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Assay Detail

CHEMBL4420272

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Binding
Inhibition of C-terminus 10x-His-taged human TFPI-1 (29 to 282 residues) assessed as suppression of TFPI-mediated inhibition of extrinsic tenase complex by measuring factor 10a activation using S-2222 substrate in presence of FVIIa, lipidated TF, phospholipid vesicles by micro-plate reader based assay
ChEMBL ↗
121
Total Activities
121
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 121 5.93 8.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4545581 — — 1 8.11
CHEMBL4473343 — — 1 7.52
CHEMBL4540848 — — 1 7.40
CHEMBL4445814 — — 1 7.40
CHEMBL4434931 — — 1 7.30
CHEMBL4453431 — — 1 7.30
CHEMBL4434917 — — 1 7.30
CHEMBL3978593 — — 1 7.22
CHEMBL4434984 — — 1 7.00
CHEMBL4456724 — — 1 7.00
CHEMBL4449306 — — 1 6.96
CHEMBL4445250 — — 1 6.82
CHEMBL4528590 — — 1 6.80
CHEMBL4447812 — — 1 6.80
CHEMBL4457268 — — 1 6.77
CHEMBL4449468 — — 1 6.77
CHEMBL4442500 — — 1 6.77
CHEMBL4442145 — — 1 6.75
CHEMBL4448151 — — 1 6.72
CHEMBL4473203 — — 1 6.70
CHEMBL4448929 — — 1 6.70
CHEMBL4443609 — — 1 6.68
CHEMBL4461743 — — 1 6.66
CHEMBL4439104 — — 1 6.66
CHEMBL4586900 — — 1 6.58
CHEMBL4442960 — — 1 6.57
CHEMBL4435801 — — 1 6.57
CHEMBL3899025 — — 1 6.55
CHEMBL3959676 — — 1 6.47
CHEMBL4463036 — — 1 6.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4545581 — EC50 = 7.8 nM 8.11
CHEMBL4473343 — EC50 = 30.0 nM 7.52
CHEMBL4540848 — EC50 = 40.0 nM 7.40
CHEMBL4445814 — EC50 = 40.0 nM 7.40
CHEMBL4434917 — EC50 = 50.0 nM 7.30
CHEMBL4453431 — EC50 = 50.0 nM 7.30
CHEMBL4434931 — EC50 = 50.0 nM 7.30
CHEMBL3978593 — EC50 = 60.0 nM 7.22
CHEMBL4456724 — EC50 = 100.0 nM 7.00
CHEMBL4434984 — EC50 = 100.0 nM 7.00
CHEMBL4449306 — EC50 = 110.0 nM 6.96
CHEMBL4445250 — EC50 = 150.0 nM 6.82
CHEMBL4447812 — EC50 = 160.0 nM 6.80
CHEMBL4528590 — EC50 = 160.0 nM 6.80
CHEMBL4442500 — EC50 = 170.0 nM 6.77
CHEMBL4457268 — EC50 = 170.0 nM 6.77
CHEMBL4449468 — EC50 = 170.0 nM 6.77
CHEMBL4442145 — EC50 = 180.0 nM 6.75
CHEMBL4448151 — EC50 = 190.0 nM 6.72
CHEMBL4473203 — EC50 = 200.0 nM 6.70
CHEMBL4448929 — EC50 = 200.0 nM 6.70
CHEMBL4443609 — EC50 = 210.0 nM 6.68
CHEMBL4439104 — EC50 = 220.0 nM 6.66
CHEMBL4461743 — EC50 = 220.0 nM 6.66
CHEMBL4586900 — EC50 = 260.0 nM 6.58
CHEMBL4442960 — EC50 = 270.0 nM 6.57
CHEMBL4435801 — EC50 = 270.0 nM 6.57
CHEMBL3899025 — EC50 = 280.0 nM 6.55
CHEMBL3959676 — EC50 = 340.0 nM 6.47
CHEMBL4463036 — EC50 = 350.0 nM 6.46
CHEMBL4530936 — EC50 = 370.0 nM 6.43
CHEMBL3981290 — EC50 = 380.0 nM 6.42
CHEMBL4471068 — EC50 = 380.0 nM 6.42
CHEMBL4440298 — EC50 = 380.0 nM 6.42
CHEMBL4449027 — EC50 = 420.0 nM 6.38
CHEMBL4472071 — EC50 = 450.0 nM 6.35
CHEMBL4547027 — EC50 = 460.0 nM 6.34
CHEMBL4465308 — EC50 = 470.0 nM 6.33
CHEMBL4476615 — EC50 = 490.0 nM 6.31
CHEMBL4451495 — EC50 = 550.0 nM 6.26
CHEMBL4441052 — EC50 = 560.0 nM 6.25
CHEMBL4450112 — EC50 = 580.0 nM 6.24
CHEMBL4457745 — EC50 = 610.0 nM 6.21
CHEMBL4471001 — EC50 = 610.0 nM 6.21
CHEMBL4537728 — EC50 = 610.0 nM 6.21
CHEMBL4461957 — EC50 = 630.0 nM 6.20
CHEMBL4540663 — EC50 = 770.0 nM 6.11
CHEMBL3974158 — EC50 = 790.0 nM 6.10
CHEMBL3895146 — EC50 = 810.0 nM 6.09
CHEMBL3910006 — EC50 = 890.0 nM 6.05