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Assay Detail

CHEMBL857876

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

Binding
Binding affinity for human Platelet Thromboxane A2 / Prostaglandin (TP), by radioligand competition binding assays using [3H]-SQ 29548 as radioligand
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Thromboxane A2 receptor (CHEMBL2069)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Iodinated analogs of trimetoquinol as highly potent and selective beta 2-adrenoceptor ligands.
De Los Angeles JE, Nikulin VI, Shams G, Konkar AA, Mehta R, Feller DR, Miller DD.
J Med Chem (1996) 39 : 3701 -3711
PubMed 8809159 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 5.83 7.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL308351 1 7.33
CHEMBL174984 TRETOQUINOL 2.0 1 6.79
CHEMBL122757 1 6.75
CHEMBL123596 1 6.73
CHEMBL122992 1 6.45
CHEMBL122990 1 6.00
CHEMBL332964 1 5.83
CHEMBL121704 1 5.27
CHEMBL121964 1 4.72
CHEMBL120278 1 4.22
CHEMBL333438 1 4.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL308351 Ki = 46.77 nM 7.33
CHEMBL174984 TRETOQUINOL Ki = 162.18 nM 6.79
CHEMBL122757 Ki = 177.83 nM 6.75
CHEMBL123596 Ki = 186.21 nM 6.73
CHEMBL122992 Ki = 354.81 nM 6.45
CHEMBL122990 Ki = 1000.0 nM 6.00
CHEMBL332964 Ki = 1479.11 nM 5.83
CHEMBL121704 Ki = 5370.32 nM 5.27
CHEMBL121964 Ki = 19054.61 nM 4.72
CHEMBL120278 Ki = 60255.96 nM 4.22
CHEMBL333438 Ki = 83176.38 nM 4.08