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Assay Detail

CHEMBL658338

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Binding
Binding affinity against human coagulation factor X
33
Total Activities
33
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

Development of serine protease inhibitors displaying a multicentered short (<2.3 A) hydrogen bond binding mode: inhibitors of urokinase-type plasminogen activator and factor Xa.
Verner E, Katz BA, Spencer JR, Allen D, Hataye J, Hruzewicz W, Hui HC, Kolesnikov A, Li Y, Luong C, Martelli A, Radika K, Rai R, She M, Shrader W, Sprengeler PA, Trapp S, Wang J, Young WB, Mackman RL.
J Med Chem (2001) 44 : 2753 -2771
PubMed 11495587 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 33 5.76 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL94775 1 7.85
CHEMBL328772 1 7.37
CHEMBL48608 1 7.28
CHEMBL96433 1 7.11
CHEMBL316334 1 7.11
CHEMBL330234 1 7.05
CHEMBL91962 1 6.68
CHEMBL52427 1 6.68
CHEMBL330244 1 6.52
CHEMBL92883 1 6.47
CHEMBL95097 1 6.24
CHEMBL96494 1 6.05
CHEMBL92251 1 6.03
CHEMBL327789 1 5.89
CHEMBL327715 1 5.68
CHEMBL284805 1 5.57
CHEMBL93269 1 5.30
CHEMBL94254 1 5.24
CHEMBL92277 1 5.17
CHEMBL318363 1 5.17
CHEMBL92250 1 5.11
CHEMBL96493 1 5.05
CHEMBL92865 1 5.03
CHEMBL319997 1 5.00
CHEMBL92964 1 5.00
CHEMBL433501 1 4.85
CHEMBL433179 1 4.80
CHEMBL94139 1 4.80
CHEMBL318526 1 4.72
CHEMBL330460 1 4.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL94775 Ki = 14.0 nM 7.85
CHEMBL328772 Ki = 43.0 nM 7.37
CHEMBL48608 Ki = 52.0 nM 7.28
CHEMBL96433 Ki = 78.0 nM 7.11
CHEMBL316334 Ki = 78.0 nM 7.11
CHEMBL330234 Ki = 89.0 nM 7.05
CHEMBL91962 Ki = 210.0 nM 6.68
CHEMBL52427 Ki = 210.0 nM 6.68
CHEMBL330244 Ki = 300.0 nM 6.52
CHEMBL92883 Ki = 340.0 nM 6.47
CHEMBL95097 Ki = 570.0 nM 6.24
CHEMBL96494 Ki = 890.0 nM 6.05
CHEMBL92251 Ki = 940.0 nM 6.03
CHEMBL327789 Ki = 1300.0 nM 5.89
CHEMBL327715 Ki = 2100.0 nM 5.68
CHEMBL284805 Ki = 2700.0 nM 5.57
CHEMBL93269 Ki = 5000.0 nM 5.30
CHEMBL94254 Ki = 5700.0 nM 5.24
CHEMBL92277 Ki = 6800.0 nM 5.17
CHEMBL318363 Ki = 6800.0 nM 5.17
CHEMBL92250 Ki = 7800.0 nM 5.11
CHEMBL96493 Ki = 8900.0 nM 5.05
CHEMBL92865 Ki = 9400.0 nM 5.03
CHEMBL319997 Ki = 9900.0 nM 5.00
CHEMBL92964 Ki = 10000.0 nM 5.00
CHEMBL433501 Ki = 14000.0 nM 4.85
CHEMBL433179 Ki = 16000.0 nM 4.80
CHEMBL94139 Ki = 16000.0 nM 4.80
CHEMBL318526 Ki = 19000.0 nM 4.72
CHEMBL330460 Ki = 25000.0 nM 4.60
CHEMBL96428 Ki = 30000.0 nM 4.52
CHEMBL321510 Ki = 43000.0 nM 4.37
CHEMBL96917 Ki = 125000.0 nM -