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Assay Detail

CHEMBL759143

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Functional
Tested functionally in vitro for inducing 50% of the maximum alkaline phosphate activity (Transactivation) against Peroxisome proliferator activated receptor gamma
29
Total Activities
29
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. 2. Structure-activity relationship and optimization of the phenyl alkyl ether moiety.
Collins JL, Blanchard SG, Boswell GE, Charifson PS, Cobb JE, Henke BR, Hull-Ryde EA, Kazmierski WM, Lake DH, Leesnitzer LM, Lehmann J, Lenhard JM, Orband-Miller LA, Gray-Nunez Y, Parks DJ, Plunkett KD, Tong WQ.
J Med Chem (1998) 41 : 5037 -5054
PubMed 9836621 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 29 7.93 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL358379 1 10.00
CHEMBL147384 1 9.90
CHEMBL147095 1 9.61
CHEMBL107367 FARGLITAZAR 2.0 1 9.47
CHEMBL356382 1 9.22
CHEMBL148459 1 8.98
CHEMBL148797 1 8.97
CHEMBL358325 1 8.89
CHEMBL343210 1 8.82
CHEMBL149876 1 8.74
CHEMBL148950 1 8.74
CHEMBL147090 1 8.68
CHEMBL146301 1 8.62
CHEMBL147935 1 8.43
CHEMBL446629 1 8.03
CHEMBL342292 1 7.91
CHEMBL146650 1 7.63
CHEMBL359285 1 7.51
CHEMBL149715 1 7.29
CHEMBL149647 1 7.09
CHEMBL149605 1 6.98
CHEMBL146231 1 6.93
CHEMBL147492 1 6.62
CHEMBL149677 1 6.57
CHEMBL343459 1 6.49
CHEMBL149835 1 6.42
CHEMBL147599 1 5.96
CHEMBL146806 1 5.91
CHEMBL356707 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL358379 EC50 = 0.1 nM 10.00
CHEMBL147384 EC50 = 0.1259 nM 9.90
CHEMBL147095 EC50 = 0.2455 nM 9.61
CHEMBL107367 FARGLITAZAR EC50 = 0.3388 nM 9.47
CHEMBL356382 EC50 = 0.6026 nM 9.22
CHEMBL148459 EC50 = 1.047 nM 8.98
CHEMBL148797 EC50 = 1.072 nM 8.97
CHEMBL358325 EC50 = 1.288 nM 8.89
CHEMBL343210 EC50 = 1.514 nM 8.82
CHEMBL149876 EC50 = 1.82 nM 8.74
CHEMBL148950 EC50 = 1.82 nM 8.74
CHEMBL147090 EC50 = 2.089 nM 8.68
CHEMBL146301 EC50 = 2.399 nM 8.62
CHEMBL147935 EC50 = 3.715 nM 8.43
CHEMBL446629 EC50 = 9.333 nM 8.03
CHEMBL342292 EC50 = 12.3 nM 7.91
CHEMBL146650 EC50 = 23.44 nM 7.63
CHEMBL359285 EC50 = 30.9 nM 7.51
CHEMBL149715 EC50 = 51.29 nM 7.29
CHEMBL149647 EC50 = 81.28 nM 7.09
CHEMBL149605 EC50 = 104.71 nM 6.98
CHEMBL146231 EC50 = 117.49 nM 6.93
CHEMBL147492 EC50 = 239.88 nM 6.62
CHEMBL149677 EC50 = 269.15 nM 6.57
CHEMBL343459 EC50 = 323.59 nM 6.49
CHEMBL149835 EC50 = 380.19 nM 6.42
CHEMBL147599 EC50 = 1096.48 nM 5.96
CHEMBL146806 EC50 = 1230.27 nM 5.91
CHEMBL356707 EC50 = 3019.95 nM 5.52