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Assay Detail

CHEMBL808338

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Binding
Inhibitory activity against thrombin (IIa)
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Prothrombin (CHEMBL204)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Polymer-assisted solution-phase (PASP) parallel synthesis of an alpha-ketothiazole library as tissue factor VIIa inhibitors.
South MS, Dice TA, Girard TJ, Lachance RM, Stevens AM, Stegeman RA, Stallings WC, Kurumbail RG, Parlow JJ.
Bioorg Med Chem Lett (2003) 13 : 2363 -2367
PubMed 12824035 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 4.57 5.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL78055 1 5.40
CHEMBL76834 1 4.95
CHEMBL78057 1 4.92
CHEMBL77428 1 4.84
CHEMBL429170 1 4.82
CHEMBL1790570 1 4.71
CHEMBL77742 1 4.66
CHEMBL77142 1 4.30
CHEMBL257867 1 4.22
CHEMBL309394 1 4.07
CHEMBL78053 1 4.00
CHEMBL427751 1 4.00
CHEMBL311553 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL78055 IC50 = 4000.0 nM 5.40
CHEMBL76834 IC50 = 11200.0 nM 4.95
CHEMBL78057 IC50 = 12000.0 nM 4.92
CHEMBL77428 IC50 = 14600.0 nM 4.84
CHEMBL429170 IC50 = 15000.0 nM 4.82
CHEMBL1790570 IC50 = 19300.0 nM 4.71
CHEMBL77742 IC50 = 21700.0 nM 4.66
CHEMBL77142 IC50 = 50000.0 nM 4.30
CHEMBL257867 IC50 = 60000.0 nM 4.22
CHEMBL309394 IC50 = 84900.0 nM 4.07
CHEMBL78053 IC50 = 100000.0 nM 4.00
CHEMBL427751 IC50 = 100000.0 nM 4.00
CHEMBL311553 IC50 > 30000.0 nM -