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Assay Detail

CHEMBL813659

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

Binding
Compound was tested for inhibition activity against human thrombin (FIIa)
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Prothrombin (CHEMBL204)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and activity of 2,6-diphenoxypyridine-derived factor Xa inhibitors.
Phillips G, Davey DD, Eagen KA, Koovakkat SK, Liang A, Ng HP, Pinkerton M, Trinh L, Whitlow M, Beatty AM, Morrissey MM.
J Med Chem (1999) 42 : 1749 -1756
PubMed 10346927 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 37 5.43 6.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL49958 1 6.44
CHEMBL48233 1 6.28
CHEMBL298415 1 6.26
CHEMBL51824 1 5.92
CHEMBL49786 1 5.85
CHEMBL52205 1 5.72
CHEMBL48691 1 5.60
CHEMBL295263 1 5.47
CHEMBL300622 1 5.47
CHEMBL48409 1 5.38
CHEMBL48199 1 5.31
CHEMBL296532 1 5.22
CHEMBL48827 1 4.96
CHEMBL50127 1 4.85
CHEMBL49636 1 4.66
CHEMBL48604 1 4.57
CHEMBL424036 1 4.43
CHEMBL46077 1 -
CHEMBL296618 1 -
CHEMBL296530 1 -
CHEMBL50714 1 -
CHEMBL48864 1 -
CHEMBL47264 1 -
CHEMBL49295 1 -
CHEMBL48206 1 -
CHEMBL49358 1 -
CHEMBL45785 1 -
CHEMBL50961 1 -
CHEMBL51482 1 -
CHEMBL19902 DX-9065A 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL49958 Ki = 360.0 nM 6.44
CHEMBL48233 Ki = 530.0 nM 6.28
CHEMBL298415 Ki = 550.0 nM 6.26
CHEMBL51824 Ki = 1200.0 nM 5.92
CHEMBL49786 Ki = 1400.0 nM 5.85
CHEMBL52205 Ki = 1900.0 nM 5.72
CHEMBL48691 Ki = 2500.0 nM 5.60
CHEMBL295263 Ki = 3400.0 nM 5.47
CHEMBL300622 Ki = 3400.0 nM 5.47
CHEMBL48409 Ki = 4200.0 nM 5.38
CHEMBL48199 Ki = 4900.0 nM 5.31
CHEMBL296532 Ki = 6000.0 nM 5.22
CHEMBL48827 Ki = 11000.0 nM 4.96
CHEMBL50127 Ki = 14000.0 nM 4.85
CHEMBL49636 Ki = 22000.0 nM 4.66
CHEMBL48604 Ki = 27000.0 nM 4.57
CHEMBL424036 Ki = 37000.0 nM 4.43
CHEMBL48595 Ki > 5000.0 nM -
CHEMBL45732 Ki > 5000.0 nM -
CHEMBL48965 Ki > 5000.0 nM -
CHEMBL50909 Ki > 5000.0 nM -
CHEMBL52479 Ki > 5000.0 nM -
CHEMBL48161 Ki > 5000.0 nM -
CHEMBL48497 Ki > 5000.0 nM -
CHEMBL19902 DX-9065A Ki > 5000.0 nM -
CHEMBL51482 Ki > 5000.0 nM -
CHEMBL50961 Ki > 5000.0 nM -
CHEMBL45785 Ki > 5000.0 nM -
CHEMBL49358 Ki > 5000.0 nM -
CHEMBL48206 Ki > 5000.0 nM -
CHEMBL49295 Ki > 5000.0 nM -
CHEMBL47264 Ki > 5000.0 nM -
CHEMBL48864 Ki > 5000.0 nM -
CHEMBL50714 Ki > 5000.0 nM -
CHEMBL296530 Ki > 5000.0 nM -
CHEMBL296618 Ki > 5000.0 nM -
CHEMBL46077 Ki > 100000.0 nM -