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Assay Detail

CHEMBL814405

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

Binding
Inhibition of thromboxane formation at a concentration of 10e -6 M.
20
Total Activities
20
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 (CHEMBL4028)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Thromboxane synthetase inhibitors and antihypertensive agents. 3. N-[(1H-imidazol-1-yl)alkyl]heteroaryl amides as potent enzyme inhibitors.
Press JB, Wright WB, Chan PS, Haug MF, Marsico JW, Tomcufcik AS.
J Med Chem (1987) 30 : 1036 -1040
PubMed 3585902 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.47 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL8887 1 8.15
CHEMBL267978 1 7.57
CHEMBL8735 1 7.40
CHEMBL406693 1 7.30
CHEMBL9088 1 7.16
CHEMBL8870 1 7.00
CHEMBL417603 1 6.70
CHEMBL8648 1 6.70
CHEMBL8489 1 6.70
CHEMBL8819 1 6.52
CHEMBL8679 1 6.52
CHEMBL8879 1 6.40
CHEMBL8987 1 6.22
CHEMBL8986 1 5.89
CHEMBL267473 DAZOXIBEN 2.0 1 5.82
CHEMBL8515 1 5.70
CHEMBL268645 1 5.52
CHEMBL8976 1 5.52
CHEMBL8778 1 5.52
CHEMBL8957 1 5.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL8887 IC50 = 7.0 nM 8.15
CHEMBL267978 IC50 = 27.0 nM 7.57
CHEMBL8735 IC50 = 40.0 nM 7.40
CHEMBL406693 IC50 = 50.0 nM 7.30
CHEMBL9088 IC50 = 70.0 nM 7.16
CHEMBL8870 IC50 = 100.0 nM 7.00
CHEMBL417603 IC50 = 200.0 nM 6.70
CHEMBL8648 IC50 = 200.0 nM 6.70
CHEMBL8489 IC50 = 200.0 nM 6.70
CHEMBL8819 IC50 = 300.0 nM 6.52
CHEMBL8679 IC50 = 300.0 nM 6.52
CHEMBL8879 IC50 = 400.0 nM 6.40
CHEMBL8987 IC50 = 600.0 nM 6.22
CHEMBL8986 IC50 = 1300.0 nM 5.89
CHEMBL267473 DAZOXIBEN IC50 = 1500.0 nM 5.82
CHEMBL8515 IC50 = 2000.0 nM 5.70
CHEMBL268645 IC50 = 3000.0 nM 5.52
CHEMBL8976 IC50 = 3000.0 nM 5.52
CHEMBL8778 IC50 = 3000.0 nM 5.52
CHEMBL8957 IC50 = 8000.0 nM 5.10