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Assay Detail

CHEMBL875197

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Binding
Inhibitory activity against coagulation factor II (thrombin)
8
Total Activities
8
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

Novel factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of P4 substituents in combination with a neutral P1 ligand.
Nazaré M, Essrich M, Will DW, Matter H, Ritter K, Urmann M, Bauer A, Schreuder H, Czech J, Lorenz M, Laux V, Wehner V.
Bioorg Med Chem Lett (2004) 14 : 4197 -4201
PubMed 15261269 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 5.38 5.56

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL182746 1 5.56
CHEMBL440755 1 5.50
CHEMBL180695 1 5.08
CHEMBL366134 1 -
CHEMBL182763 1 -
CHEMBL185556 1 -
CHEMBL182975 1 -
CHEMBL183426 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL182746 Ki = 2760.0 nM 5.56
CHEMBL440755 Ki = 3160.0 nM 5.50
CHEMBL180695 Ki = 8220.0 nM 5.08
CHEMBL366134 Ki > 10000.0 nM -
CHEMBL182763 Ki > 10000.0 nM -
CHEMBL185556 Ki > 10000.0 nM -
CHEMBL182975 Ki > 10000.0 nM -
CHEMBL183426 Ki > 10000.0 nM -