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Assay Detail

CHEMBL682004

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Binding
Inhibitory activity against factor Xa using human purified enzyme.
29
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Nonbenzamidine isoxazoline derivatives as factor Xa inhibitors.
Quan ML, Ellis CD, He MY, Liauw AY, Lam PY, Rossi KA, Knabb RM, Luettgen JM, Wright MR, Wong PC, Wexler RR.
Bioorg Med Chem Lett (2003) 13 : 1023 -1028
PubMed 12643903 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 29 8.08 9.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL7651 2 9.96
CHEMBL275957 1 8.92
CHEMBL7626 3 8.82
CHEMBL269065 1 8.77
CHEMBL268329 1 8.66
CHEMBL267438 3 8.60
CHEMBL7928 1 8.52
CHEMBL269393 1 8.48
CHEMBL8135 1 8.43
CHEMBL8018 1 8.34
CHEMBL7854 1 8.26
CHEMBL268225 3 8.15
CHEMBL7967 1 8.14
CHEMBL268129 1 8.00
CHEMBL267681 1 7.96
CHEMBL267387 3 7.85
CHEMBL8090 1 7.82
CHEMBL7676 1 7.47
CHEMBL8356 1 7.16
CHEMBL7905 1 6.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL7651 Ki = 0.11 nM 9.96
CHEMBL7651 Ki = 0.17 nM 9.77
CHEMBL275957 Ki = 1.2 nM 8.92
CHEMBL7626 Ki = 1.5 nM 8.82
CHEMBL269065 Ki = 1.7 nM 8.77
CHEMBL7626 Ki = 1.9 nM 8.72
CHEMBL268329 Ki = 2.2 nM 8.66
CHEMBL267438 Ki = 2.5 nM 8.60
CHEMBL267438 Ki = 2.5 nM 8.60
CHEMBL7928 Ki = 3.0 nM 8.52
CHEMBL269393 Ki = 3.3 nM 8.48
CHEMBL8135 Ki = 3.7 nM 8.43
CHEMBL8018 Ki = 4.6 nM 8.34
CHEMBL7854 Ki = 5.5 nM 8.26
CHEMBL268225 Ki = 7.1 nM 8.15
CHEMBL7967 Ki = 7.2 nM 8.14
CHEMBL268225 Ki = 10.0 nM 8.00
CHEMBL268129 Ki = 10.0 nM 8.00
CHEMBL267681 Ki = 11.0 nM 7.96
CHEMBL267387 Ki = 14.0 nM 7.85
CHEMBL8090 Ki = 15.0 nM 7.82
CHEMBL267387 Ki = 15.0 nM 7.82
CHEMBL7676 Ki = 34.0 nM 7.47
CHEMBL8356 Ki = 69.0 nM 7.16
CHEMBL267438 Ki = 69.0 nM 7.16
CHEMBL7905 Ki = 130.0 nM 6.89
CHEMBL7626 Ki = 240.0 nM 6.62
CHEMBL268225 Ki = 320.0 nM 6.50
CHEMBL267387 Ki = 1100.0 nM 5.96