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Assay Detail

CHEMBL3887451

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

Binding
In Vitro Assay: FVIIa-Xase Ki (37° C.): S2765 (0.5 mM), PCPS (25 μM), calcium chloride (5 mM), full-length human TF (3 nM), human FVIIa (5 pM), and FVIIa inhibitor were incubated for 15 min at 37° C. Reactions were initiated by the addition of human FX (range of concentrations). Preliminary experiments revealed that the plasma purified FX contains a residual amount of human FVIIa which could not be removed by affinity chromatography. The residual FVIIa is sufficient, when combined with PCPS, calcium and TF to catalyze the conversion of FX to Xa, and was increased by the addition of 5 pM human FVIIa. FXa in turn hydrolyses S2765, which was monitored for 60 min at 405 nm.
ChEMBL ↗
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Plasma
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Coagulation factor VII (CHEMBL3991) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Macrocyclic factor VIIa inhibitors
(2015)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 43 9.31 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3930738 — — 1 10.70
CHEMBL3986081 — — 1 10.30
CHEMBL3902759 — — 1 9.92
CHEMBL3969432 — — 1 9.85
CHEMBL3903215 — — 1 9.85
CHEMBL3967595 — — 1 9.85
CHEMBL3977297 — — 1 9.85
CHEMBL3906646 — — 1 9.82
CHEMBL3961226 — — 1 9.77
CHEMBL3915633 — — 1 9.77
CHEMBL3891120 — — 1 9.77
CHEMBL3920165 — — 1 9.70
CHEMBL3892246 — — 1 9.64
CHEMBL3901391 — — 1 9.64
CHEMBL3901206 — — 1 9.60
CHEMBL3973659 — — 1 9.55
CHEMBL3897709 — — 1 9.52
CHEMBL3949417 — — 1 9.51
CHEMBL3970623 — — 1 9.47
CHEMBL3908500 — — 1 9.44
CHEMBL3902498 — — 1 9.37
CHEMBL3913920 — — 1 9.36
CHEMBL3983744 — — 1 9.34
CHEMBL3922904 — — 1 9.30
CHEMBL3898371 — — 1 9.26
CHEMBL3917434 — — 1 9.24
CHEMBL3956442 — — 1 9.21
CHEMBL3980787 — — 1 9.21
CHEMBL3917941 — — 1 9.18
CHEMBL3979309 — — 1 9.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3930738 — Ki = 0.02 nM 10.70
CHEMBL3986081 — Ki = 0.05 nM 10.30
CHEMBL3902759 — Ki = 0.12 nM 9.92
CHEMBL3969432 — Ki = 0.14 nM 9.85
CHEMBL3903215 — Ki = 0.14 nM 9.85
CHEMBL3967595 — Ki = 0.14 nM 9.85
CHEMBL3977297 — Ki = 0.14 nM 9.85
CHEMBL3906646 — Ki = 0.15 nM 9.82
CHEMBL3961226 — Ki = 0.17 nM 9.77
CHEMBL3915633 — Ki = 0.17 nM 9.77
CHEMBL3891120 — Ki = 0.17 nM 9.77
CHEMBL3920165 — Ki = 0.2 nM 9.70
CHEMBL3892246 — Ki = 0.23 nM 9.64
CHEMBL3901391 — Ki = 0.23 nM 9.64
CHEMBL3901206 — Ki = 0.25 nM 9.60
CHEMBL3973659 — Ki = 0.28 nM 9.55
CHEMBL3897709 — Ki = 0.3 nM 9.52
CHEMBL3949417 — Ki = 0.31 nM 9.51
CHEMBL3970623 — Ki = 0.34 nM 9.47
CHEMBL3908500 — Ki = 0.36 nM 9.44
CHEMBL3902498 — Ki = 0.43 nM 9.37
CHEMBL3913920 — Ki = 0.44 nM 9.36
CHEMBL3983744 — Ki = 0.46 nM 9.34
CHEMBL3922904 — Ki = 0.5 nM 9.30
CHEMBL3898371 — Ki = 0.55 nM 9.26
CHEMBL3917434 — Ki = 0.57 nM 9.24
CHEMBL3956442 — Ki = 0.61 nM 9.21
CHEMBL3980787 — Ki = 0.62 nM 9.21
CHEMBL3917941 — Ki = 0.66 nM 9.18
CHEMBL3979309 — Ki = 0.9 nM 9.05
CHEMBL3909009 — Ki = 1.0 nM 9.00
CHEMBL4114547 — Ki = 1.1 nM 8.96
CHEMBL3907868 — Ki = 1.2 nM 8.92
CHEMBL3951355 — Ki = 1.2 nM 8.92
CHEMBL3895397 — Ki = 1.8 nM 8.74
CHEMBL4106751 — Ki = 2.0 nM 8.70
CHEMBL4113473 — Ki = 2.2 nM 8.66
CHEMBL3939509 — Ki = 2.3 nM 8.64
CHEMBL4108610 — Ki = 2.3 nM 8.64
CHEMBL3930523 — Ki = 2.5 nM 8.60
CHEMBL4108209 — Ki = 11.0 nM 7.96
CHEMBL4110036 — Ki = 38.0 nM 7.42
CHEMBL3808399 — Ki > 140.0 nM -