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Assay Detail

CHEMBL946440

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

Binding
Inhibition of human thrombin
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prothrombin (CHEMBL204)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Achieving structural diversity using the perpendicular conformation of alpha-substituted phenylcyclopropanes to mimic the bioactive conformation of ortho-substituted biphenyl P4 moieties: discovery of novel, highly potent inhibitors of Factor Xa.
Qiao JX, Cheney DL, Alexander RS, Smallwood AM, King SR, He K, Rendina AR, Luettgen JM, Knabb RM, Wexler RR, Lam PY.
Bioorg Med Chem Lett (2008) 18 : 4118 -4123
PubMed 18550370 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 6.50 6.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL461297 1 6.72
CHEMBL206335 RAZAXABAN 2.0 1 6.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL461297 Ki = 191.0 nM 6.72
CHEMBL206335 RAZAXABAN Ki = 540.0 nM 6.27