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Assay Detail

CHEMBL946423

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Binding
Inhibition of human factor 10a
32
Total Activities
32
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

Coagulation factor X (CHEMBL244)
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 32 9.32 10.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL461091 1 10.68
CHEMBL471550 1 10.60
CHEMBL461297 1 10.46
CHEMBL508428 1 10.42
CHEMBL518648 1 10.38
CHEMBL513062 1 10.27
CHEMBL511486 1 10.26
CHEMBL471565 1 10.19
CHEMBL471734 1 10.13
CHEMBL461090 1 9.92
CHEMBL517711 1 9.85
CHEMBL479925 1 9.85
CHEMBL237226 1 9.82
CHEMBL460884 1 9.74
CHEMBL206335 RAZAXABAN 2.0 1 9.72
CHEMBL459849 1 9.55
CHEMBL218525 1 9.52
CHEMBL517263 1 9.24
CHEMBL221296 1 9.12
CHEMBL459430 1 8.85
CHEMBL452535 1 8.80
CHEMBL460056 1 8.74
CHEMBL508927 1 8.74
CHEMBL452793 1 8.72
CHEMBL511082 1 8.62
CHEMBL460681 1 8.52
CHEMBL507737 1 8.48
CHEMBL452802 1 8.24
CHEMBL510344 1 7.52
CHEMBL460055 1 7.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL461091 Ki = 0.021 nM 10.68
CHEMBL471550 Ki = 0.025 nM 10.60
CHEMBL461297 Ki = 0.035 nM 10.46
CHEMBL508428 Ki = 0.038 nM 10.42
CHEMBL518648 Ki = 0.042 nM 10.38
CHEMBL513062 Ki = 0.054 nM 10.27
CHEMBL511486 Ki = 0.055 nM 10.26
CHEMBL471565 Ki = 0.064 nM 10.19
CHEMBL471734 Ki = 0.074 nM 10.13
CHEMBL461090 Ki = 0.12 nM 9.92
CHEMBL517711 Ki = 0.14 nM 9.85
CHEMBL479925 Ki = 0.14 nM 9.85
CHEMBL237226 Ki = 0.15 nM 9.82
CHEMBL460884 Ki = 0.18 nM 9.74
CHEMBL206335 RAZAXABAN Ki = 0.19 nM 9.72
CHEMBL459849 Ki = 0.28 nM 9.55
CHEMBL218525 Ki = 0.3 nM 9.52
CHEMBL517263 Ki = 0.57 nM 9.24
CHEMBL221296 Ki = 0.76 nM 9.12
CHEMBL459430 Ki = 1.4 nM 8.85
CHEMBL452535 Ki = 1.6 nM 8.80
CHEMBL460056 Ki = 1.8 nM 8.74
CHEMBL508927 Ki = 1.8 nM 8.74
CHEMBL452793 Ki = 1.9 nM 8.72
CHEMBL511082 Ki = 2.4 nM 8.62
CHEMBL460681 Ki = 3.0 nM 8.52
CHEMBL507737 Ki = 3.3 nM 8.48
CHEMBL452802 Ki = 5.8 nM 8.24
CHEMBL510344 Ki = 30.0 nM 7.52
CHEMBL460055 Ki = 54.0 nM 7.27
CHEMBL459854 Ki = 169.0 nM 6.77
CHEMBL452524 Ki < 0.02 nM -