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Assay Detail

CHEMBL1831674

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

Functional
Antagonist activity at mouse prostanoid TP receptor expressed in QBI-HEK 293A cells assessed as inhibition of 1-BOP-induced increase in inositol monophosphate after 1 hr by time-resolved fluorescence assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Thromboxane A2 receptor (CHEMBL1795181)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Cyclopentane-1,3-dione: a novel isostere for the carboxylic acid functional group. Application to the design of potent thromboxane (A2) receptor antagonists.
Ballatore C, Soper JH, Piscitelli F, James M, Huang L, Atasoylu O, Huryn DM, Trojanowski JQ, Lee VM, Brunden KR, Smith AB.
J Med Chem (2011) 54 : 6969 -6983
PubMed 21863799 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.04 8.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1829806 1 8.51
CHEMBL1829812 1 8.24
CHEMBL1829801 1 8.10
CHEMBL1829808 1 8.03
CHEMBL1829810 1 7.75
CHEMBL65121 1 7.57
CHEMBL1829805 1 7.28
CHEMBL1829802 1 7.04
CHEMBL1829811 1 6.59
CHEMBL1829809 1 6.33
CHEMBL1829804 1 5.91
CHEMBL1828642 1 5.79
CHEMBL1829807 1 5.75
CHEMBL1829813 1 5.60
CHEMBL1829803 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1829806 IC50 = 3.1 nM 8.51
CHEMBL1829812 IC50 = 5.8 nM 8.24
CHEMBL1829801 IC50 = 8.0 nM 8.10
CHEMBL1829808 IC50 = 9.4 nM 8.03
CHEMBL1829810 IC50 = 18.0 nM 7.75
CHEMBL65121 IC50 = 27.0 nM 7.57
CHEMBL1829805 IC50 = 52.0 nM 7.28
CHEMBL1829802 IC50 = 91.0 nM 7.04
CHEMBL1829811 IC50 = 259.0 nM 6.59
CHEMBL1829809 IC50 = 463.0 nM 6.33
CHEMBL1829804 IC50 = 1229.0 nM 5.91
CHEMBL1828642 IC50 = 1627.0 nM 5.79
CHEMBL1829807 IC50 = 1786.0 nM 5.75
CHEMBL1829813 IC50 = 2524.0 nM 5.60
CHEMBL1829803 IC50 > 10000.0 nM -