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Assay Detail

CHEMBL830433

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

Binding
Inhibition of [3H]SQ-29,548 binding to thromboxane A2 receptors (TP) of human platelet membrane
23
Total Activities
19
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

Development of dual-acting benzofurans for thromboxane A2 receptor antagonist and prostacyclin receptor agonist: synthesis, structure-activity relationship, and evaluation of benzofuran derivatives.
Ohno M, Miyamoto M, Hoshi K, Takeda T, Yamada N, Ohtake A.
J Med Chem (2005) 48 : 5279 -5294
PubMed 16078846 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 6.44 8.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL190288 1 8.37
CHEMBL190236 1 8.35
CHEMBL191056 1 7.58
CHEMBL365501 1 7.29
CHEMBL190840 1 7.14
CHEMBL192662 1 7.11
CHEMBL190708 1 7.06
CHEMBL191118 1 6.82
CHEMBL189694 1 6.75
CHEMBL188384 1 6.51
CHEMBL187544 1 5.60
CHEMBL361939 5 5.51
CHEMBL187758 1 5.51
CHEMBL189063 1 5.51
CHEMBL192661 1 5.29
CHEMBL190735 1 -
CHEMBL188758 1 -
CHEMBL191175 1 -
CHEMBL191162 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL190288 Ki = 4.3 nM 8.37
CHEMBL190236 Ki = 4.5 nM 8.35
CHEMBL191056 Ki = 26.0 nM 7.58
CHEMBL365501 Ki = 51.0 nM 7.29
CHEMBL190840 Ki = 72.0 nM 7.14
CHEMBL192662 Ki = 78.0 nM 7.11
CHEMBL190708 Ki = 88.0 nM 7.06
CHEMBL191118 Ki = 150.0 nM 6.82
CHEMBL189694 Ki = 180.0 nM 6.75
CHEMBL188384 Ki = 310.0 nM 6.51
CHEMBL187544 Ki = 2500.0 nM 5.60
CHEMBL187758 Ki = 3100.0 nM 5.51
CHEMBL189063 Ki = 3100.0 nM 5.51
CHEMBL361939 Ki = 3100.0 nM 5.51
CHEMBL361939 Ki = 3100.0 nM 5.51
CHEMBL361939 Ki = 3100.0 nM 5.51
CHEMBL361939 Ki = 3100.0 nM 5.51
CHEMBL361939 Ki = 3100.0 nM 5.51
CHEMBL192661 Ki = 5100.0 nM 5.29
CHEMBL188758 Ki > 15000.0 nM -
CHEMBL191175 Ki > 15000.0 nM -
CHEMBL190735 Ki > 10000.0 nM -
CHEMBL191162 Ki > 5900.0 nM -