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Assay Detail

CHEMBL813715

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Binding
In vitro inhibition of Thromboxane A2 synthase
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Thromboxane-A synthase (CHEMBL1835)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 4. 8-[[(4-Chlorophenyl)sulfonyl]amino]-4-(3-(3-pyridinyl) propyl)octanoic acid and analogs.
Bhagwat SS, Gude C, Boswell C, Contardo N, Cohen DS, Dotson R, Mathis J, Lee W, Furness P, Zoganas H.
J Med Chem (1992) 35 : 4373 -4383
PubMed 1447738 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 8.17 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL136762 1 9.00
CHEMBL435590 1 9.00
CHEMBL137402 1 9.00
CHEMBL136738 1 8.82
CHEMBL341686 1 8.70
CHEMBL139372 1 8.70
CHEMBL136371 1 8.52
CHEMBL136934 1 8.52
CHEMBL134580 1 8.52
CHEMBL280728 RIDOGREL 2.0 1 8.52
CHEMBL63904 1 8.52
CHEMBL344457 1 8.52
CHEMBL138328 1 8.40
CHEMBL137505 1 8.40
CHEMBL138743 1 8.30
CHEMBL136880 1 8.15
CHEMBL345105 1 8.15
CHEMBL134686 1 8.00
CHEMBL343535 1 7.75
CHEMBL134365 1 7.70
CHEMBL65414 1 7.70
CHEMBL136918 1 7.40
CHEMBL136149 1 7.22
CHEMBL136130 1 7.16
CHEMBL136997 1 7.05
CHEMBL137187 1 6.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL136762 IC50 = 1.0 nM 9.00
CHEMBL435590 IC50 = 1.0 nM 9.00
CHEMBL137402 IC50 = 1.0 nM 9.00
CHEMBL136738 IC50 = 1.5 nM 8.82
CHEMBL341686 IC50 = 2.0 nM 8.70
CHEMBL139372 IC50 = 2.0 nM 8.70
CHEMBL136371 IC50 = 3.0 nM 8.52
CHEMBL136934 IC50 = 3.0 nM 8.52
CHEMBL134580 IC50 = 3.0 nM 8.52
CHEMBL280728 RIDOGREL IC50 = 3.0 nM 8.52
CHEMBL63904 IC50 = 3.0 nM 8.52
CHEMBL344457 IC50 = 3.0 nM 8.52
CHEMBL138328 IC50 = 4.0 nM 8.40
CHEMBL137505 IC50 = 4.0 nM 8.40
CHEMBL138743 IC50 = 5.0 nM 8.30
CHEMBL136880 IC50 = 7.0 nM 8.15
CHEMBL345105 IC50 = 7.0 nM 8.15
CHEMBL134686 IC50 = 10.0 nM 8.00
CHEMBL343535 IC50 = 18.0 nM 7.75
CHEMBL134365 IC50 = 20.0 nM 7.70
CHEMBL65414 IC50 = 20.0 nM 7.70
CHEMBL136918 IC50 = 40.0 nM 7.40
CHEMBL136149 IC50 = 60.0 nM 7.22
CHEMBL136130 IC50 = 70.0 nM 7.16
CHEMBL136997 IC50 = 90.0 nM 7.05
CHEMBL137187 IC50 = 150.0 nM 6.82