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Assay Detail

CHEMBL4420274

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 at 10 uM using thrombin-specific fluorogenic substrate Z-Gly-Gly-Arg-AMC by calibrated automated thrombography
327
Total Activities
327
Compounds Tested
2
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
Activity 324 - -
EC50 3 7.79 8.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4546481 1 8.32
CHEMBL4473203 1 8.00
CHEMBL4545581 1 7.06
CHEMBL4468325 1 -
CHEMBL4464679 1 -
CHEMBL4448683 1 -
CHEMBL4452712 1 -
CHEMBL4474759 1 -
CHEMBL4441789 1 -
CHEMBL4450866 1 -
CHEMBL4521549 1 -
CHEMBL4525286 1 -
CHEMBL4438997 1 -
CHEMBL4533244 1 -
CHEMBL4444481 1 -
CHEMBL3983321 1 -
CHEMBL4441212 1 -
CHEMBL4441617 1 -
CHEMBL4469457 1 -
CHEMBL4442183 1 -
CHEMBL4437738 1 -
CHEMBL4465308 1 -
CHEMBL4552854 1 -
CHEMBL4472478 1 -
CHEMBL4450021 1 -
CHEMBL4447278 1 -
CHEMBL4458645 1 -
CHEMBL4475946 1 -
CHEMBL4439952 1 -
CHEMBL4446430 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4546481 EC50 = 4.8 nM 8.32
CHEMBL4473203 EC50 = 10.0 nM 8.00
CHEMBL4545581 EC50 = 88.0 nM 7.06
CHEMBL3927791 Activity = 151.0 mU/ml -
CHEMBL3896444 Activity = 49.0 mU/ml -
CHEMBL3919315 Activity = 163.0 mU/ml -
CHEMBL3909443 Activity = 156.0 mU/ml -
CHEMBL4444450 Activity = 165.0 mU/ml -
CHEMBL3947562 Activity = 192.0 mU/ml -
CHEMBL3979191 Activity = 95.0 mU/ml -
CHEMBL3890567 Activity = 62.0 mU/ml -
CHEMBL3908506 Activity = 204.0 mU/ml -
CHEMBL3975098 Activity = 82.0 mU/ml -
CHEMBL3948427 Activity = 69.0 mU/ml -
CHEMBL3950569 Activity = 86.0 mU/ml -
CHEMBL4440103 Activity = 34.0 mU/ml -
CHEMBL3985851 Activity = 38.0 mU/ml -
CHEMBL3898666 Activity = 105.0 mU/ml -
CHEMBL4438102 Activity = 100.0 mU/ml -
CHEMBL4454094 Activity = 40.0 mU/ml -
CHEMBL3940709 Activity - -
CHEMBL3940379 Activity = 133.0 mU/ml -
CHEMBL3908160 Activity = 197.0 mU/ml -
CHEMBL3955549 Activity = 220.0 mU/ml -
CHEMBL4482926 Activity = 147.0 mU/ml -
CHEMBL3938403 Activity = 79.0 mU/ml -
CHEMBL3943623 Activity = 180.0 mU/ml -
CHEMBL4522409 Activity = 36.0 mU/ml -
CHEMBL4474279 Activity = 153.0 mU/ml -
CHEMBL4446952 Activity = 331.0 mU/ml -
CHEMBL4455442 Activity = 101.0 mU/ml -
CHEMBL4514015 Activity = 316.0 mU/ml -
CHEMBL3958151 Activity = 197.0 mU/ml -
CHEMBL3960826 Activity = 188.0 mU/ml -
CHEMBL3901896 Activity = 202.0 mU/ml -
CHEMBL3958681 Activity = 202.0 mU/ml -
CHEMBL3939160 Activity = 161.0 mU/ml -
CHEMBL3936395 Activity = 161.0 mU/ml -
CHEMBL3893542 Activity = 124.0 mU/ml -
CHEMBL3940948 Activity = 168.0 mU/ml -
CHEMBL3953245 Activity = 183.0 mU/ml -
CHEMBL3950581 Activity = 191.0 mU/ml -
CHEMBL3958577 Activity = 178.0 mU/ml -
CHEMBL3966852 Activity = 186.0 mU/ml -
CHEMBL3954974 Activity = 171.0 mU/ml -
CHEMBL4536290 Activity = 178.0 mU/ml -
CHEMBL3924693 Activity = 193.0 mU/ml -
CHEMBL3931437 Activity = 185.0 mU/ml -
CHEMBL3934143 Activity = 162.0 mU/ml -
CHEMBL3896235 Activity = 169.0 mU/ml -