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Assay Detail

CHEMBL758987

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

Functional
Activation of peroxisome proliferator activated receptor gamma measured by induction of 50% of maximum alkaline phosphatase activity, transfection assay in CV-1 cells
32
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type CV-1
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 1. Discovery of a novel series of potent antihyperglycemic and antihyperlipidemic agents.
Henke BR, Blanchard SG, Brackeen MF, Brown KK, Cobb JE, Collins JL, Harrington WW, Hashim MA, Hull-Ryde EA, Kaldor I, Kliewer SA, Lake DH, Leesnitzer LM, Lehmann JM, Lenhard JM, Orband-Miller LA, Miller JF, Mook RA, Noble SA, Oliver W, Parks DJ, Plunket KD, Szewczyk JR, Willson TM.
J Med Chem (1998) 41 : 5020 -5036
PubMed 9836620 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 32 6.76 9.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL107367 FARGLITAZAR 2.0 1 9.47
CHEMBL423026 2 8.58
CHEMBL59132 1 8.50
CHEMBL358137 1 8.30
CHEMBL148301 1 8.04
CHEMBL434063 3 8.04
CHEMBL17805 BRL-48482 1 7.95
CHEMBL146822 1 7.54
CHEMBL346219 1 7.30
CHEMBL121 ROSIGLITAZONE 4.0 1 7.05
CHEMBL147826 1 6.97
CHEMBL146614 1 6.78
CHEMBL356350 2 6.64
CHEMBL343469 1 6.35
CHEMBL148060 1 6.31
CHEMBL146201 1 6.31
CHEMBL408 TROGLITAZONE 4.0 1 6.27
CHEMBL595 PIOGLITAZONE 4.0 1 6.23
CHEMBL357479 1 6.21
CHEMBL144877 1 6.16
CHEMBL145829 1 6.07
CHEMBL147694 1 6.03
CHEMBL146322 1 5.86
CHEMBL146123 1 5.74
CHEMBL147608 1 5.60
CHEMBL346415 1 4.99
CHEMBL359377 1 4.78
CHEMBL7002 CIGLITAZONE 2.0 1 4.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL107367 FARGLITAZAR EC50 = 0.3388 nM 9.47
CHEMBL423026 EC50 = 2.63 nM 8.58
CHEMBL423026 EC50 = 2.63 nM 8.58
CHEMBL59132 EC50 = 3.162 nM 8.50
CHEMBL358137 EC50 = 5.012 nM 8.30
CHEMBL434063 EC50 = 9.12 nM 8.04
CHEMBL434063 EC50 = 9.12 nM 8.04
CHEMBL148301 EC50 = 9.12 nM 8.04
CHEMBL17805 BRL-48482 EC50 = 11.22 nM 7.95
CHEMBL146822 EC50 = 28.84 nM 7.54
CHEMBL346219 EC50 = 50.12 nM 7.30
CHEMBL121 ROSIGLITAZONE EC50 = 89.13 nM 7.05
CHEMBL147826 EC50 = 107.15 nM 6.97
CHEMBL146614 EC50 = 165.96 nM 6.78
CHEMBL356350 EC50 = 229.09 nM 6.64
CHEMBL434063 EC50 = 389.05 nM 6.41
CHEMBL343469 EC50 = 446.68 nM 6.35
CHEMBL148060 EC50 = 489.78 nM 6.31
CHEMBL146201 EC50 = 489.78 nM 6.31
CHEMBL408 TROGLITAZONE EC50 = 537.03 nM 6.27
CHEMBL595 PIOGLITAZONE EC50 = 588.84 nM 6.23
CHEMBL357479 EC50 = 616.6 nM 6.21
CHEMBL144877 EC50 = 691.83 nM 6.16
CHEMBL145829 EC50 = 851.14 nM 6.07
CHEMBL147694 EC50 = 933.25 nM 6.03
CHEMBL146322 EC50 = 1380.38 nM 5.86
CHEMBL146123 EC50 = 1819.7 nM 5.74
CHEMBL147608 EC50 = 2511.89 nM 5.60
CHEMBL346415 EC50 = 10232.93 nM 4.99
CHEMBL359377 EC50 = 16595.87 nM 4.78
CHEMBL356350 EC50 = 21877.62 nM 4.66
CHEMBL7002 CIGLITAZONE EC50 = 22908.68 nM 4.64