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Assay Detail

CHEMBL927722

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Binding
Inhibition of human factor 10a
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Coagulation factor X (CHEMBL244)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
Varnes JG, Wacker DA, Pinto DJ, Orwat MJ, Theroff JP, Wells B, Galemo RA, Luettgen JM, Knabb RM, Bai S, He K, Lam PY, Wexler RR.
Bioorg Med Chem Lett (2008) 18 : 749 -754
PubMed 18054227 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 9.18 10.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL378093 1 10.52
CHEMBL252454 1 10.48
CHEMBL403196 1 10.15
CHEMBL252853 1 10.05
CHEMBL403042 1 9.96
CHEMBL253297 1 9.80
CHEMBL206335 RAZAXABAN 2.0 1 9.72
CHEMBL252453 1 9.49
CHEMBL402166 1 9.47
CHEMBL404061 1 9.28
CHEMBL253926 1 9.24
CHEMBL253094 1 9.17
CHEMBL442292 1 9.01
CHEMBL252651 1 9.00
CHEMBL253093 1 8.82
CHEMBL253713 1 8.64
CHEMBL269191 1 8.55
CHEMBL402167 1 8.48
CHEMBL253298 1 8.33
CHEMBL252650 1 8.16
CHEMBL252649 1 7.92
CHEMBL404286 1 7.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL378093 Ki = 0.03 nM 10.52
CHEMBL252454 Ki = 0.033 nM 10.48
CHEMBL403196 Ki = 0.07 nM 10.15
CHEMBL252853 Ki = 0.09 nM 10.05
CHEMBL403042 Ki = 0.11 nM 9.96
CHEMBL253297 Ki = 0.16 nM 9.80
CHEMBL206335 RAZAXABAN Ki = 0.19 nM 9.72
CHEMBL252453 Ki = 0.32 nM 9.49
CHEMBL402166 Ki = 0.34 nM 9.47
CHEMBL404061 Ki = 0.53 nM 9.28
CHEMBL253926 Ki = 0.57 nM 9.24
CHEMBL253094 Ki = 0.68 nM 9.17
CHEMBL442292 Ki = 0.97 nM 9.01
CHEMBL252651 Ki = 1.0 nM 9.00
CHEMBL253093 Ki = 1.5 nM 8.82
CHEMBL253713 Ki = 2.3 nM 8.64
CHEMBL269191 Ki = 2.8 nM 8.55
CHEMBL402167 Ki = 3.3 nM 8.48
CHEMBL253298 Ki = 4.7 nM 8.33
CHEMBL252650 Ki = 6.9 nM 8.16
CHEMBL252649 Ki = 12.0 nM 7.92
CHEMBL404286 Ki = 22.0 nM 7.66