Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL813627

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

Binding
Inhibitory potency was measured against human thrombin
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Prothrombin (CHEMBL204)
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 31 5.84 6.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL332322 1 6.90
CHEMBL331213 1 6.85
CHEMBL309541 1 6.75
CHEMBL331690 1 6.72
CHEMBL120438 1 6.72
CHEMBL332189 1 6.60
CHEMBL332388 1 6.55
CHEMBL55035 1 6.28
CHEMBL298415 1 6.26
CHEMBL333266 1 6.20
CHEMBL84065 1 6.09
CHEMBL419651 1 5.96
CHEMBL79303 1 5.96
CHEMBL330802 1 5.92
CHEMBL49786 1 5.85
CHEMBL310373 1 5.85
CHEMBL73193 FIDEXABAN 2.0 1 5.70
CHEMBL79986 1 5.64
CHEMBL83675 1 5.58
CHEMBL72318 1 5.35
CHEMBL50127 1 4.85
CHEMBL70730 1 4.82
CHEMBL312378 1 4.66
CHEMBL49636 1 4.66
CHEMBL48604 1 4.57
CHEMBL424036 1 4.43
CHEMBL311608 1 -
CHEMBL315014 1 -
CHEMBL48864 1 -
CHEMBL81852 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL332322 Ki = 125.0 nM 6.90
CHEMBL331213 Ki = 140.0 nM 6.85
CHEMBL309541 Ki = 180.0 nM 6.75
CHEMBL331690 Ki = 190.0 nM 6.72
CHEMBL120438 Ki = 192.0 nM 6.72
CHEMBL332189 Ki = 250.0 nM 6.60
CHEMBL332388 Ki = 280.0 nM 6.55
CHEMBL55035 Ki = 530.0 nM 6.28
CHEMBL298415 Ki = 550.0 nM 6.26
CHEMBL333266 Ki = 630.0 nM 6.20
CHEMBL84065 Ki = 810.0 nM 6.09
CHEMBL419651 Ki = 1100.0 nM 5.96
CHEMBL79303 Ki = 1100.0 nM 5.96
CHEMBL330802 Ki = 1200.0 nM 5.92
CHEMBL49786 Ki = 1400.0 nM 5.85
CHEMBL310373 Ki = 1400.0 nM 5.85
CHEMBL73193 FIDEXABAN Ki = 2000.0 nM 5.70
CHEMBL79986 Ki = 2300.0 nM 5.64
CHEMBL83675 Ki = 2600.0 nM 5.58
CHEMBL72318 Ki = 4500.0 nM 5.35
CHEMBL50127 Ki = 14000.0 nM 4.85
CHEMBL70730 Ki = 15000.0 nM 4.82
CHEMBL312378 Ki = 22000.0 nM 4.66
CHEMBL49636 Ki = 22000.0 nM 4.66
CHEMBL48604 Ki = 27000.0 nM 4.57
CHEMBL424036 Ki = 37000.0 nM 4.43
CHEMBL311608 Ki > 5000.0 nM -
CHEMBL315014 Ki > 5000.0 nM -
CHEMBL48864 Ki > 5000.0 nM -
CHEMBL81852 Ki > 5000.0 nM -
CHEMBL81579 Ki > 5000.0 nM -