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Assay Detail

CHEMBL662230

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Binding
Inhibitory activity against tissue coagulation factor VII.
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Coagulation factor VII (CHEMBL3991)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Polymer-assisted solution-phase library synthesis and crystal structure of alpha-ketothiazoles as tissue factor VIIa inhibitors.
Parlow JJ, Dice TA, Lachance RM, Girard TJ, Stevens AM, Stegeman RA, Stallings WC, Kurumbail RG, South MS.
J Med Chem (2003) 46 : 4043 -4049
PubMed 12954057 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 6.12 7.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL78055 1 7.38
CHEMBL311553 1 7.05
CHEMBL275859 1 6.96
CHEMBL76834 1 6.80
CHEMBL337238 1 6.77
CHEMBL78057 1 6.77
CHEMBL339241 1 6.72
CHEMBL429170 1 6.70
CHEMBL78053 1 6.70
CHEMBL131401 1 6.70
CHEMBL77428 1 6.64
CHEMBL77742 1 6.62
CHEMBL1790570 1 6.52
CHEMBL77142 1 6.47
CHEMBL334121 1 6.30
CHEMBL130464 1 6.24
CHEMBL264258 1 6.17
CHEMBL422973 1 6.16
CHEMBL422974 1 6.16
CHEMBL339341 1 6.12
CHEMBL309394 1 6.10
CHEMBL337930 1 6.09
CHEMBL132057 1 6.05
CHEMBL257867 1 5.99
CHEMBL131192 1 5.89
CHEMBL427751 1 5.84
CHEMBL131452 1 5.82
CHEMBL337014 1 5.81
CHEMBL130773 1 5.74
CHEMBL130592 1 5.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL78055 IC50 = 42.0 nM 7.38
CHEMBL311553 IC50 = 90.0 nM 7.05
CHEMBL275859 IC50 = 110.0 nM 6.96
CHEMBL76834 IC50 = 160.0 nM 6.80
CHEMBL337238 IC50 = 170.0 nM 6.77
CHEMBL78057 IC50 = 170.0 nM 6.77
CHEMBL339241 IC50 = 190.0 nM 6.72
CHEMBL429170 IC50 = 200.0 nM 6.70
CHEMBL78053 IC50 = 200.0 nM 6.70
CHEMBL131401 IC50 = 200.0 nM 6.70
CHEMBL77428 IC50 = 230.0 nM 6.64
CHEMBL77742 IC50 = 240.0 nM 6.62
CHEMBL1790570 IC50 = 300.0 nM 6.52
CHEMBL77142 IC50 = 340.0 nM 6.47
CHEMBL334121 IC50 = 500.0 nM 6.30
CHEMBL130464 IC50 = 570.0 nM 6.24
CHEMBL264258 IC50 = 680.0 nM 6.17
CHEMBL422973 IC50 = 700.0 nM 6.16
CHEMBL422974 IC50 = 700.0 nM 6.16
CHEMBL339341 IC50 = 760.0 nM 6.12
CHEMBL309394 IC50 = 800.0 nM 6.10
CHEMBL337930 IC50 = 820.0 nM 6.09
CHEMBL132057 IC50 = 900.0 nM 6.05
CHEMBL257867 IC50 = 1030.0 nM 5.99
CHEMBL131192 IC50 = 1290.0 nM 5.89
CHEMBL427751 IC50 = 1450.0 nM 5.84
CHEMBL131452 IC50 = 1530.0 nM 5.82
CHEMBL337014 IC50 = 1560.0 nM 5.81
CHEMBL130773 IC50 = 1830.0 nM 5.74
CHEMBL130592 IC50 = 1950.0 nM 5.71
CHEMBL337654 IC50 = 2820.0 nM 5.55
CHEMBL132395 IC50 = 3180.0 nM 5.50
CHEMBL339956 IC50 = 3300.0 nM 5.48
CHEMBL130252 IC50 = 5600.0 nM 5.25
CHEMBL130344 IC50 = 5880.0 nM 5.23
CHEMBL336553 IC50 = 9970.0 nM 5.00
CHEMBL128019 IC50 = 13700.0 nM 4.86
CHEMBL407142 IC50 = 17800.0 nM 4.75