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Assay Detail

CHEMBL889272

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Functional
Agonist activity at human PPARdelta receptor by cell based transactivation assay
26
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Discovery of para-alkylthiophenoxyacetic acids as a novel series of potent and selective PPARdelta agonists.
Zhang R, Wang A, DeAngelis A, Pelton P, Xu J, Zhu P, Zhou L, Demarest K, Murray WV, Kuo GH.
Bioorg Med Chem Lett (2007) 17 : 3855 -3859
PubMed 17524639 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 26 8.01 10.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL390005 2 10.52
CHEMBL230063 1 10.22
CHEMBL230158 SELADELPAR 4.0 1 8.72
CHEMBL231223 1 8.68
CHEMBL230050 1 8.47
CHEMBL230269 1 8.41
CHEMBL389769 1 8.37
CHEMBL231528 1 8.34
CHEMBL395558 1 8.20
CHEMBL230177 1 8.16
CHEMBL230268 1 8.15
CHEMBL390004 1 8.13
CHEMBL390199 1 7.82
CHEMBL231531 1 7.77
CHEMBL230372 1 7.73
CHEMBL231527 1 7.62
CHEMBL230179 1 7.61
CHEMBL389768 1 7.60
CHEMBL230605 1 7.22
CHEMBL397449 1 7.21
CHEMBL231428 2 7.16
CHEMBL397970 1 7.10
CHEMBL397218 1 6.90
CHEMBL230287 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL390005 EC50 = 0.03 nM 10.52
CHEMBL230063 EC50 = 0.06 nM 10.22
CHEMBL230158 SELADELPAR EC50 = 1.9 nM 8.72
CHEMBL231223 EC50 = 2.1 nM 8.68
CHEMBL230050 EC50 = 3.4 nM 8.47
CHEMBL230269 EC50 = 3.9 nM 8.41
CHEMBL389769 EC50 = 4.3 nM 8.37
CHEMBL231528 EC50 = 4.6 nM 8.34
CHEMBL395558 EC50 = 6.3 nM 8.20
CHEMBL230177 EC50 = 6.9 nM 8.16
CHEMBL230268 EC50 = 7.0 nM 8.15
CHEMBL390004 EC50 = 7.4 nM 8.13
CHEMBL390199 EC50 = 15.2 nM 7.82
CHEMBL231531 EC50 = 17.0 nM 7.77
CHEMBL230372 EC50 = 18.8 nM 7.73
CHEMBL231527 EC50 = 23.9 nM 7.62
CHEMBL230179 EC50 = 24.3 nM 7.61
CHEMBL389768 EC50 = 25.0 nM 7.60
CHEMBL230605 EC50 = 60.0 nM 7.22
CHEMBL397449 EC50 = 62.1 nM 7.21
CHEMBL231428 EC50 = 70.0 nM 7.16
CHEMBL231428 EC50 = 70.0 nM 7.16
CHEMBL397970 EC50 = 79.0 nM 7.10
CHEMBL390005 EC50 = 79.0 nM 7.10
CHEMBL397218 EC50 = 126.0 nM 6.90
CHEMBL230287 EC50 > 3000.0 nM -