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Assay Detail

CHEMBL5156324

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Binding
Agonist activity at human PPARdelta measured by dual luciferase reporter gene assay
17
Total Activities
17
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

Discovery of new and highly effective quadruple FFA1 and PPARα/γ/δ agonists as potential anti-fatty liver agents.
Zhou Z, Ren Q, Jiao S, Cai Z, Geng X, Deng L, Wang B, Hu L, Zhang L, Yang Y, Li Z.
Eur J Med Chem (2022) 229 : 114061 -114061
PubMed 34954593 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 17 5.35 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38508 1 7.89
CHEMBL5197077 1 5.55
CHEMBL5171660 1 5.35
CHEMBL5200141 1 5.32
CHEMBL5201581 1 5.29
CHEMBL5196235 1 5.24
CHEMBL5195742 1 5.19
CHEMBL5184567 1 5.14
CHEMBL5171128 1 5.11
CHEMBL5169664 1 5.08
CHEMBL5200259 1 5.06
CHEMBL5179638 1 4.99
CHEMBL5197145 1 4.97
CHEMBL5208754 1 4.68
CHEMBL1829174 FASIGLIFAM 3.0 1 -
CHEMBL121 ROSIGLITAZONE 4.0 1 -
CHEMBL21241 GW7647 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38508 EC50 = 13.0 nM 7.89
CHEMBL5197077 EC50 = 2800.0 nM 5.55
CHEMBL5171660 EC50 = 4500.0 nM 5.35
CHEMBL5200141 EC50 = 4800.0 nM 5.32
CHEMBL5201581 EC50 = 5160.0 nM 5.29
CHEMBL5196235 EC50 = 5700.0 nM 5.24
CHEMBL5195742 EC50 = 6500.0 nM 5.19
CHEMBL5184567 EC50 = 7200.0 nM 5.14
CHEMBL5171128 EC50 = 7800.0 nM 5.11
CHEMBL5169664 EC50 = 8370.0 nM 5.08
CHEMBL5200259 EC50 = 8750.0 nM 5.06
CHEMBL5179638 EC50 = 10200.0 nM 4.99
CHEMBL5197145 EC50 = 10800.0 nM 4.97
CHEMBL5208754 EC50 = 20800.0 nM 4.68
CHEMBL1829174 FASIGLIFAM EC50 - -
CHEMBL121 ROSIGLITAZONE EC50 - -
CHEMBL21241 GW7647 EC50 - -