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Assay Detail

CHEMBL759115

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

Binding
Binding affinity to human Peroxisome proliferator activated receptor gamma using scintillation proximity assay
16
Total Activities
15
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

Synthesis and biological activity of L-tyrosine-based PPARgamma agonists with reduced molecular weight.
Liu KG, Lambert MH, Ayscue AH, Henke BR, Leesnitzer LM, Oliver WR, Plunket KD, Xu HE, Sternbach DD, Willson TM.
Bioorg Med Chem Lett (2001) 11 : 3111 -3113
PubMed 11720854 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 6.81 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL107367 FARGLITAZAR 2.0 1 8.96
CHEMBL106666 GW7845 1 8.43
CHEMBL104850 2 8.16
CHEMBL321634 1 7.28
CHEMBL121 ROSIGLITAZONE 4.0 1 6.92
CHEMBL104246 1 6.80
CHEMBL104494 1 6.55
CHEMBL326668 1 6.44
CHEMBL431448 1 6.32
CHEMBL105088 1 6.21
CHEMBL595 PIOGLITAZONE 4.0 1 6.20
CHEMBL318104 1 6.07
CHEMBL107794 1 6.01
CHEMBL104458 1 5.68
CHEMBL107741 1 5.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL107367 FARGLITAZAR Ki = 1.1 nM 8.96
CHEMBL106666 GW7845 Ki = 3.7 nM 8.43
CHEMBL104850 Ki = 6.9 nM 8.16
CHEMBL104850 Ki = 51.0 nM 7.29
CHEMBL321634 Ki = 52.0 nM 7.28
CHEMBL121 ROSIGLITAZONE Ki = 120.0 nM 6.92
CHEMBL104246 Ki = 158.0 nM 6.80
CHEMBL104494 Ki = 280.0 nM 6.55
CHEMBL326668 Ki = 360.0 nM 6.44
CHEMBL431448 Ki = 480.0 nM 6.32
CHEMBL105088 Ki = 620.0 nM 6.21
CHEMBL595 PIOGLITAZONE Ki = 630.0 nM 6.20
CHEMBL318104 Ki = 850.0 nM 6.07
CHEMBL107794 Ki = 980.0 nM 6.01
CHEMBL104458 Ki = 2100.0 nM 5.68
CHEMBL107741 Ki = 2600.0 nM 5.58