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Assay Detail

CHEMBL762151

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

Binding
Inhibition by 50% of in vitro binding to Peroxisome proliferator activated receptor gamma
ChEMBL ↗
71
Total Activities
65
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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
Ki 71 7.30 9.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL446629 — — 1 9.16
CHEMBL149876 — — 1 9.11
CHEMBL147095 — — 1 9.07
CHEMBL147090 — — 1 9.06
CHEMBL343210 — — 1 9.05
CHEMBL146301 — — 1 9.01
CHEMBL358379 — — 1 8.96
CHEMBL356382 — — 1 8.96
CHEMBL107367 FARGLITAZAR 2.0 1 8.94
CHEMBL147935 — — 1 8.90
CHEMBL148950 — — 1 8.85
CHEMBL147384 — — 1 8.80
CHEMBL148797 — — 1 8.75
CHEMBL148459 — — 1 8.72
CHEMBL149647 — — 1 8.70
CHEMBL358325 — — 1 8.66
CHEMBL359285 — — 1 8.59
CHEMBL149835 — — 1 8.59
CHEMBL146650 — — 1 8.58
CHEMBL146231 — — 1 8.36
CHEMBL342292 — — 1 8.32
CHEMBL149605 — — 2 8.03
CHEMBL145941 — — 2 7.94
CHEMBL356707 — — 1 7.91
CHEMBL343459 — — 2 7.73
CHEMBL149677 — — 2 7.71
CHEMBL146806 — — 1 7.56
CHEMBL147599 — — 2 7.41
CHEMBL148664 — — 1 7.14
CHEMBL148341 — — 1 7.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL446629 — Ki = 0.6918 nM 9.16
CHEMBL149876 — Ki = 0.7762 nM 9.11
CHEMBL147095 — Ki = 0.8511 nM 9.07
CHEMBL147090 — Ki = 0.871 nM 9.06
CHEMBL343210 — Ki = 0.8913 nM 9.05
CHEMBL146301 — Ki = 0.9772 nM 9.01
CHEMBL356382 — Ki = 1.096 nM 8.96
CHEMBL358379 — Ki = 1.096 nM 8.96
CHEMBL107367 FARGLITAZAR Ki = 1.148 nM 8.94
CHEMBL147935 — Ki = 1.259 nM 8.90
CHEMBL148950 — Ki = 1.413 nM 8.85
CHEMBL147384 — Ki = 1.585 nM 8.80
CHEMBL148797 — Ki = 1.778 nM 8.75
CHEMBL148459 — Ki = 1.905 nM 8.72
CHEMBL149647 — Ki = 1.995 nM 8.70
CHEMBL358325 — Ki = 2.188 nM 8.66
CHEMBL149835 — Ki = 2.57 nM 8.59
CHEMBL359285 — Ki = 2.57 nM 8.59
CHEMBL146650 — Ki = 2.63 nM 8.58
CHEMBL146231 — Ki = 4.365 nM 8.36
CHEMBL342292 — Ki = 4.786 nM 8.32
CHEMBL149605 — Ki = 9.333 nM 8.03
CHEMBL145941 — Ki = 11.48 nM 7.94
CHEMBL356707 — Ki = 12.3 nM 7.91
CHEMBL343459 — Ki = 18.62 nM 7.73
CHEMBL149677 — Ki = 19.5 nM 7.71
CHEMBL146806 — Ki = 27.54 nM 7.56
CHEMBL147599 — Ki = 38.9 nM 7.41
CHEMBL148664 — Ki = 72.44 nM 7.14
CHEMBL149677 — Ki = 72.44 nM 7.14
CHEMBL148341 — Ki = 91.2 nM 7.04
CHEMBL149782 — Ki = 93.33 nM 7.03
CHEMBL147492 — Ki = 104.71 nM 6.98
CHEMBL146320 — Ki = 107.15 nM 6.97
CHEMBL343260 — Ki = 112.2 nM 6.95
CHEMBL146029 — Ki = 117.49 nM 6.93
CHEMBL146864 — Ki = 120.23 nM 6.92
CHEMBL147323 — Ki = 128.82 nM 6.89
CHEMBL265551 — Ki = 131.83 nM 6.88
CHEMBL343459 — Ki = 141.25 nM 6.85
CHEMBL149605 — Ki = 144.54 nM 6.84
CHEMBL146369 — Ki = 144.54 nM 6.84
CHEMBL356773 — Ki = 158.49 nM 6.80
CHEMBL146341 — Ki = 162.18 nM 6.79
CHEMBL149715 — Ki = 169.82 nM 6.77
CHEMBL145941 — Ki = 199.53 nM 6.70
CHEMBL148540 — Ki = 234.42 nM 6.63
CHEMBL146133 — Ki = 269.15 nM 6.57
CHEMBL342514 — Ki = 346.74 nM 6.46
CHEMBL147480 — Ki = 354.81 nM 6.45