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Assay Detail

CHEMBL4383871

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

Binding
Inhibition of human factor Xa using S-2222 as substrate preincubated for 30 mins followed by substrate addition and measured for 20 mins
23
Total Activities
23
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

Design, synthesis and biological evaluation of anthranilamide derivatives as potential factor Xa (fXa) inhibitors.
Xing J, Yang L, Zhou J, Zhang H.
Bioorg Med Chem (2018) 26 : 5987 -5999
PubMed 30446438 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 6.89 8.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4441346 1 8.46
CHEMBL512351 BETRIXABAN 4.0 1 8.35
CHEMBL4469752 1 8.32
CHEMBL4469308 1 8.00
CHEMBL4439939 1 7.75
CHEMBL4530584 1 7.70
CHEMBL4574442 1 7.62
CHEMBL4586397 1 7.52
CHEMBL4514976 1 7.35
CHEMBL4450264 1 7.11
CHEMBL4530694 1 6.75
CHEMBL4459345 1 6.63
CHEMBL4543553 1 6.61
CHEMBL4438123 1 6.57
CHEMBL4445604 1 6.50
CHEMBL4572670 1 6.29
CHEMBL4470300 1 6.18
CHEMBL4439436 1 6.01
CHEMBL4448395 1 5.97
CHEMBL4525969 1 5.86
CHEMBL4472454 1 5.81
CHEMBL4472318 1 5.68
CHEMBL4439648 1 5.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4441346 IC50 = 3.5 nM 8.46
CHEMBL512351 BETRIXABAN IC50 = 4.5 nM 8.35
CHEMBL4469752 IC50 = 4.8 nM 8.32
CHEMBL4469308 IC50 = 10.0 nM 8.00
CHEMBL4439939 IC50 = 18.0 nM 7.75
CHEMBL4530584 IC50 = 20.0 nM 7.70
CHEMBL4574442 IC50 = 24.0 nM 7.62
CHEMBL4586397 IC50 = 30.0 nM 7.52
CHEMBL4514976 IC50 = 45.0 nM 7.35
CHEMBL4450264 IC50 = 77.0 nM 7.11
CHEMBL4530694 IC50 = 179.0 nM 6.75
CHEMBL4459345 IC50 = 234.0 nM 6.63
CHEMBL4543553 IC50 = 246.0 nM 6.61
CHEMBL4438123 IC50 = 272.0 nM 6.57
CHEMBL4445604 IC50 = 315.0 nM 6.50
CHEMBL4572670 IC50 = 513.0 nM 6.29
CHEMBL4470300 IC50 = 653.0 nM 6.18
CHEMBL4439436 IC50 = 981.0 nM 6.01
CHEMBL4448395 IC50 = 1079.0 nM 5.97
CHEMBL4525969 IC50 = 1387.0 nM 5.86
CHEMBL4472454 IC50 = 1543.0 nM 5.81
CHEMBL4472318 IC50 = 2087.0 nM 5.68
CHEMBL4439648 IC50 = 3189.0 nM 5.50