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Assay Detail

CHEMBL4420280

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

Binding
Inhibition of TFPI in human plasma with induced factor-8 deficiency assessed as increase in thrombin generation by measuring FEIBA using thrombin-specific fluorogenic substrate Z-Gly-Gly-Arg-AMC by calibrated automated thrombography
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Plasma
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 44 6.04 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3958046 1 6.96
CHEMBL3930464 1 6.92
CHEMBL4545754 1 6.89
CHEMBL3894172 1 6.80
CHEMBL3935596 1 6.77
CHEMBL3960763 1 6.68
CHEMBL3891294 1 6.58
CHEMBL3974158 1 6.58
CHEMBL4543933 1 6.54
CHEMBL3975755 1 6.50
CHEMBL4446952 1 6.38
CHEMBL3932312 1 6.33
CHEMBL4448151 1 6.24
CHEMBL4447278 1 6.20
CHEMBL4529374 1 6.11
CHEMBL4473601 1 6.09
CHEMBL4443384 1 6.07
CHEMBL3955549 1 6.07
CHEMBL3912278 1 6.05
CHEMBL4475522 1 6.05
CHEMBL4449783 1 6.03
CHEMBL4547511 1 6.02
CHEMBL4444694 1 5.97
CHEMBL4473322 1 5.96
CHEMBL4454557 1 5.93
CHEMBL4454621 1 5.89
CHEMBL4452013 1 5.86
CHEMBL4452653 1 5.84
CHEMBL4548910 1 5.83
CHEMBL4519206 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3958046 EC50 = 110.0 nM 6.96
CHEMBL3930464 EC50 = 120.0 nM 6.92
CHEMBL4545754 EC50 = 130.0 nM 6.89
CHEMBL3894172 EC50 = 160.0 nM 6.80
CHEMBL3935596 EC50 = 170.0 nM 6.77
CHEMBL3960763 EC50 = 210.0 nM 6.68
CHEMBL3891294 EC50 = 260.0 nM 6.58
CHEMBL3974158 EC50 = 260.0 nM 6.58
CHEMBL4543933 EC50 = 290.0 nM 6.54
CHEMBL3975755 EC50 = 320.0 nM 6.50
CHEMBL4446952 EC50 = 420.0 nM 6.38
CHEMBL3932312 EC50 = 470.0 nM 6.33
CHEMBL4448151 EC50 = 570.0 nM 6.24
CHEMBL4447278 EC50 = 630.0 nM 6.20
CHEMBL4529374 EC50 = 770.0 nM 6.11
CHEMBL4473601 EC50 = 820.0 nM 6.09
CHEMBL4443384 EC50 = 850.0 nM 6.07
CHEMBL3955549 EC50 = 850.0 nM 6.07
CHEMBL3912278 EC50 = 890.0 nM 6.05
CHEMBL4475522 EC50 = 890.0 nM 6.05
CHEMBL4449783 EC50 = 940.0 nM 6.03
CHEMBL4547511 EC50 = 950.0 nM 6.02
CHEMBL4444694 EC50 = 1060.0 nM 5.97
CHEMBL4473322 EC50 = 1100.0 nM 5.96
CHEMBL4454557 EC50 = 1170.0 nM 5.93
CHEMBL4454621 EC50 = 1300.0 nM 5.89
CHEMBL4452013 EC50 = 1380.0 nM 5.86
CHEMBL4452653 EC50 = 1450.0 nM 5.84
CHEMBL4548910 EC50 = 1480.0 nM 5.83
CHEMBL4519206 EC50 = 1530.0 nM 5.82
CHEMBL4461969 EC50 = 1550.0 nM 5.81
CHEMBL3910529 EC50 = 1600.0 nM 5.80
CHEMBL4449463 EC50 = 1630.0 nM 5.79
CHEMBL4517694 EC50 = 1750.0 nM 5.76
CHEMBL4458443 EC50 = 2460.0 nM 5.61
CHEMBL4545704 EC50 = 2500.0 nM 5.60
CHEMBL4436238 EC50 = 2540.0 nM 5.59
CHEMBL4471068 EC50 = 2780.0 nM 5.56
CHEMBL4539699 EC50 = 2990.0 nM 5.52
CHEMBL4456248 EC50 = 3100.0 nM 5.51
CHEMBL4448999 EC50 = 3150.0 nM 5.50
CHEMBL4440205 EC50 = 3800.0 nM 5.42
CHEMBL4442429 EC50 = 4790.0 nM 5.32
CHEMBL4440967 EC50 = 7920.0 nM 5.10