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Assay Detail

CHEMBL854671

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

Functional
Agonist potency at PPARalpha in CV1 cells by cell based transient transfection assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CV-1
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Substituted 2-[(4-aminomethyl)phenoxy]-2-methylpropionic acid PPARalpha agonists. 1. Discovery of a novel series of potent HDLc raising agents.
Sierra ML, Beneton V, Boullay AB, Boyer T, Brewster AG, Donche F, Forest MC, Fouchet MH, Gellibert FJ, Grillot DA, Lambert MH, Laroze A, Le Grumelec C, Linget JM, Montana VG, Nguyen VL, Nicodème E, Patel V, Penfornis A, Pineau O, Pohin D, Potvain F, Poulain G, Ruault CB, Saunders M, Toum J, Xu HE, Xu RX, Pianetti PM.
J Med Chem (2007) 50 : 685 -695
PubMed 17243659 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 23 6.99 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL376641 1 8.40
CHEMBL219626 1 8.40
CHEMBL375760 1 8.40
CHEMBL219586 GW590735 2.0 1 8.40
CHEMBL221074 1 8.30
CHEMBL220281 1 8.00
CHEMBL218691 1 8.00
CHEMBL218637 1 7.52
CHEMBL219587 1 7.40
CHEMBL218094 1 7.16
CHEMBL221201 1 6.96
CHEMBL218784 1 6.92
CHEMBL218687 1 6.68
CHEMBL220926 1 6.62
CHEMBL375761 1 6.33
CHEMBL221146 1 5.88
CHEMBL38943 GW501516 2.0 1 5.72
CHEMBL218442 1 5.72
CHEMBL221755 1 5.70
CHEMBL221254 1 5.25
CHEMBL374355 1 5.02
CHEMBL220751 1 -
CHEMBL376050 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL376641 EC50 = 4.0 nM 8.40
CHEMBL219626 EC50 = 4.0 nM 8.40
CHEMBL375760 EC50 = 4.0 nM 8.40
CHEMBL219586 GW590735 EC50 = 4.0 nM 8.40
CHEMBL221074 EC50 = 5.0 nM 8.30
CHEMBL220281 EC50 = 10.0 nM 8.00
CHEMBL218691 EC50 = 10.0 nM 8.00
CHEMBL218637 EC50 = 30.0 nM 7.52
CHEMBL219587 EC50 = 40.0 nM 7.40
CHEMBL218094 EC50 = 70.0 nM 7.16
CHEMBL221201 EC50 = 110.0 nM 6.96
CHEMBL218784 EC50 = 120.0 nM 6.92
CHEMBL218687 EC50 = 210.0 nM 6.68
CHEMBL220926 EC50 = 240.0 nM 6.62
CHEMBL375761 EC50 = 465.0 nM 6.33
CHEMBL221146 EC50 = 1320.0 nM 5.88
CHEMBL38943 GW501516 EC50 = 1888.0 nM 5.72
CHEMBL218442 EC50 = 1890.0 nM 5.72
CHEMBL221755 EC50 = 2000.0 nM 5.70
CHEMBL221254 EC50 = 5640.0 nM 5.25
CHEMBL374355 EC50 = 9500.0 nM 5.02
CHEMBL220751 EC50 > 10000.0 nM -
CHEMBL376050 EC50 > 10000.0 nM -