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Assay Detail

CHEMBL857526

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Binding
Inhibition constant against human factor Xa
59
Total Activities
59
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Structure-activity relationships of substituted benzothiophene-anthranilamide factor Xa inhibitors.
Chou YL, Davey DD, Eagen KA, Griedel BD, Karanjawala R, Phillips GB, Sacchi KL, Shaw KJ, Wu SC, Lentz D, Liang AM, Trinh L, Morrissey MM, Kochanny MJ.
Bioorg Med Chem Lett (2003) 13 : 507 -511
PubMed 12565961 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 59 7.49 9.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54237 1 9.49
CHEMBL147645 1 9.34
CHEMBL149421 1 9.22
CHEMBL356112 1 8.74
CHEMBL146079 1 8.66
CHEMBL146207 1 8.64
CHEMBL357709 1 8.43
CHEMBL149756 1 8.30
CHEMBL149764 1 8.23
CHEMBL145839 1 8.15
CHEMBL149393 1 8.15
CHEMBL150063 1 8.15
CHEMBL146641 1 8.14
CHEMBL50024 1 7.96
CHEMBL148687 1 7.96
CHEMBL422844 1 7.85
CHEMBL149787 1 7.82
CHEMBL345940 1 7.80
CHEMBL53011 1 7.80
CHEMBL146149 1 7.75
CHEMBL358275 1 7.72
CHEMBL357971 1 7.66
CHEMBL147573 1 7.66
CHEMBL342806 1 7.62
CHEMBL147518 1 7.60
CHEMBL359219 1 7.58
CHEMBL146184 1 7.58
CHEMBL147982 1 7.52
CHEMBL148458 1 7.27
CHEMBL358135 1 7.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54237 Ki = 0.32 nM 9.49
CHEMBL147645 Ki = 0.46 nM 9.34
CHEMBL149421 Ki = 0.6 nM 9.22
CHEMBL356112 Ki = 1.8 nM 8.74
CHEMBL146079 Ki = 2.2 nM 8.66
CHEMBL146207 Ki = 2.3 nM 8.64
CHEMBL357709 Ki = 3.7 nM 8.43
CHEMBL149756 Ki = 5.0 nM 8.30
CHEMBL149764 Ki = 5.9 nM 8.23
CHEMBL145839 Ki = 7.0 nM 8.15
CHEMBL149393 Ki = 7.1 nM 8.15
CHEMBL150063 Ki = 7.0 nM 8.15
CHEMBL146641 Ki = 7.2 nM 8.14
CHEMBL148687 Ki = 11.0 nM 7.96
CHEMBL50024 Ki = 11.0 nM 7.96
CHEMBL422844 Ki = 14.0 nM 7.85
CHEMBL149787 Ki = 15.0 nM 7.82
CHEMBL345940 Ki = 16.0 nM 7.80
CHEMBL53011 Ki = 16.0 nM 7.80
CHEMBL146149 Ki = 18.0 nM 7.75
CHEMBL358275 Ki = 19.0 nM 7.72
CHEMBL357971 Ki = 22.0 nM 7.66
CHEMBL147573 Ki = 22.0 nM 7.66
CHEMBL342806 Ki = 24.0 nM 7.62
CHEMBL147518 Ki = 25.0 nM 7.60
CHEMBL359219 Ki = 26.0 nM 7.58
CHEMBL146184 Ki = 26.0 nM 7.58
CHEMBL147982 Ki = 30.0 nM 7.52
CHEMBL148458 Ki = 54.0 nM 7.27
CHEMBL358135 Ki = 58.0 nM 7.24
CHEMBL146365 Ki = 73.0 nM 7.14
CHEMBL358610 Ki = 78.0 nM 7.11
CHEMBL149657 Ki = 100.0 nM 7.00
CHEMBL149875 Ki = 130.0 nM 6.89
CHEMBL148917 Ki = 150.0 nM 6.82
CHEMBL148791 Ki = 160.0 nM 6.80
CHEMBL146592 Ki = 210.0 nM 6.68
CHEMBL342733 Ki = 210.0 nM 6.68
CHEMBL342551 Ki = 260.0 nM 6.58
CHEMBL149006 Ki = 280.0 nM 6.55
CHEMBL146511 Ki = 390.0 nM 6.41
CHEMBL422134 Ki = 470.0 nM 6.33
CHEMBL345769 Ki = 590.0 nM 6.23
CHEMBL347983 Ki = 960.0 nM 6.02
CHEMBL148036 Ki = 1400.0 nM 5.85
CHEMBL149718 Ki = 4400.0 nM 5.36
CHEMBL150216 Ki = 4700.0 nM 5.33
CHEMBL356132 Ki > 5000.0 nM -
CHEMBL146160 Ki > 5000.0 nM -
CHEMBL148587 Ki > 5000.0 nM -