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Assay Detail

CHEMBL833209

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Functional
Inhibitory concentration in dilute prothrombin time assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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
IC50 8 6.30 6.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL440755 1 6.72
CHEMBL182763 1 6.64
CHEMBL185556 1 6.43
CHEMBL183426 1 6.43
CHEMBL182746 1 6.38
CHEMBL366134 1 6.21
CHEMBL182975 1 5.81
CHEMBL180695 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL440755 IC50 = 190.0 nM 6.72
CHEMBL182763 IC50 = 230.0 nM 6.64
CHEMBL185556 IC50 = 370.0 nM 6.43
CHEMBL183426 IC50 = 370.0 nM 6.43
CHEMBL182746 IC50 = 420.0 nM 6.38
CHEMBL366134 IC50 = 620.0 nM 6.21
CHEMBL182975 IC50 = 1550.0 nM 5.81
CHEMBL180695 IC50 = 1790.0 nM 5.75