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Assay Detail

CHEMBL980783

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

Functional
Agonist activity at human PPARgamma receptor expressed in african green monkey COS cells after 48 hrs by GAL4 transactivation assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Peroxisome proliferator-activated receptor gamma (CHEMBL235)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Highly functionalized 7-azaindoles as selective PPAR gamma modulators.
Debenham SD, Chan A, Lau FW, Liu W, Wood HB, Lemme K, Colwell L, Habulihaz B, Akiyama TE, Einstein M, Doebber TW, Sharma N, Wang CF, Wu M, Berger JP, Meinke PT.
Bioorg Med Chem Lett (2008) 18 : 4798 -4801
PubMed 18701276 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 19 8.03 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL459466 1 9.00
CHEMBL460072 1 9.00
CHEMBL462378 1 9.00
CHEMBL452051 1 9.00
CHEMBL460073 1 8.70
CHEMBL509236 1 8.70
CHEMBL455127 1 8.52
CHEMBL507477 1 8.52
CHEMBL518499 1 8.40
CHEMBL461378 1 8.40
CHEMBL461944 1 8.40
CHEMBL510180 1 8.05
CHEMBL517436 1 7.64
CHEMBL455126 1 7.57
CHEMBL452054 1 7.44
CHEMBL461379 1 7.03
CHEMBL455130 1 6.85
CHEMBL509369 1 6.81
CHEMBL452299 1 5.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL459466 EC50 = 1.0 nM 9.00
CHEMBL460072 EC50 = 1.0 nM 9.00
CHEMBL462378 EC50 = 1.0 nM 9.00
CHEMBL452051 EC50 = 1.0 nM 9.00
CHEMBL460073 EC50 = 2.0 nM 8.70
CHEMBL509236 EC50 = 2.0 nM 8.70
CHEMBL455127 EC50 = 3.0 nM 8.52
CHEMBL507477 EC50 = 3.0 nM 8.52
CHEMBL518499 EC50 = 4.0 nM 8.40
CHEMBL461378 EC50 = 4.0 nM 8.40
CHEMBL461944 EC50 = 4.0 nM 8.40
CHEMBL510180 EC50 = 9.0 nM 8.05
CHEMBL517436 EC50 = 23.0 nM 7.64
CHEMBL455126 EC50 = 27.0 nM 7.57
CHEMBL452054 EC50 = 36.0 nM 7.44
CHEMBL461379 EC50 = 94.0 nM 7.03
CHEMBL455130 EC50 = 140.0 nM 6.85
CHEMBL509369 EC50 = 156.0 nM 6.81
CHEMBL452299 EC50 = 2926.0 nM 5.53