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Assay Detail

CHEMBL2155306

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

Binding
Inhibition of human F10a using S-2765 as substrate after 45 mins
12
Total Activities
12
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

Synthesis and structure-activity relationship of potent, selective and orally active anthranilamide-based factor Xa inhibitors: application of weakly basic sulfoximine group as novel S4 binding element.
Pandya V, Jain M, Chakrabarti G, Soni H, Parmar B, Chaugule B, Patel J, Jarag T, Joshi J, Joshi N, Rath A, Unadkat V, Sharma B, Ajani H, Kumar J, Sairam KV, Patel H, Patel P.
Eur J Med Chem (2012) 58 : 136 -152
PubMed 23124211 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 8.39 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL198362 RIVAROXABAN 4.0 1 8.80
CHEMBL3392119 1 8.68
CHEMBL3392130 1 8.62
CHEMBL3392115 1 8.57
CHEMBL3392121 1 8.49
CHEMBL3392131 1 8.47
CHEMBL3392116 1 8.40
CHEMBL3392114 1 8.27
CHEMBL3392129 1 8.25
CHEMBL3392132 1 8.19
CHEMBL3392118 1 8.05
CHEMBL3392133 1 7.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL198362 RIVAROXABAN IC50 = 1.6 nM 8.80
CHEMBL3392119 IC50 = 2.1 nM 8.68
CHEMBL3392130 IC50 = 2.4 nM 8.62
CHEMBL3392115 IC50 = 2.7 nM 8.57
CHEMBL3392121 IC50 = 3.2 nM 8.49
CHEMBL3392131 IC50 = 3.4 nM 8.47
CHEMBL3392116 IC50 = 4.0 nM 8.40
CHEMBL3392114 IC50 = 5.4 nM 8.27
CHEMBL3392129 IC50 = 5.6 nM 8.25
CHEMBL3392132 IC50 = 6.4 nM 8.19
CHEMBL3392118 IC50 = 9.0 nM 8.05
CHEMBL3392133 IC50 = 11.6 nM 7.94