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Assay Detail

CHEMBL954028

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

Binding
Inhibition of human factor 10a
21
Total Activities
21
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

Discovery of imidazo[1,5-c]imidazol-3-ones: weakly basic, orally active factor Xa inhibitors.
Imaeda Y, Kuroita T, Sakamoto H, Kawamoto T, Tobisu M, Konishi N, Hiroe K, Kawamura M, Tanaka T, Kubo K.
J Med Chem (2008) 51 : 3422 -3436
PubMed 18507371 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 7.12 8.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL487105 1 8.32
CHEMBL487306 1 8.28
CHEMBL485876 1 8.16
CHEMBL259603 1 8.01
CHEMBL486716 1 7.92
CHEMBL519562 1 7.64
CHEMBL484097 1 7.51
CHEMBL514861 1 7.43
CHEMBL519897 1 7.27
CHEMBL521315 1 7.25
CHEMBL477279 1 7.25
CHEMBL483135 1 6.92
CHEMBL484098 1 6.80
CHEMBL486717 1 6.77
CHEMBL482889 1 6.77
CHEMBL482684 1 6.64
CHEMBL488358 1 6.52
CHEMBL478159 1 6.34
CHEMBL514224 1 6.04
CHEMBL482685 1 5.85
CHEMBL482890 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL487105 IC50 = 4.8 nM 8.32
CHEMBL487306 IC50 = 5.3 nM 8.28
CHEMBL485876 IC50 = 6.9 nM 8.16
CHEMBL259603 IC50 = 9.7 nM 8.01
CHEMBL486716 IC50 = 12.0 nM 7.92
CHEMBL519562 IC50 = 23.0 nM 7.64
CHEMBL484097 IC50 = 31.0 nM 7.51
CHEMBL514861 IC50 = 37.0 nM 7.43
CHEMBL519897 IC50 = 54.0 nM 7.27
CHEMBL521315 IC50 = 56.0 nM 7.25
CHEMBL477279 IC50 = 56.0 nM 7.25
CHEMBL483135 IC50 = 120.0 nM 6.92
CHEMBL484098 IC50 = 160.0 nM 6.80
CHEMBL486717 IC50 = 170.0 nM 6.77
CHEMBL482889 IC50 = 170.0 nM 6.77
CHEMBL482684 IC50 = 230.0 nM 6.64
CHEMBL488358 IC50 = 300.0 nM 6.52
CHEMBL478159 IC50 = 460.0 nM 6.34
CHEMBL514224 IC50 = 910.0 nM 6.04
CHEMBL482685 IC50 = 1400.0 nM 5.85
CHEMBL482890 IC50 = 1600.0 nM 5.80