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Assay Detail

CHEMBL817137

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

Binding
Binding affinity against trypsin
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Serine protease 1 (CHEMBL209)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, SAR and in vivo activity of novel thienopyridine sulfonamide pyrrolidinones as factor Xa inhibitors.
Becker MR, Ewing WR, Davis RS, Pauls HW, Ly C, Li A, Mason HJ, Choi-Sledeski YM, Spada AP, Chu V, Brown KD, Colussi DJ, Leadley RJ, Bentley R, Bostwick J, Kasiewski C, Morgan S.
Bioorg Med Chem Lett (1999) 9 : 2753 -2758
PubMed 10509929 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 5.89 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL93854 1 6.52
CHEMBL96218 1 6.07
CHEMBL330572 1 6.00
CHEMBL431267 1 5.80
CHEMBL431281 1 5.75
CHEMBL328721 1 5.54
CHEMBL85757 1 5.54
CHEMBL93431 1 -
CHEMBL431461 1 -
CHEMBL92893 1 -
CHEMBL314754 1 -
CHEMBL92345 1 -
CHEMBL93190 1 -
CHEMBL93740 1 -
CHEMBL92614 1 -
CHEMBL327636 1 -
CHEMBL330582 1 -
CHEMBL330011 1 -
CHEMBL328893 1 -
CHEMBL93741 1 -
CHEMBL421367 1 -
CHEMBL90741 1 -
CHEMBL93151 1 -
CHEMBL327560 1 -
CHEMBL92406 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL93854 Ki = 305.0 nM 6.52
CHEMBL96218 Ki = 860.0 nM 6.07
CHEMBL330572 Ki = 1000.0 nM 6.00
CHEMBL431267 Ki = 1600.0 nM 5.80
CHEMBL431281 Ki = 1800.0 nM 5.75
CHEMBL328721 Ki = 2900.0 nM 5.54
CHEMBL85757 Ki = 2900.0 nM 5.54
CHEMBL93431 Ki > 2900.0 nM -
CHEMBL431461 Ki > 2900.0 nM -
CHEMBL92893 Ki > 2900.0 nM -
CHEMBL314754 Ki > 2900.0 nM -
CHEMBL92345 Ki > 2900.0 nM -
CHEMBL93190 Ki > 2900.0 nM -
CHEMBL93740 Ki > 2900.0 nM -
CHEMBL92614 Ki > 2900.0 nM -
CHEMBL327636 Ki > 2900.0 nM -
CHEMBL330582 Ki > 2900.0 nM -
CHEMBL330011 Ki > 2900.0 nM -
CHEMBL328893 Ki > 2900.0 nM -
CHEMBL93741 Ki > 2900.0 nM -
CHEMBL421367 Ki > 2900.0 nM -
CHEMBL90741 Ki > 2900.0 nM -
CHEMBL93151 Ki > 2900.0 nM -
CHEMBL327560 Ki > 2900.0 nM -
CHEMBL92406 Ki > 2900.0 nM -