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Assay Detail

CHEMBL971469

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

Binding
Displacement of radioligand from human recombinant TP receptor expressed in HEK293 cells by scintillation proximity assay
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of potent and selective DP1 receptor antagonists in the azaindole series.
Leblanc Y, Roy P, Dufresne C, Lachance N, Wang Z, O'Neill G, Greig G, Denis D, Mathieu MC, Slipetz D, Sawyer N, Tsou N.
Bioorg Med Chem Lett (2009) 19 : 2125 -2128
PubMed 19307115 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 35 6.50 8.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL482547 1 8.42
CHEMBL509685 1 8.15
CHEMBL521290 1 7.86
CHEMBL484327 1 7.75
CHEMBL520480 1 7.64
CHEMBL484130 1 7.61
CHEMBL483939 1 7.45
CHEMBL484525 1 7.41
CHEMBL519862 1 7.38
CHEMBL520481 1 7.19
CHEMBL482548 1 7.10
CHEMBL485535 1 6.76
CHEMBL520007 1 6.73
CHEMBL482953 1 6.47
CHEMBL484779 1 6.41
CHEMBL482744 1 6.38
CHEMBL518988 1 6.33
CHEMBL483152 1 6.23
CHEMBL518987 1 6.20
CHEMBL482743 1 6.19
CHEMBL521122 1 6.16
CHEMBL483991 1 6.03
CHEMBL519803 1 6.00
CHEMBL474502 1 6.00
CHEMBL482550 1 5.77
CHEMBL483159 1 5.68
CHEMBL483346 1 5.55
CHEMBL474702 1 5.54
CHEMBL483154 1 5.46
CHEMBL484778 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL482547 Ki = 3.8 nM 8.42
CHEMBL509685 Ki = 7.0 nM 8.15
CHEMBL521290 Ki = 13.9 nM 7.86
CHEMBL484327 Ki = 17.9 nM 7.75
CHEMBL520480 Ki = 23.1 nM 7.64
CHEMBL484130 Ki = 24.5 nM 7.61
CHEMBL483939 Ki = 35.7 nM 7.45
CHEMBL484525 Ki = 39.4 nM 7.41
CHEMBL519862 Ki = 41.5 nM 7.38
CHEMBL520481 Ki = 64.8 nM 7.19
CHEMBL482548 Ki = 78.9 nM 7.10
CHEMBL485535 Ki = 171.6 nM 6.76
CHEMBL520007 Ki = 186.0 nM 6.73
CHEMBL482953 Ki = 339.8 nM 6.47
CHEMBL484779 Ki = 387.0 nM 6.41
CHEMBL482744 Ki = 415.0 nM 6.38
CHEMBL518988 Ki = 468.0 nM 6.33
CHEMBL483152 Ki = 587.0 nM 6.23
CHEMBL518987 Ki = 626.0 nM 6.20
CHEMBL482743 Ki = 646.4 nM 6.19
CHEMBL521122 Ki = 687.0 nM 6.16
CHEMBL483991 Ki = 935.0 nM 6.03
CHEMBL519803 Ki = 990.0 nM 6.00
CHEMBL474502 Ki = 995.0 nM 6.00
CHEMBL482550 Ki = 1687.0 nM 5.77
CHEMBL483159 Ki = 2081.0 nM 5.68
CHEMBL483346 Ki = 2813.0 nM 5.55
CHEMBL474702 Ki = 2917.0 nM 5.54
CHEMBL483154 Ki = 3428.0 nM 5.46
CHEMBL484778 Ki = 5039.0 nM 5.30
CHEMBL484777 Ki = 6144.0 nM 5.21
CHEMBL506909 Ki = 6887.0 nM 5.16
CHEMBL514802 Ki = 12183.0 nM 4.91
CHEMBL514964 Ki > 20000.0 nM -
CHEMBL484404 Ki > 20000.0 nM -