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Assay Detail

CHEMBL813670

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

Binding
In vitro inhibition of human thrombin(FIIa).
ChEMBL ↗
44
Total Activities
44
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

Synthesis, characterization, and structure-activity relationships of amidine-substituted (bis)benzylidene-cycloketone olefin isomers as potent and selective factor Xa inhibitors.
Guilford WJ, Shaw KJ, Dallas JL, Koovakkat S, Lee W, Liang A, Light DR, McCarrick MA, Whitlow M, Ye B, Morrissey MM.
J Med Chem (1999) 42 : 5415 -5425
PubMed 10639283 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 44 6.01 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL358910 — — 1 6.96
CHEMBL151481 — — 1 6.92
CHEMBL151049 — — 1 6.92
CHEMBL94336 — — 1 6.89
CHEMBL356862 — — 1 6.82
CHEMBL422321 — — 1 6.70
CHEMBL150739 — — 1 6.54
CHEMBL358918 — — 1 6.52
CHEMBL150612 — — 1 6.49
CHEMBL357795 — — 1 6.46
CHEMBL151480 — — 1 6.46
CHEMBL356630 — — 1 6.44
CHEMBL345492 — — 1 6.42
CHEMBL55035 — — 1 6.28
CHEMBL151293 — — 1 6.22
CHEMBL151661 — — 1 6.20
CHEMBL149410 — — 1 6.20
CHEMBL150434 — — 1 6.14
CHEMBL355969 — — 1 6.13
CHEMBL150277 — — 1 6.09
CHEMBL325022 — — 1 6.00
CHEMBL151144 — — 1 5.96
CHEMBL331437 — — 1 5.85
CHEMBL356466 — — 1 5.85
CHEMBL151562 — — 1 5.80
CHEMBL358180 — — 1 5.77
CHEMBL326552 — — 1 5.68
CHEMBL150309 — — 1 5.68
CHEMBL150962 — — 1 5.66
CHEMBL150138 — — 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL358910 — Ki = 110.0 nM 6.96
CHEMBL151481 — Ki = 120.0 nM 6.92
CHEMBL151049 — Ki = 120.0 nM 6.92
CHEMBL94336 — Ki = 130.0 nM 6.89
CHEMBL356862 — Ki = 150.0 nM 6.82
CHEMBL422321 — Ki = 200.0 nM 6.70
CHEMBL150739 — Ki = 290.0 nM 6.54
CHEMBL358918 — Ki = 300.0 nM 6.52
CHEMBL150612 — Ki = 325.0 nM 6.49
CHEMBL357795 — Ki = 350.0 nM 6.46
CHEMBL151480 — Ki = 350.0 nM 6.46
CHEMBL356630 — Ki = 360.0 nM 6.44
CHEMBL345492 — Ki = 380.0 nM 6.42
CHEMBL55035 — Ki = 530.0 nM 6.28
CHEMBL151293 — Ki = 600.0 nM 6.22
CHEMBL151661 — Ki = 630.0 nM 6.20
CHEMBL149410 — Ki = 630.0 nM 6.20
CHEMBL150434 — Ki = 730.0 nM 6.14
CHEMBL355969 — Ki = 740.0 nM 6.13
CHEMBL150277 — Ki = 810.0 nM 6.09
CHEMBL325022 — Ki = 1000.0 nM 6.00
CHEMBL151144 — Ki = 1100.0 nM 5.96
CHEMBL331437 — Ki = 1400.0 nM 5.85
CHEMBL356466 — Ki = 1400.0 nM 5.85
CHEMBL151562 — Ki = 1600.0 nM 5.80
CHEMBL358180 — Ki = 1700.0 nM 5.77
CHEMBL326552 — Ki = 2100.0 nM 5.68
CHEMBL150309 — Ki = 2100.0 nM 5.68
CHEMBL150962 — Ki = 2200.0 nM 5.66
CHEMBL150138 — Ki = 2900.0 nM 5.54
CHEMBL150308 — Ki = 3000.0 nM 5.52
CHEMBL348671 — Ki = 3300.0 nM 5.48
CHEMBL359275 — Ki = 3700.0 nM 5.43
CHEMBL153659 — Ki = 3700.0 nM 5.43
CHEMBL345990 — Ki = 4400.0 nM 5.36
CHEMBL48233 — Ki = 6200.0 nM 5.21
CHEMBL153660 — Ki = 12850.0 nM 4.89
CHEMBL149960 — Ki = 19200.0 nM 4.72
CHEMBL345710 — Ki = 21500.0 nM 4.67
CHEMBL151164 — Ki > 50000.0 nM -
CHEMBL150718 — Ki > 5000.0 nM -
CHEMBL151113 — Ki > 5000.0 nM -
CHEMBL357083 — Ki > 5000.0 nM -
CHEMBL150547 — Ki > 500.0 nM -