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Assay Detail

CHEMBL1035202

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

Binding
Inhibition of tissue factor/factor 7a
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Coagulation factor VII/tissue factor (CHEMBL2095194)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Design, parallel synthesis, and crystal structures of biphenyl antithrombotics as selective inhibitors of tissue factor FVIIa complex. Part 1: Exploration of S2 pocket pharmacophores.
Kotian PL, Krishnan R, Rowland S, El-Kattan Y, Saini SK, Upshaw R, Bantia S, Arnold S, Babu YS, Chand P.
Bioorg Med Chem (2009) 17 : 3934 -3958
PubMed 19409795 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 45 10.17 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL505190 1 11.00
CHEMBL505189 1 11.00
CHEMBL484616 1 10.96
CHEMBL506771 1 10.96
CHEMBL526504 1 10.96
CHEMBL523251 1 10.92
CHEMBL520364 1 10.89
CHEMBL506772 1 10.85
CHEMBL524370 1 10.70
CHEMBL524732 1 10.68
CHEMBL503584 1 10.62
CHEMBL487956 1 10.60
CHEMBL507281 1 10.54
CHEMBL488778 1 10.52
CHEMBL507020 1 10.48
CHEMBL484615 1 10.47
CHEMBL499632 1 10.44
CHEMBL487955 1 10.38
CHEMBL505720 1 10.35
CHEMBL497067 1 10.28
CHEMBL498047 1 10.22
CHEMBL519886 1 10.17
CHEMBL527118 1 10.12
CHEMBL500948 1 10.04
CHEMBL485705 1 10.01
CHEMBL525274 1 10.01
CHEMBL524548 1 9.98
CHEMBL224485 1 9.92
CHEMBL526193 1 9.89
CHEMBL499829 1 9.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL505190 IC50 = 0.01 nM 11.00
CHEMBL505189 IC50 = 0.01 nM 11.00
CHEMBL506771 IC50 = 0.011 nM 10.96
CHEMBL526504 IC50 = 0.011 nM 10.96
CHEMBL484616 IC50 = 0.011 nM 10.96
CHEMBL523251 IC50 = 0.012 nM 10.92
CHEMBL520364 IC50 = 0.013 nM 10.89
CHEMBL506772 IC50 = 0.014 nM 10.85
CHEMBL524370 IC50 = 0.02 nM 10.70
CHEMBL524732 IC50 = 0.021 nM 10.68
CHEMBL503584 IC50 = 0.024 nM 10.62
CHEMBL487956 IC50 = 0.025 nM 10.60
CHEMBL507281 IC50 = 0.029 nM 10.54
CHEMBL488778 IC50 = 0.03 nM 10.52
CHEMBL507020 IC50 = 0.033 nM 10.48
CHEMBL484615 IC50 = 0.034 nM 10.47
CHEMBL499632 IC50 = 0.036 nM 10.44
CHEMBL487955 IC50 = 0.042 nM 10.38
CHEMBL505720 IC50 = 0.045 nM 10.35
CHEMBL497067 IC50 = 0.052 nM 10.28
CHEMBL498047 IC50 = 0.06 nM 10.22
CHEMBL519886 IC50 = 0.067 nM 10.17
CHEMBL527118 IC50 = 0.076 nM 10.12
CHEMBL500948 IC50 = 0.092 nM 10.04
CHEMBL485705 IC50 = 0.097 nM 10.01
CHEMBL525274 IC50 = 0.098 nM 10.01
CHEMBL524548 IC50 = 0.104 nM 9.98
CHEMBL224485 IC50 = 0.12 nM 9.92
CHEMBL526193 IC50 = 0.13 nM 9.89
CHEMBL499829 IC50 = 0.19 nM 9.72
CHEMBL504391 IC50 = 0.231 nM 9.64
CHEMBL502557 IC50 = 0.32 nM 9.49
CHEMBL502292 IC50 = 0.33 nM 9.48
CHEMBL501749 IC50 = 0.5 nM 9.30
CHEMBL504657 IC50 = 0.546 nM 9.26
CHEMBL501218 IC50 = 0.65 nM 9.19
CHEMBL500947 IC50 = 0.926 nM 9.03
CHEMBL498726 IC50 = 1.22 nM 8.91
CHEMBL498545 IC50 = 1.61 nM 8.79
CHEMBL451066 IC50 = 0.009 nM -
CHEMBL502293 IC50 = 0.009 nM -
CHEMBL505455 IC50 = 0.009 nM -
CHEMBL486112 IC50 = 0.009 nM -
CHEMBL485704 IC50 = 0.009 nM -
CHEMBL507279 IC50 = 0.008 nM -