEMBL198269 EC50 = 126.0 nM 6.90
CHEMBL198207 EC50 = 136.0 nM 6.87
CHEMBL426294 EC50 = 161.0 nM 6.79
CHEMBL198623 EC50 = 176.0 nM 6.75
CHEMBL372107 EC50 = 233.0 nM 6.63
CHEMBL372091 EC50 = 299.0 nM 6.52
CHEMBL198605 EC50 = 334.0 nM 6.48
CHEMBL381889 EC50 = 411.0 nM 6.39
CHEMBL197848 EC50 = 464.0 nM 6.33
CHEMBL198493 EC50 = 755.0 nM 6.12