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Assay Detail

CHEMBL4401964

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

Binding
Inhibition of human factor Xa using Z-D-Arg-Gly-Arg-pNA.2HCl as substrate preincubated for 15 mins followed by substrate addition by UV absorption analysis
13
Total Activities
13
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

Coagulation factor X (CHEMBL244)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Semisynthesis of epoxy-pimarane diterpenoids from kirenol and their FXa inhibition activities.
Wang J, Wu M, Gao C, Fu H.
Bioorg Med Chem (2019) 27 : 1320 -1326
PubMed 30792102 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.57 8.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1269025 EDOXABAN 4.0 1 8.47
CHEMBL4526357 1 6.66
CHEMBL4561623 1 6.02
CHEMBL4474248 1 5.77
CHEMBL1089731 KIRENOL 1 5.60
CHEMBL4555342 1 5.33
CHEMBL4452613 1 5.21
CHEMBL4577469 1 5.14
CHEMBL4581081 1 5.13
CHEMBL4455162 1 5.10
CHEMBL4560959 1 4.75
CHEMBL4464490 1 4.73
CHEMBL4468511 1 4.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1269025 EDOXABAN IC50 = 3.4 nM 8.47
CHEMBL4526357 IC50 = 220.0 nM 6.66
CHEMBL4561623 IC50 = 960.0 nM 6.02
CHEMBL4474248 IC50 = 1700.0 nM 5.77
CHEMBL1089731 KIRENOL IC50 = 2500.0 nM 5.60
CHEMBL4555342 IC50 = 4700.0 nM 5.33
CHEMBL4452613 IC50 = 6100.0 nM 5.21
CHEMBL4577469 IC50 = 7200.0 nM 5.14
CHEMBL4581081 IC50 = 7400.0 nM 5.13
CHEMBL4455162 IC50 = 7900.0 nM 5.10
CHEMBL4560959 IC50 = 17800.0 nM 4.75
CHEMBL4464490 IC50 = 18500.0 nM 4.73
CHEMBL4468511 IC50 = 27900.0 nM 4.55