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Assay Detail

CHEMBL1001152

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

Binding
Displacement of radiolabeled ligand from human PPARalpha by competition-binding assay
35
Total Activities
35
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 alpha (CHEMBL239)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a novel class of PPARdelta partial agonists.
Shearer BG, Patel HS, Billin AN, Way JM, Winegar DA, Lambert MH, Xu RX, Leesnitzer LM, Merrihew RV, Huet S, Willson TM.
Bioorg Med Chem Lett (2008) 18 : 5018 -5022
PubMed 18722772 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 5.49 6.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL496744 1 6.10
CHEMBL498171 1 6.00
CHEMBL495904 1 6.00
CHEMBL525366 1 5.90
CHEMBL495905 1 5.90
CHEMBL522224 1 5.80
CHEMBL497991 1 5.80
CHEMBL522619 1 5.80
CHEMBL498172 1 5.70
CHEMBL38943 GW501516 2.0 1 5.70
CHEMBL522575 1 5.60
CHEMBL522577 1 5.50
CHEMBL497789 1 5.50
CHEMBL496733 1 5.50
CHEMBL496534 1 5.50
CHEMBL496743 1 5.50
CHEMBL496136 1 5.40
CHEMBL484266 1 5.40
CHEMBL496116 1 5.40
CHEMBL485088 1 5.30
CHEMBL484467 1 5.30
CHEMBL498401 1 5.30
CHEMBL498608 1 5.20
CHEMBL519345 1 5.20
CHEMBL496726 1 5.10
CHEMBL520827 1 5.10
CHEMBL525552 1 5.10
CHEMBL496933 1 5.00
CHEMBL524829 1 5.00
CHEMBL485087 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL496744 IC50 = 794.33 nM 6.10
CHEMBL498171 IC50 = 1000.0 nM 6.00
CHEMBL495904 IC50 = 1000.0 nM 6.00
CHEMBL525366 IC50 = 1258.93 nM 5.90
CHEMBL495905 IC50 = 1258.93 nM 5.90
CHEMBL522224 IC50 = 1584.89 nM 5.80
CHEMBL497991 IC50 = 1584.89 nM 5.80
CHEMBL522619 IC50 = 1584.89 nM 5.80
CHEMBL498172 IC50 = 1995.26 nM 5.70
CHEMBL38943 GW501516 IC50 = 1995.26 nM 5.70
CHEMBL522575 IC50 = 2511.89 nM 5.60
CHEMBL496534 IC50 = 3162.28 nM 5.50
CHEMBL496733 IC50 = 3162.28 nM 5.50
CHEMBL496743 IC50 = 3162.28 nM 5.50
CHEMBL497789 IC50 = 3162.28 nM 5.50
CHEMBL522577 IC50 = 3162.28 nM 5.50
CHEMBL496116 IC50 = 3981.07 nM 5.40
CHEMBL484266 IC50 = 3981.07 nM 5.40
CHEMBL496136 IC50 = 3981.07 nM 5.40
CHEMBL498401 IC50 = 5011.87 nM 5.30
CHEMBL484467 IC50 = 5011.87 nM 5.30
CHEMBL485088 IC50 = 5011.87 nM 5.30
CHEMBL498608 IC50 = 6309.57 nM 5.20
CHEMBL519345 IC50 = 6309.57 nM 5.20
CHEMBL525552 IC50 = 7943.28 nM 5.10
CHEMBL520827 IC50 = 7943.28 nM 5.10
CHEMBL496726 IC50 = 7943.28 nM 5.10
CHEMBL496933 IC50 = 10000.0 nM 5.00
CHEMBL524829 IC50 = 10000.0 nM 5.00
CHEMBL485087 IC50 = 10000.0 nM 5.00
CHEMBL523594 IC50 > 10000.0 nM -
CHEMBL484466 IC50 > 10000.0 nM -
CHEMBL484465 IC50 > 10000.0 nM -
CHEMBL495506 IC50 > 10000.0 nM -
CHEMBL523395 IC50 > 10000.0 nM -