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Assay Detail

CHEMBL874927

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Functional
Inhibition of U-46,619-induced inositol phosphate accumulation at human Thromboxane A2 receptor
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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
IC50 4 6.38 8.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL361812 RAMATROBAN 4.0 1 8.02
CHEMBL194085 1 5.77
CHEMBL373118 1 5.34
CHEMBL179036 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL361812 RAMATROBAN IC50 = 9.6 nM 8.02
CHEMBL194085 IC50 = 1700.0 nM 5.77
CHEMBL373118 IC50 = 4600.0 nM 5.34
CHEMBL179036 IC50 > 10000.0 nM -