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Assay Detail

CHEMBL661582

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Binding
Compound was evaluated for the inhibition of human Coagulation factor Xa
ChEMBL ↗
46
Total Activities
46
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

Design and structure-activity relationships of potent and selective inhibitors of blood coagulation factor Xa.
Ewing WR, Becker MR, Manetta VE, Davis RS, Pauls HW, Mason H, Choi-Sledeski YM, Green D, Cha D, Spada AP, Cheney DL, Mason JS, Maignan S, Guilloteau JP, Brown K, Colussi D, Bentley R, Bostwick J, Kasiewski CJ, Morgan SR, Leadley RJ, Dunwiddie CT, Perrone MH, Chu V.
J Med Chem (1999) 42 : 3557 -3571
PubMed 10479288 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 46 6.82 10.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL118494 — — 1 10.33
CHEMBL331943 — — 1 8.15
CHEMBL118361 — — 1 7.96
CHEMBL119456 — — 1 7.72
CHEMBL119964 — — 1 7.68
CHEMBL333678 — — 1 7.66
CHEMBL419049 — — 1 7.60
CHEMBL118156 — — 1 7.51
CHEMBL116378 — — 1 7.47
CHEMBL340336 — — 1 7.39
CHEMBL324569 — — 1 7.37
CHEMBL327600 — — 1 7.33
CHEMBL325529 — — 1 7.25
CHEMBL331686 — — 1 7.16
CHEMBL331955 — — 1 7.11
CHEMBL331939 — — 1 7.08
CHEMBL332619 — — 1 7.00
CHEMBL119913 — — 1 7.00
CHEMBL333639 — — 1 6.96
CHEMBL93681 — — 1 6.92
CHEMBL324337 — — 1 6.92
CHEMBL120341 — — 1 6.92
CHEMBL333548 — — 1 6.80
CHEMBL120749 — — 1 6.75
CHEMBL332160 — — 1 6.72
CHEMBL435585 — — 1 6.66
CHEMBL93796 — — 1 6.64
CHEMBL331896 — — 1 6.60
CHEMBL409260 — — 1 6.55
CHEMBL117156 — — 1 6.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL118494 — Ki = 0.047 nM 10.33
CHEMBL331943 — Ki = 7.0 nM 8.15
CHEMBL118361 — Ki = 11.0 nM 7.96
CHEMBL119456 — Ki = 19.0 nM 7.72
CHEMBL119964 — Ki = 21.0 nM 7.68
CHEMBL333678 — Ki = 22.0 nM 7.66
CHEMBL419049 — Ki = 25.0 nM 7.60
CHEMBL118156 — Ki = 31.0 nM 7.51
CHEMBL116378 — Ki = 34.0 nM 7.47
CHEMBL340336 — Ki = 41.0 nM 7.39
CHEMBL324569 — Ki = 43.0 nM 7.37
CHEMBL327600 — Ki = 47.0 nM 7.33
CHEMBL325529 — Ki = 56.0 nM 7.25
CHEMBL331686 — Ki = 70.0 nM 7.16
CHEMBL331955 — Ki = 78.0 nM 7.11
CHEMBL331939 — Ki = 83.0 nM 7.08
CHEMBL332619 — Ki = 100.0 nM 7.00
CHEMBL119913 — Ki = 100.0 nM 7.00
CHEMBL333639 — Ki = 110.0 nM 6.96
CHEMBL93681 — Ki = 120.0 nM 6.92
CHEMBL324337 — Ki = 120.0 nM 6.92
CHEMBL120341 — Ki = 120.0 nM 6.92
CHEMBL333548 — Ki = 160.0 nM 6.80
CHEMBL120749 — Ki = 180.0 nM 6.75
CHEMBL332160 — Ki = 190.0 nM 6.72
CHEMBL435585 — Ki = 220.0 nM 6.66
CHEMBL93796 — Ki = 230.0 nM 6.64
CHEMBL331896 — Ki = 250.0 nM 6.60
CHEMBL409260 — Ki = 280.0 nM 6.55
CHEMBL117156 — Ki = 340.0 nM 6.47
CHEMBL118799 — Ki = 370.0 nM 6.43
CHEMBL119249 — Ki = 380.0 nM 6.42
CHEMBL331774 — Ki = 440.0 nM 6.36
CHEMBL333958 — Ki = 440.0 nM 6.36
CHEMBL118334 — Ki = 500.0 nM 6.30
CHEMBL436563 — Ki = 570.0 nM 6.24
CHEMBL331648 — Ki = 750.0 nM 6.12
CHEMBL118906 — Ki = 900.0 nM 6.05
CHEMBL333891 — Ki = 970.0 nM 6.01
CHEMBL419227 — Ki = 1000.0 nM 6.00
CHEMBL326316 — Ki = 1100.0 nM 5.96
CHEMBL118836 — Ki = 1300.0 nM 5.89
CHEMBL121032 — Ki = 7000.0 nM 5.16
CHEMBL120387 — Ki = 9800.0 nM 5.01
CHEMBL120765 — Ki = 9900.0 nM 5.00
CHEMBL326046 — Ki > 10000.0 nM -