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Assay Detail

CHEMBL758983

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

Functional
Ability to promote differentiation of C3H10T1/2 stem cells to adipocytes using lipogenesis assay mediated through activation of Peroxisome proliferator activated receptor gamma
17
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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 17 6.54 8.83

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL107367 FARGLITAZAR 2.0 1 8.83
CHEMBL423026 1 8.36
CHEMBL434063 2 7.74
CHEMBL146822 1 7.33
CHEMBL148301 1 6.44
CHEMBL147826 1 6.33
CHEMBL346219 1 6.30
CHEMBL148060 1 6.24
CHEMBL146614 1 6.02
CHEMBL147694 1 5.94
CHEMBL357479 1 5.94
CHEMBL145829 1 5.91
CHEMBL343469 1 5.88
CHEMBL146322 1 5.87
CHEMBL359377 1 5.82
CHEMBL146123 1 5.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL107367 FARGLITAZAR EC50 = 1.479 nM 8.83
CHEMBL423026 EC50 = 4.365 nM 8.36
CHEMBL434063 EC50 = 18.2 nM 7.74
CHEMBL146822 EC50 = 46.77 nM 7.33
CHEMBL148301 EC50 = 363.08 nM 6.44
CHEMBL147826 EC50 = 467.74 nM 6.33
CHEMBL346219 EC50 = 501.19 nM 6.30
CHEMBL148060 EC50 = 575.44 nM 6.24
CHEMBL146614 EC50 = 954.99 nM 6.02
CHEMBL147694 EC50 = 1148.15 nM 5.94
CHEMBL357479 EC50 = 1148.15 nM 5.94
CHEMBL145829 EC50 = 1230.27 nM 5.91
CHEMBL343469 EC50 = 1318.26 nM 5.88
CHEMBL146322 EC50 = 1348.96 nM 5.87
CHEMBL359377 EC50 = 1513.56 nM 5.82
CHEMBL146123 EC50 = 2187.76 nM 5.66
CHEMBL434063 EC50 < 1000.0 nM -