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Assay Detail

CHEMBL2319887

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Binding
Inhibition of tissue factor procoagulant activity in LPS-stimulated human THP1 cells preincubated for 1 hr before LPS addition measured after 5 hrs
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type THP-1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Tissue factor (CHEMBL4081)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Chemical and microbial semi-synthesis of tetrahydroprotoberberines as inhibitors on tissue factor procoagulant activity.
Ge HX, Zhang J, Chen L, Kou JP, Yu BY.
Bioorg Med Chem (2013) 21 : 62 -69
PubMed 23199480 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 7.24 8.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2314739 1 8.43
CHEMBL2314733 1 8.17
CHEMBL275097 TETRAHYDROBERBERINE 1 8.08
CHEMBL2314742 1 8.06
CHEMBL2314746 1 7.92
CHEMBL2314744 1 7.90
CHEMBL187892 1 7.82
CHEMBL2314743 1 7.78
CHEMBL487182 TETRAHYDROPALMATINE 2.0 1 7.64
CHEMBL2314732 1 7.44
CHEMBL2314741 1 7.41
CHEMBL2314734 1 7.20
CHEMBL487387 STEPHOLIDINE 1 6.98
CHEMBL2314735 1 6.92
CHEMBL448891 1 6.82
CHEMBL2314745 1 6.73
CHEMBL2314740 1 6.70
CHEMBL140 CURCUMIN 3.0 1 6.70
CHEMBL2314737 1 6.42
CHEMBL2314738 1 6.25
CHEMBL2314747 1 6.01
CHEMBL2314736 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2314739 IC50 = 3.75 nM 8.43
CHEMBL2314733 IC50 = 6.75 nM 8.17
CHEMBL275097 TETRAHYDROBERBERINE IC50 = 8.35 nM 8.08
CHEMBL2314742 IC50 = 8.79 nM 8.06
CHEMBL2314746 IC50 = 12.17 nM 7.92
CHEMBL2314744 IC50 = 12.61 nM 7.90
CHEMBL187892 IC50 = 14.98 nM 7.82
CHEMBL2314743 IC50 = 16.8 nM 7.78
CHEMBL487182 TETRAHYDROPALMATINE IC50 = 22.78 nM 7.64
CHEMBL2314732 IC50 = 36.41 nM 7.44
CHEMBL2314741 IC50 = 38.59 nM 7.41
CHEMBL2314734 IC50 = 63.06 nM 7.20
CHEMBL487387 STEPHOLIDINE IC50 = 104.58 nM 6.98
CHEMBL2314735 IC50 = 118.8 nM 6.92
CHEMBL448891 IC50 = 152.43 nM 6.82
CHEMBL2314745 IC50 = 187.26 nM 6.73
CHEMBL2314740 IC50 = 201.93 nM 6.70
CHEMBL140 CURCUMIN IC50 = 199.63 nM 6.70
CHEMBL2314737 IC50 = 376.52 nM 6.42
CHEMBL2314738 IC50 = 555.37 nM 6.25
CHEMBL2314747 IC50 = 968.9 nM 6.01
CHEMBL2314736 IC50 = 1501.43 nM 5.82