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Assay Detail

CHEMBL658079

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

Binding
Inhibitory constant against human coagulation factor II (thrombin) for selectivity within coagulation cascade
ChEMBL ↗
72
Total Activities
72
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

Design, synthesis, and activity of a novel series of factor Xa inhibitors: optimization of arylamidine groups.
Phillips G, Guilford WJ, Buckman BO, Davey DD, Eagen KA, Koovakkat S, Liang A, McCarrick M, Mohan R, Ng HP, Pinkerton M, Subramanyam B, Ho E, Trinh L, Whitlow M, Wu S, Xu W, Morrissey MM.
J Med Chem (2002) 45 : 2484 -2493
PubMed 12036356 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 72 5.83 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL84437 — — 1 6.92
CHEMBL309541 — — 1 6.75
CHEMBL82925 — — 1 6.72
CHEMBL84275 — — 1 6.52
CHEMBL79303 — — 1 6.31
CHEMBL79828 — — 1 6.19
CHEMBL309879 — — 1 6.17
CHEMBL314591 — — 1 6.14
CHEMBL420963 — — 1 6.13
CHEMBL84065 — — 1 6.09
CHEMBL79529 — — 1 6.06
CHEMBL84419 — — 1 6.02
CHEMBL419651 — — 1 5.96
CHEMBL82456 — — 1 5.92
CHEMBL310373 — — 1 5.85
CHEMBL310575 — — 1 5.75
CHEMBL81632 — — 1 5.66
CHEMBL79986 — — 1 5.64
CHEMBL83675 — — 1 5.58
CHEMBL83106 — — 1 5.52
CHEMBL432939 — — 1 5.47
CHEMBL82831 — — 1 5.42
CHEMBL441450 — — 1 5.31
CHEMBL82006 — — 1 5.29
CHEMBL84502 — — 1 5.28
CHEMBL419661 — — 1 5.28
CHEMBL49636 — — 1 4.66
CHEMBL48604 — — 1 4.57
CHEMBL79258 — — 1 -
CHEMBL81852 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL84437 — Ki = 120.0 nM 6.92
CHEMBL309541 — Ki = 180.0 nM 6.75
CHEMBL82925 — Ki = 190.0 nM 6.72
CHEMBL84275 — Ki = 300.0 nM 6.52
CHEMBL79303 — Ki = 490.0 nM 6.31
CHEMBL79828 — Ki = 650.0 nM 6.19
CHEMBL309879 — Ki = 680.0 nM 6.17
CHEMBL314591 — Ki = 730.0 nM 6.14
CHEMBL420963 — Ki = 740.0 nM 6.13
CHEMBL84065 — Ki = 810.0 nM 6.09
CHEMBL79529 — Ki = 880.0 nM 6.06
CHEMBL84419 — Ki = 950.0 nM 6.02
CHEMBL419651 — Ki = 1100.0 nM 5.96
CHEMBL82456 — Ki = 1200.0 nM 5.92
CHEMBL310373 — Ki = 1400.0 nM 5.85
CHEMBL310575 — Ki = 1800.0 nM 5.75
CHEMBL81632 — Ki = 2200.0 nM 5.66
CHEMBL79986 — Ki = 2300.0 nM 5.64
CHEMBL83675 — Ki = 2600.0 nM 5.58
CHEMBL83106 — Ki = 3000.0 nM 5.52
CHEMBL432939 — Ki = 3400.0 nM 5.47
CHEMBL82831 — Ki = 3800.0 nM 5.42
CHEMBL441450 — Ki = 4900.0 nM 5.31
CHEMBL82006 — Ki = 5100.0 nM 5.29
CHEMBL419661 — Ki = 5300.0 nM 5.28
CHEMBL84502 — Ki = 5300.0 nM 5.28
CHEMBL49636 — Ki = 22000.0 nM 4.66
CHEMBL48604 — Ki = 27000.0 nM 4.57
CHEMBL70730 — Ki > 5000.0 nM -
CHEMBL315014 — Ki > 5000.0 nM -
CHEMBL82739 — Ki > 5000.0 nM -
CHEMBL81932 — Ki > 5000.0 nM -
CHEMBL84030 — Ki > 5000.0 nM -
CHEMBL81893 — Ki > 5000.0 nM -
CHEMBL83175 — Ki > 5000.0 nM -
CHEMBL83925 — Ki > 5000.0 nM -
CHEMBL309617 — Ki > 5000.0 nM -
CHEMBL311608 — Ki > 5000.0 nM -
CHEMBL82339 — Ki > 5000.0 nM -
CHEMBL83431 — Ki > 5000.0 nM -
CHEMBL81579 — Ki > 5000.0 nM -
CHEMBL83798 — Ki > 5000.0 nM -
CHEMBL83648 — Ki > 5000.0 nM -
CHEMBL83324 — Ki > 5000.0 nM -
CHEMBL84379 — Ki > 5000.0 nM -
CHEMBL82873 — Ki > 5000.0 nM -
CHEMBL312275 — Ki > 5000.0 nM -
CHEMBL81301 — Ki > 5000.0 nM -
CHEMBL81852 — Ki > 5000.0 nM -
CHEMBL79258 — Ki > 5000.0 nM -