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Assay Detail

CHEMBL662831

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

Binding
In vitro inhibitory activity against Coagulation factor X
22
Total Activities
22
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

Discovery of a novel, selective, and orally bioavailable class of thrombin inhibitors incorporating aminopyridyl moieties at the P1 position.
Feng DM, Gardell SJ, Lewis SD, Bock MG, Chen Z, Freidinger RM, Naylor-Olsen AM, Ramjit HG, Woltmann R, Baskin EP, Lynch JJ, Lucas R, Shafer JA, Dancheck KB, Chen IW, Mao SS, Krueger JA, Hare TR, Mulichak AM, Vacca JP.
J Med Chem (1997) 40 : 3726 -3733
PubMed 9371237 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 4.79 5.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL122331 1 5.36
CHEMBL121982 1 5.12
CHEMBL421437 1 5.08
CHEMBL122801 1 5.00
CHEMBL123759 1 4.85
CHEMBL123142 1 4.80
CHEMBL421272 1 4.57
CHEMBL338788 1 4.28
CHEMBL96486 1 4.03
CHEMBL331181 1 -
CHEMBL124408 1 -
CHEMBL420334 1 -
CHEMBL121661 1 -
CHEMBL122432 1 -
CHEMBL331160 1 -
CHEMBL122601 1 -
CHEMBL331908 1 -
CHEMBL123942 1 -
CHEMBL125181 1 -
CHEMBL122488 1 -
CHEMBL435012 1 -
CHEMBL337923 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL122331 Ki = 4400.0 nM 5.36
CHEMBL121982 Ki = 7600.0 nM 5.12
CHEMBL421437 Ki = 8300.0 nM 5.08
CHEMBL122801 Ki = 10000.0 nM 5.00
CHEMBL123759 Ki = 14000.0 nM 4.85
CHEMBL123142 Ki = 16000.0 nM 4.80
CHEMBL421272 Ki = 27000.0 nM 4.57
CHEMBL338788 Ki = 52000.0 nM 4.28
CHEMBL96486 Ki = 94000.0 nM 4.03
CHEMBL331181 Ki > 100000.0 nM -
CHEMBL124408 Ki = 230000.0 nM -
CHEMBL420334 Ki > 100000.0 nM -
CHEMBL121661 Ki > 100000.0 nM -
CHEMBL122432 Ki > 100000.0 nM -
CHEMBL331160 Ki = 420000.0 nM -
CHEMBL122601 Ki = 240000.0 nM -
CHEMBL331908 Ki > 200000.0 nM -
CHEMBL123942 Ki = 160000.0 nM -
CHEMBL125181 Ki > 1000000.0 nM -
CHEMBL122488 Ki > 200000.0 nM -
CHEMBL435012 Ki > 100000.0 nM -
CHEMBL337923 Ki = 160000.0 nM -