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Assay Detail

CHEMBL880426

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

Binding
Inhibitory concentration against human peroxisome proliferator activated receptor gamma in SPA assay
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Synthesis and biological activities of novel aryl indole-2-carboxylic acid analogs as PPARgamma partial agonists.
Dropinski JF, Akiyama T, Einstein M, Habulihaz B, Doebber T, Berger JP, Meinke PT, Shi GQ.
Bioorg Med Chem Lett (2005) 15 : 5035 -5038
PubMed 16153845 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 7.33 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL199244 1 8.70
CHEMBL370443 1 8.30
CHEMBL198269 1 7.96
CHEMBL373237 1 7.92
CHEMBL370648 1 7.89
CHEMBL198207 1 7.77
CHEMBL198091 1 7.75
CHEMBL198266 1 7.75
CHEMBL372639 1 7.72
CHEMBL198623 1 7.68
CHEMBL370152 1 7.58
CHEMBL381865 1 7.57
CHEMBL197671 1 7.41
CHEMBL196428 1 7.31
CHEMBL372107 1 7.31
CHEMBL198365 1 7.24
CHEMBL197636 1 7.22
CHEMBL197848 1 7.12
CHEMBL426294 1 7.11
CHEMBL372780 1 7.08
CHEMBL372091 1 7.00
CHEMBL372850 1 6.99
CHEMBL198493 1 6.98
CHEMBL194740 1 6.97
CHEMBL198605 1 6.94
CHEMBL197637 1 6.92
CHEMBL197823 1 6.70
CHEMBL121 ROSIGLITAZONE 4.0 1 6.68
CHEMBL426105 1 6.60
CHEMBL381889 1 6.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL199244 IC50 = 2.0 nM 8.70
CHEMBL370443 IC50 = 5.0 nM 8.30
CHEMBL198269 IC50 = 11.0 nM 7.96
CHEMBL373237 IC50 = 12.0 nM 7.92
CHEMBL370648 IC50 = 13.0 nM 7.89
CHEMBL198207 IC50 = 17.0 nM 7.77
CHEMBL198091 IC50 = 18.0 nM 7.75
CHEMBL198266 IC50 = 18.0 nM 7.75
CHEMBL372639 IC50 = 19.0 nM 7.72
CHEMBL198623 IC50 = 21.0 nM 7.68
CHEMBL370152 IC50 = 26.0 nM 7.58
CHEMBL381865 IC50 = 27.0 nM 7.57
CHEMBL197671 IC50 = 39.0 nM 7.41
CHEMBL196428 IC50 = 49.0 nM 7.31
CHEMBL372107 IC50 = 49.0 nM 7.31
CHEMBL198365 IC50 = 58.0 nM 7.24
CHEMBL197636 IC50 = 60.0 nM 7.22
CHEMBL197848 IC50 = 75.0 nM 7.12
CHEMBL426294 IC50 = 78.0 nM 7.11
CHEMBL372780 IC50 = 83.0 nM 7.08
CHEMBL372091 IC50 = 100.0 nM 7.00
CHEMBL372850 IC50 = 102.0 nM 6.99
CHEMBL198493 IC50 = 104.0 nM 6.98
CHEMBL194740 IC50 = 107.0 nM 6.97
CHEMBL198605 IC50 = 115.0 nM 6.94
CHEMBL197637 IC50 = 120.0 nM 6.92
CHEMBL197823 IC50 = 202.0 nM 6.70
CHEMBL121 ROSIGLITAZONE IC50 = 210.0 nM 6.68
CHEMBL426105 IC50 = 251.0 nM 6.60
CHEMBL381889 IC50 = 298.0 nM 6.53
CHEMBL373048 IC50 = 318.0 nM 6.50