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Assay Detail

CHEMBL837872

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Functional
Effective concentration against hamster PPAR-alpha in Gal4 transactivation assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Peroxisome proliferator-activated receptor alpha (CHEMBL239)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel 2,3-dihydrobenzofuran-2-carboxylic acids: highly potent and subtype-selective PPARalpha agonists with potent hypolipidemic activity.
Shi GQ, Dropinski JF, Zhang Y, Santini C, Sahoo SP, Berger JP, Macnaul KL, Zhou G, Agrawal A, Alvaro R, Cai TQ, Hernandez M, Wright SD, Moller DE, Heck JV, Meinke PT.
J Med Chem (2005) 48 : 5589 -5599
PubMed 16107159 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 18 6.92 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL366145 1 7.82
CHEMBL190603 1 7.60
CHEMBL189110 1 7.58
CHEMBL425725 1 7.51
CHEMBL363780 1 7.47
CHEMBL370024 1 7.43
CHEMBL192500 1 7.00
CHEMBL190976 1 6.89
CHEMBL190334 1 6.60
CHEMBL190968 1 6.55
CHEMBL363006 1 6.43
CHEMBL192638 1 6.40
CHEMBL426269 1 6.38
CHEMBL192609 1 6.12
CHEMBL192582 1 6.07
CHEMBL193459 1 -
CHEMBL192774 1 -
CHEMBL363154 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL366145 EC50 = 15.0 nM 7.82
CHEMBL190603 EC50 = 25.0 nM 7.60
CHEMBL189110 EC50 = 26.0 nM 7.58
CHEMBL425725 EC50 = 31.0 nM 7.51
CHEMBL363780 EC50 = 34.0 nM 7.47
CHEMBL370024 EC50 = 37.0 nM 7.43
CHEMBL192500 EC50 = 100.0 nM 7.00
CHEMBL190976 EC50 = 130.0 nM 6.89
CHEMBL190334 EC50 = 250.0 nM 6.60
CHEMBL190968 EC50 = 280.0 nM 6.55
CHEMBL363006 EC50 = 370.0 nM 6.43
CHEMBL192638 EC50 = 402.0 nM 6.40
CHEMBL426269 EC50 = 420.0 nM 6.38
CHEMBL192609 EC50 = 750.0 nM 6.12
CHEMBL192582 EC50 = 860.0 nM 6.07
CHEMBL193459 EC50 > 3000.0 nM -
CHEMBL192774 EC50 > 3000.0 nM -
CHEMBL363154 EC50 > 3000.0 nM -