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Assay Detail

CHEMBL904425

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

Binding
Inhibition of human TF/FVIIa complex by chromogenic assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Tissue factor (CHEMBL4081)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis and biological activity of selective and orally available TF/FVIIa complex inhibitors containing non-amidine P1 ligands.
Miura M, Seki N, Koike T, Ishihara T, Niimi T, Hirayama F, Shigenaga T, Sakai-Moritani Y, Tagawa A, Kawasaki T, Sakamoto S, Okada M, Ohta M, Tsukamoto S.
Bioorg Med Chem (2007) 15 : 160 -173
PubMed 17064913 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 5.78 7.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL224485 1 7.05
CHEMBL376806 1 6.82
CHEMBL388161 1 6.75
CHEMBL225450 1 6.52
CHEMBL225501 1 6.52
CHEMBL426187 1 6.23
CHEMBL375051 1 6.16
CHEMBL376187 1 6.07
CHEMBL389006 1 5.89
CHEMBL441714 1 5.66
CHEMBL224925 1 5.62
CHEMBL389191 1 5.50
CHEMBL388402 1 5.38
CHEMBL225185 1 5.38
CHEMBL374175 1 5.07
CHEMBL390784 1 4.72
CHEMBL225322 1 4.72
CHEMBL376188 1 4.04
CHEMBL225130 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL224485 IC50 = 89.0 nM 7.05
CHEMBL376806 IC50 = 150.0 nM 6.82
CHEMBL388161 IC50 = 180.0 nM 6.75
CHEMBL225450 IC50 = 300.0 nM 6.52
CHEMBL225501 IC50 = 300.0 nM 6.52
CHEMBL426187 IC50 = 590.0 nM 6.23
CHEMBL375051 IC50 = 690.0 nM 6.16
CHEMBL376187 IC50 = 860.0 nM 6.07
CHEMBL389006 IC50 = 1300.0 nM 5.89
CHEMBL441714 IC50 = 2200.0 nM 5.66
CHEMBL224925 IC50 = 2400.0 nM 5.62
CHEMBL389191 IC50 = 3200.0 nM 5.50
CHEMBL388402 IC50 = 4200.0 nM 5.38
CHEMBL225185 IC50 = 4200.0 nM 5.38
CHEMBL374175 IC50 = 8500.0 nM 5.07
CHEMBL390784 IC50 = 19000.0 nM 4.72
CHEMBL225322 IC50 = 19000.0 nM 4.72
CHEMBL376188 IC50 = 91000.0 nM 4.04
CHEMBL225130 IC50 = 191000.0 nM -