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Assay Detail

CHEMBL880442

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

Binding
In vitro inhibition of human coagulation factor Xa after incubation for 10 min at 25 degree C
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Discovery of the novel antithrombotic agent 5-chloro-N-({(5S)-2-oxo-3- [4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene- 2-carboxamide (BAY 59-7939): an oral, direct factor Xa inhibitor.
Roehrig S, Straub A, Pohlmann J, Lampe T, Pernerstorfer J, Schlemmer KH, Reinemer P, Perzborn E.
J Med Chem (2005) 48 : 5900 -5908
PubMed 16161994 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 7.43 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL383361 1 9.40
CHEMBL198362 RIVAROXABAN 4.0 1 9.15
CHEMBL194186 1 9.00
CHEMBL364284 1 8.85
CHEMBL196539 1 8.60
CHEMBL197377 1 8.40
CHEMBL370614 1 8.38
CHEMBL194193 1 8.10
CHEMBL371336 1 8.07
CHEMBL196515 1 7.70
CHEMBL196492 1 7.70
CHEMBL381866 1 7.58
CHEMBL197547 1 7.54
CHEMBL196162 1 7.50
CHEMBL372956 1 7.40
CHEMBL196551 1 7.37
CHEMBL198654 1 7.13
CHEMBL194810 1 7.05
CHEMBL436293 1 7.03
CHEMBL381016 1 6.92
CHEMBL197624 1 6.85
CHEMBL198421 1 6.71
CHEMBL370176 1 6.54
CHEMBL372568 1 5.93
CHEMBL194889 1 5.92
CHEMBL196589 1 5.90
CHEMBL196669 1 5.70
CHEMBL371106 1 5.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL383361 IC50 = 0.4 nM 9.40
CHEMBL198362 RIVAROXABAN IC50 = 0.7 nM 9.15
CHEMBL194186 IC50 = 1.0 nM 9.00
CHEMBL364284 IC50 = 1.4 nM 8.85
CHEMBL196539 IC50 = 2.5 nM 8.60
CHEMBL197377 IC50 = 4.0 nM 8.40
CHEMBL370614 IC50 = 4.2 nM 8.38
CHEMBL194193 IC50 = 8.0 nM 8.10
CHEMBL371336 IC50 = 8.5 nM 8.07
CHEMBL196515 IC50 = 20.0 nM 7.70
CHEMBL196492 IC50 = 20.0 nM 7.70
CHEMBL381866 IC50 = 26.0 nM 7.58
CHEMBL197547 IC50 = 29.0 nM 7.54
CHEMBL196162 IC50 = 32.0 nM 7.50
CHEMBL372956 IC50 = 40.0 nM 7.40
CHEMBL196551 IC50 = 43.0 nM 7.37
CHEMBL198654 IC50 = 74.0 nM 7.13
CHEMBL194810 IC50 = 90.0 nM 7.05
CHEMBL436293 IC50 = 94.0 nM 7.03
CHEMBL381016 IC50 = 120.0 nM 6.92
CHEMBL197624 IC50 = 140.0 nM 6.85
CHEMBL198421 IC50 = 197.0 nM 6.71
CHEMBL370176 IC50 = 290.0 nM 6.54
CHEMBL372568 IC50 = 1170.0 nM 5.93
CHEMBL194889 IC50 = 1200.0 nM 5.92
CHEMBL196589 IC50 = 1260.0 nM 5.90
CHEMBL196669 IC50 = 2000.0 nM 5.70
CHEMBL371106 IC50 = 2300.0 nM 5.64