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Assay Detail

CHEMBL808532

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

Binding
Inhibition of human platelet thromboxane synthase (TXA2) was determined in human platelets
29
Total Activities
29
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

N-(heterocyclic alkyl)pyrido[2,1-b]quinazoline-8-carboxamides as orally active antiallergy agents.
Tilley JW, Levitan P, Lind J, Welton AF, Crowley HJ, Tobias LD, O'Donnell M.
J Med Chem (1987) 30 : 185 -193
PubMed 2879917 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 6.69 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL60625 1 7.70
CHEMBL57489 1 7.70
CHEMBL56418 1 7.70
CHEMBL1202758 1 7.30
CHEMBL57480 1 7.22
CHEMBL57716 1 7.22
CHEMBL300338 1 7.00
CHEMBL1204216 1 7.00
CHEMBL1204214 1 7.00
CHEMBL58518 1 7.00
CHEMBL1204213 1 7.00
CHEMBL1204224 1 7.00
CHEMBL1204215 1 7.00
CHEMBL60930 1 6.70
CHEMBL294706 1 6.70
CHEMBL293362 1 6.70
CHEMBL1204223 1 6.70
CHEMBL57736 1 6.70
CHEMBL267473 DAZOXIBEN 2.0 1 6.60
CHEMBL60572 1 6.52
CHEMBL418452 1 6.52
CHEMBL301215 1 6.30
CHEMBL1202757 1 6.22
CHEMBL1202763 1 6.22
CHEMBL1202755 1 6.00
CHEMBL1204218 1 5.40
CHEMBL1202756 1 5.30
CHEMBL267475 FPL-55712 1 5.00
CHEMBL56742 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL60625 IC50 = 20.0 nM 7.70
CHEMBL57489 IC50 = 20.0 nM 7.70
CHEMBL56418 IC50 = 20.0 nM 7.70
CHEMBL1202758 IC50 = 50.0 nM 7.30
CHEMBL57480 IC50 = 60.0 nM 7.22
CHEMBL57716 IC50 = 60.0 nM 7.22
CHEMBL300338 IC50 = 100.0 nM 7.00
CHEMBL1204216 IC50 = 100.0 nM 7.00
CHEMBL1204214 IC50 = 100.0 nM 7.00
CHEMBL58518 IC50 = 100.0 nM 7.00
CHEMBL1204213 IC50 = 100.0 nM 7.00
CHEMBL1204224 IC50 = 100.0 nM 7.00
CHEMBL1204215 IC50 = 100.0 nM 7.00
CHEMBL60930 IC50 = 200.0 nM 6.70
CHEMBL294706 IC50 = 200.0 nM 6.70
CHEMBL293362 IC50 = 200.0 nM 6.70
CHEMBL1204223 IC50 = 200.0 nM 6.70
CHEMBL57736 IC50 = 200.0 nM 6.70
CHEMBL267473 DAZOXIBEN IC50 = 250.0 nM 6.60
CHEMBL60572 IC50 = 300.0 nM 6.52
CHEMBL418452 IC50 = 300.0 nM 6.52
CHEMBL301215 IC50 = 500.0 nM 6.30
CHEMBL1202757 IC50 = 600.0 nM 6.22
CHEMBL1202763 IC50 = 600.0 nM 6.22
CHEMBL1202755 IC50 = 1000.0 nM 6.00
CHEMBL1204218 IC50 = 4000.0 nM 5.40
CHEMBL1202756 IC50 = 5000.0 nM 5.30
CHEMBL267475 FPL-55712 IC50 = 10000.0 nM 5.00
CHEMBL56742 IC50 > 10000.0 nM -