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Assay Detail

CHEMBL661794

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Binding
Inhibitory potency was measured against human coagulation factor X
32
Total Activities
32
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

Discovery of N-[2-[5-[Amino(imino)methyl]-2-hydroxyphenoxy]-3, 5-difluoro-6-[3-(4, 5-dihydro-1-methyl-1H-imidazol-2-yl)phenoxy]pyridin-4-yl]-N-methylgl y cine (ZK-807834): a potent, selective, and orally active inhibitor of the blood coagulation enzyme factor Xa.
Phillips GB, Buckman BO, Davey DD, Eagen KA, Guilford WJ, Hinchman J, Ho E, Koovakkat S, Liang A, Light DR, Mohan R, Ng HP, Post JM, Shaw KJ, Smith D, Subramanyam B, Sullivan ME, Trinh L, Vergona R, Walters J, White K, Whitlow M, Wu S, Xu W, Morrissey MM.
J Med Chem (1998) 41 : 3557 -3562
PubMed 9733480 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 32 7.94 9.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL73193 FIDEXABAN 2.0 1 9.96
CHEMBL332322 1 9.62
CHEMBL333266 1 9.59
CHEMBL331690 1 9.51
CHEMBL332189 1 9.48
CHEMBL72318 1 9.39
CHEMBL331213 1 9.37
CHEMBL120438 1 9.19
CHEMBL55035 1 9.18
CHEMBL332388 1 9.15
CHEMBL419651 1 8.92
CHEMBL84065 1 8.62
CHEMBL79303 1 8.41
CHEMBL309541 1 8.05
CHEMBL49636 1 7.89
CHEMBL79986 1 7.85
CHEMBL424036 1 7.62
CHEMBL310373 1 7.58
CHEMBL50127 1 7.28
CHEMBL48604 1 7.23
CHEMBL70730 1 7.10
CHEMBL315014 1 7.07
CHEMBL330802 1 6.89
CHEMBL48864 1 6.89
CHEMBL83675 1 6.80
CHEMBL81579 1 6.55
CHEMBL298415 1 6.40
CHEMBL49786 1 6.21
CHEMBL312378 1 6.19
CHEMBL311608 1 6.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL73193 FIDEXABAN Ki = 0.11 nM 9.96
CHEMBL332322 Ki = 0.24 nM 9.62
CHEMBL333266 Ki = 0.26 nM 9.59
CHEMBL331690 Ki = 0.31 nM 9.51
CHEMBL332189 Ki = 0.33 nM 9.48
CHEMBL72318 Ki = 0.41 nM 9.39
CHEMBL331213 Ki = 0.43 nM 9.37
CHEMBL120438 Ki = 0.65 nM 9.19
CHEMBL55035 Ki = 0.66 nM 9.18
CHEMBL332388 Ki = 0.71 nM 9.15
CHEMBL419651 Ki = 1.2 nM 8.92
CHEMBL84065 Ki = 2.4 nM 8.62
CHEMBL79303 Ki = 3.9 nM 8.41
CHEMBL309541 Ki = 9.0 nM 8.05
CHEMBL49636 Ki = 13.0 nM 7.89
CHEMBL79986 Ki = 14.0 nM 7.85
CHEMBL424036 Ki = 24.0 nM 7.62
CHEMBL310373 Ki = 26.0 nM 7.58
CHEMBL50127 Ki = 53.0 nM 7.28
CHEMBL48604 Ki = 59.0 nM 7.23
CHEMBL70730 Ki = 80.0 nM 7.10
CHEMBL315014 Ki = 85.0 nM 7.07
CHEMBL330802 Ki = 130.0 nM 6.89
CHEMBL48864 Ki = 130.0 nM 6.89
CHEMBL83675 Ki = 160.0 nM 6.80
CHEMBL81579 Ki = 280.0 nM 6.55
CHEMBL298415 Ki = 400.0 nM 6.40
CHEMBL49786 Ki = 620.0 nM 6.21
CHEMBL312378 Ki = 640.0 nM 6.19
CHEMBL311608 Ki = 740.0 nM 6.13
CHEMBL79735 Ki = 1300.0 nM 5.89
CHEMBL81852 Ki > 5000.0 nM -