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Assay Detail

CHEMBL1067914

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

Binding
Inhibition of human factor 10a by microplate spectrophotometry
15
Total Activities
15
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 SAR of cis-1,2-diaminocyclohexane derivatives as potent factor Xa inhibitors. Part II: exploration of 6-6 fused rings as alternative S1 moieties.
Yoshikawa K, Kobayashi S, Nakamoto Y, Haginoya N, Komoriya S, Yoshino T, Nagata T, Mochizuki A, Watanabe K, Suzuki M, Kanno H, Ohta T.
Bioorg Med Chem (2009) 17 : 8221 -8233
PubMed 19900814 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 8.00 9.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL596107 1 9.37
CHEMBL593604 1 8.85
CHEMBL479863 1 8.64
CHEMBL605310 1 8.52
CHEMBL595663 1 8.48
CHEMBL595710 1 8.47
CHEMBL605507 1 8.39
CHEMBL594308 1 8.31
CHEMBL593315 1 8.24
CHEMBL593603 1 8.02
CHEMBL594532 1 7.92
CHEMBL593326 1 7.92
CHEMBL596106 1 7.46
CHEMBL594487 1 6.06
CHEMBL604884 1 5.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL596107 IC50 = 0.43 nM 9.37
CHEMBL593604 IC50 = 1.4 nM 8.85
CHEMBL479863 IC50 = 2.3 nM 8.64
CHEMBL605310 IC50 = 3.0 nM 8.52
CHEMBL595663 IC50 = 3.3 nM 8.48
CHEMBL595710 IC50 = 3.4 nM 8.47
CHEMBL605507 IC50 = 4.1 nM 8.39
CHEMBL594308 IC50 = 4.9 nM 8.31
CHEMBL593315 IC50 = 5.7 nM 8.24
CHEMBL593603 IC50 = 9.5 nM 8.02
CHEMBL594532 IC50 = 12.0 nM 7.92
CHEMBL593326 IC50 = 12.0 nM 7.92
CHEMBL596106 IC50 = 35.0 nM 7.46
CHEMBL594487 IC50 = 870.0 nM 6.06
CHEMBL604884 IC50 = 4000.0 nM 5.40