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Assay Detail

CHEMBL3855495

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

Binding
Inhibition of recombinant human TF-factor 7a using factor 10 as substrate at 37 degC
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and P1' SAR exploration of potent macrocyclic tissue factor-factor VIIa inhibitors.
Ladziata VU, Glunz PW, Zou Y, Zhang X, Jiang W, Jacutin-Porte S, Cheney DL, Wei A, Luettgen JM, Harper TM, Wong PC, Seiffert D, Wexler RR, Priestley ES.
Bioorg Med Chem Lett (2016) 26 : 5051 -5057
PubMed 27612545 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 9.18 10.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3956096 1 10.22
CHEMBL3900166 1 9.85
CHEMBL3984725 1 9.66
CHEMBL3898371 1 9.26
CHEMBL3967204 1 9.14
CHEMBL3895930 1 8.36
CHEMBL3934882 1 7.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3956096 Ki = 0.06 nM 10.22
CHEMBL3900166 Ki = 0.14 nM 9.85
CHEMBL3984725 Ki = 0.22 nM 9.66
CHEMBL3898371 Ki = 0.55 nM 9.26
CHEMBL3967204 Ki = 0.72 nM 9.14
CHEMBL3895930 Ki = 4.4 nM 8.36
CHEMBL3934882 Ki = 18.0 nM 7.75