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Assay Detail

CHEMBL830409

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

Binding
Inhibition of [3H]SQ-29,548 binding to human Thromboxane A2 receptor
4
Total Activities
4
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

Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist.
Ulven T, Kostenis E.
J Med Chem (2005) 48 : 897 -900
PubMed 15715457 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 6.71 8.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL361812 RAMATROBAN 4.0 1 8.35
CHEMBL194085 1 6.27
CHEMBL373118 1 5.52
CHEMBL179036 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL361812 RAMATROBAN Ki = 4.5 nM 8.35
CHEMBL194085 Ki = 540.0 nM 6.27
CHEMBL373118 Ki = 3000.0 nM 5.52
CHEMBL179036 Ki > 10000.0 nM -