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Assay Detail

CHEMBL892965

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

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 Intermediate

Target

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

Publication

Prodrug-based design, synthesis, and biological evaluation of N-benzenesulfonylpiperidine derivatives as novel, orally active factor Xa inhibitors.
Ishihara T, Seki N, Hirayama F, Orita M, Koshio H, Taniuchi Y, Sakai-Moritani Y, Iwatsuki Y, Kaku S, Kawasaki T, Matsumoto Y, Tsukamoto S.
Bioorg Med Chem (2007) 15 : 4175 -4192
PubMed 17416533 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 6.90 8.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL244640 1 8.09
CHEMBL390266 1 8.00
CHEMBL244219 1 7.96
CHEMBL244221 1 7.92
CHEMBL244436 1 7.89
CHEMBL244641 1 7.89
CHEMBL244014 1 7.41
CHEMBL19902 DX-9065A 1 7.40
CHEMBL242500 1 7.31
CHEMBL244015 1 7.24
CHEMBL243804 1 7.19
CHEMBL243402 1 7.05
CHEMBL243805 1 7.00
CHEMBL242928 1 6.77
CHEMBL389976 1 6.72
CHEMBL242929 1 6.70
CHEMBL397489 1 6.60
CHEMBL242125 1 6.46
CHEMBL243592 1 6.25
CHEMBL244435 1 6.23
CHEMBL387790 1 6.10
CHEMBL241911 1 6.07
CHEMBL242124 1 6.02
CHEMBL242715 1 5.80
CHEMBL243153 1 5.77
CHEMBL243154 1 5.64
CHEMBL242501 1 -
CHEMBL396028 1 -
CHEMBL241910 1 -
CHEMBL243368 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL244640 IC50 = 8.1 nM 8.09
CHEMBL390266 IC50 = 10.0 nM 8.00
CHEMBL244219 IC50 = 11.0 nM 7.96
CHEMBL244221 IC50 = 12.0 nM 7.92
CHEMBL244436 IC50 = 13.0 nM 7.89
CHEMBL244641 IC50 = 13.0 nM 7.89
CHEMBL244014 IC50 = 39.0 nM 7.41
CHEMBL19902 DX-9065A IC50 = 40.0 nM 7.40
CHEMBL242500 IC50 = 49.0 nM 7.31
CHEMBL244015 IC50 = 58.0 nM 7.24
CHEMBL243804 IC50 = 65.0 nM 7.19
CHEMBL243402 IC50 = 90.0 nM 7.05
CHEMBL243805 IC50 = 100.0 nM 7.00
CHEMBL242928 IC50 = 170.0 nM 6.77
CHEMBL389976 IC50 = 190.0 nM 6.72
CHEMBL242929 IC50 = 200.0 nM 6.70
CHEMBL397489 IC50 = 250.0 nM 6.60
CHEMBL242125 IC50 = 350.0 nM 6.46
CHEMBL243592 IC50 = 560.0 nM 6.25
CHEMBL244435 IC50 = 590.0 nM 6.23
CHEMBL387790 IC50 = 800.0 nM 6.10
CHEMBL241911 IC50 = 850.0 nM 6.07
CHEMBL242124 IC50 = 950.0 nM 6.02
CHEMBL242715 IC50 = 1600.0 nM 5.80
CHEMBL243153 IC50 = 1700.0 nM 5.77
CHEMBL243154 IC50 = 2300.0 nM 5.64
CHEMBL242501 IC50 > 100000.0 nM -
CHEMBL396028 IC50 > 100000.0 nM -
CHEMBL241910 IC50 > 100000.0 nM -
CHEMBL243368 IC50 > 100000.0 nM -
CHEMBL243370 IC50 > 100000.0 nM -
CHEMBL243591 IC50 > 100000.0 nM -