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Assay Detail

CHEMBL4419593

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

Binding
Inhibition of C-terminus 10x-His-taged human TFPI-1 (29 to 282 residues) assessed as inhibition of factor 10a using S-2222 substrate incubated for 115 mins by micro-plate reader based assay
253
Total Activities
253
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Tissue factor pathway inhibitor (CHEMBL3713062)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

TFPI inhibitors and methods of use
(2013)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 253 6.18 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4445250 1 8.92
CHEMBL4447812 1 8.68
CHEMBL4454272 1 8.68
CHEMBL4530936 1 8.62
CHEMBL4449468 1 8.32
CHEMBL3894172 1 7.70
CHEMBL3899635 1 7.52
CHEMBL4545754 1 7.40
CHEMBL4568357 1 7.30
CHEMBL3975755 1 7.30
CHEMBL3950682 1 7.30
CHEMBL3974158 1 7.22
CHEMBL3958046 1 7.22
CHEMBL4442500 1 7.10
CHEMBL3984087 1 7.05
CHEMBL3980096 1 7.00
CHEMBL4472071 1 7.00
CHEMBL3978085 1 6.92
CHEMBL3969514 1 6.89
CHEMBL3908913 1 6.89
CHEMBL3935596 1 6.89
CHEMBL3953204 1 6.82
CHEMBL3976722 1 6.80
CHEMBL3904040 1 6.80
CHEMBL3926366 1 6.77
CHEMBL3965457 1 6.77
CHEMBL3910796 1 6.75
CHEMBL3920502 1 6.75
CHEMBL3916916 1 6.75
CHEMBL4449783 1 6.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4445250 EC50 = 1.2 nM 8.92
CHEMBL4454272 EC50 = 2.1 nM 8.68
CHEMBL4447812 EC50 = 2.1 nM 8.68
CHEMBL4530936 EC50 = 2.4 nM 8.62
CHEMBL4449468 EC50 = 4.8 nM 8.32
CHEMBL3894172 EC50 = 20.0 nM 7.70
CHEMBL3899635 EC50 = 30.0 nM 7.52
CHEMBL4545754 EC50 = 40.0 nM 7.40
CHEMBL3950682 EC50 = 50.0 nM 7.30
CHEMBL4568357 EC50 = 50.3 nM 7.30
CHEMBL3975755 EC50 = 50.0 nM 7.30
CHEMBL3958046 EC50 = 60.0 nM 7.22
CHEMBL3974158 EC50 = 60.0 nM 7.22
CHEMBL4442500 EC50 = 80.0 nM 7.10
CHEMBL3984087 EC50 = 90.0 nM 7.05
CHEMBL4472071 EC50 = 100.0 nM 7.00
CHEMBL3980096 EC50 = 100.0 nM 7.00
CHEMBL3978085 EC50 = 120.0 nM 6.92
CHEMBL3935596 EC50 = 130.0 nM 6.89
CHEMBL3908913 EC50 = 130.0 nM 6.89
CHEMBL3969514 EC50 = 130.0 nM 6.89
CHEMBL3953204 EC50 = 152.3 nM 6.82
CHEMBL3904040 EC50 = 160.0 nM 6.80
CHEMBL3976722 EC50 = 160.0 nM 6.80
CHEMBL3926366 EC50 = 170.0 nM 6.77
CHEMBL3965457 EC50 = 170.0 nM 6.77
CHEMBL3916916 EC50 = 180.0 nM 6.75
CHEMBL3920502 EC50 = 180.0 nM 6.75
CHEMBL3910796 EC50 = 180.0 nM 6.75
CHEMBL3976800 EC50 = 190.0 nM 6.72
CHEMBL3961042 EC50 = 190.0 nM 6.72
CHEMBL4449783 EC50 = 190.0 nM 6.72
CHEMBL3892215 EC50 = 200.0 nM 6.70
CHEMBL4453765 EC50 = 200.0 nM 6.70
CHEMBL3949179 EC50 = 200.0 nM 6.70
CHEMBL3927717 EC50 = 210.0 nM 6.68
CHEMBL4530715 EC50 = 210.0 nM 6.68
CHEMBL3961378 EC50 = 210.0 nM 6.68
CHEMBL3897272 EC50 = 220.0 nM 6.66
CHEMBL3958468 EC50 = 220.0 nM 6.66
CHEMBL3958681 EC50 = 220.0 nM 6.66
CHEMBL3949739 EC50 = 220.0 nM 6.66
CHEMBL3891294 EC50 = 230.0 nM 6.64
CHEMBL4446952 EC50 = 240.0 nM 6.62
CHEMBL3906782 EC50 = 240.0 nM 6.62
CHEMBL3952366 EC50 = 240.0 nM 6.62
CHEMBL3960826 EC50 = 250.0 nM 6.60
CHEMBL3907128 EC50 = 250.0 nM 6.60
CHEMBL3937934 EC50 = 250.0 nM 6.60
CHEMBL3901896 EC50 = 250.0 nM 6.60