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Assay Detail

CHEMBL5113087

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Binding
Inverse agonist activity at GAL4-tagged human PPARdelta LBD expressed in CHO cells measured after 6 hrs by firefly luciferase reporter assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Peroxisome proliferator-activated receptor delta (CHEMBL3979)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and Structure-Based Design of Potent Covalent PPARγ Inverse-Agonists <b>BAY-4931</b> and <b>BAY-0069</b>.
Orsi DL, Pook E, Bräuer N, Friberg A, Lienau P, Lemke CT, Stellfeld T, Brüggemeier U, Pütter V, Meyer H, Baco M, Tang S, Cherniack AD, Westlake L, Bender SA, Kocak M, Strathdee CA, Meyerson M, Eis K, Goldstein JT.
J Med Chem (2022) 65 : 14843 -14863
PubMed 36270630 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.05 5.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5187164 1 5.05
CHEMBL5207130 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5187164 IC50 = 9000.0 nM 5.05
CHEMBL5207130 IC50 > 50000.0 nM -