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Assay Detail

CHEMBL5733793

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Binding
Inhibition Assay: Factor XIa determinations were made in 50 mM HEPES buffer at pH 7.4 containing 145 mM NaCl, 5 mM KCl, and 0.1% PEG 8000 (polyethylene glycol; JT Baker or Fisher Scientific). Determinations were made using purified human Factor XIa at a final concentration of 25-200 pM (Haematologic Technologies) and the synthetic substrate S-2366 (pyroGlu-Pro-Arg-pNA; CHROMOGENIX® or AnaSpec) at a concentration of 0.0002-0.001 M.
ChEMBL ↗
675
Total Activities
216
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

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

Target

Coagulation factor XI (CHEMBL2820) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Dihydropyridone P1 as factor XIa inhibitors
(2018)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 225 8.26 10.52
kon 225 - -
k_off 225 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4107149 — — 3 10.52
CHEMBL4110926 — — 3 10.40
CHEMBL4112773 — — 3 10.30
CHEMBL4114881 — — 3 10.30
CHEMBL4113483 — — 3 10.22
CHEMBL4109568 — — 3 10.22
CHEMBL4108033 — — 3 10.15
CHEMBL4115630 — — 3 10.10
CHEMBL4110983 — — 3 10.10
CHEMBL4111429 — — 3 10.05
CHEMBL4106708 — — 3 10.05
CHEMBL3948120 — — 3 10.05
CHEMBL4113824 — — 3 10.05
CHEMBL4114933 — — 3 10.00
CHEMBL4107808 — — 3 10.00
CHEMBL4115423 — — 3 9.96
CHEMBL4110346 — — 3 9.89
CHEMBL4110901 — — 3 9.82
CHEMBL4107795 — — 3 9.77
CHEMBL4115353 — — 3 9.74
CHEMBL4112648 — — 3 9.70
CHEMBL4114611 — — 3 9.68
CHEMBL4114880 — — 3 9.64
CHEMBL4112546 — — 3 9.64
CHEMBL4112357 — — 3 9.57
CHEMBL4109665 — — 3 9.51
CHEMBL4111371 — — 3 9.42
CHEMBL4112342 — — 3 9.38
CHEMBL4106934 — — 3 9.36
CHEMBL4107368 — — 3 9.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4107149 — Ki = 0.03 nM 10.52
CHEMBL4110926 — Ki = 0.04 nM 10.40
CHEMBL4112773 — Ki = 0.05 nM 10.30
CHEMBL4114881 — Ki = 0.05 nM 10.30
CHEMBL4113483 — Ki = 0.06 nM 10.22
CHEMBL4109568 — Ki = 0.06 nM 10.22
CHEMBL4108033 — Ki = 0.07 nM 10.15
CHEMBL4110983 — Ki = 0.08 nM 10.10
CHEMBL4115630 — Ki = 0.08 nM 10.10
CHEMBL4113824 — Ki = 0.09 nM 10.05
CHEMBL4106708 — Ki = 0.09 nM 10.05
CHEMBL3948120 — Ki = 0.09 nM 10.05
CHEMBL4111429 — Ki = 0.09 nM 10.05
CHEMBL4114933 — Ki = 0.1 nM 10.00
CHEMBL4107808 — Ki = 0.1 nM 10.00
CHEMBL4115423 — Ki = 0.11 nM 9.96
CHEMBL4110346 — Ki = 0.13 nM 9.89
CHEMBL4110901 — Ki = 0.15 nM 9.82
CHEMBL4107795 — Ki = 0.17 nM 9.77
CHEMBL4115353 — Ki = 0.18 nM 9.74
CHEMBL4112648 — Ki = 0.2 nM 9.70
CHEMBL4114611 — Ki = 0.21 nM 9.68
CHEMBL4114880 — Ki = 0.23 nM 9.64
CHEMBL4112546 — Ki = 0.23 nM 9.64
CHEMBL4112357 — Ki = 0.27 nM 9.57
CHEMBL4109665 — Ki = 0.31 nM 9.51
CHEMBL4111371 — Ki = 0.38 nM 9.42
CHEMBL4112342 — Ki = 0.42 nM 9.38
CHEMBL4106934 — Ki = 0.44 nM 9.36
CHEMBL4107368 — Ki = 0.45 nM 9.35
CHEMBL4112597 — Ki = 0.46 nM 9.34
CHEMBL4111663 — Ki = 0.47 nM 9.33
CHEMBL4109580 — Ki = 0.55 nM 9.26
CHEMBL4112483 — Ki = 0.56 nM 9.25
CHEMBL4111142 — Ki = 0.56 nM 9.25
CHEMBL4111308 — Ki = 0.59 nM 9.23
CHEMBL4113149 — Ki = 0.62 nM 9.21
CHEMBL4114332 — Ki = 0.67 nM 9.17
CHEMBL4115130 — Ki = 0.69 nM 9.16
CHEMBL4114872 — Ki = 0.72 nM 9.14
CHEMBL4113427 — Ki = 0.8 nM 9.10
CHEMBL4112921 — Ki = 0.8 nM 9.10
CHEMBL4113230 — Ki = 0.81 nM 9.09
CHEMBL4109928 — Ki = 0.84 nM 9.08
CHEMBL4112474 — Ki = 0.87 nM 9.06
CHEMBL4112921 — Ki = 0.88 nM 9.06
CHEMBL4110812 — Ki = 0.87 nM 9.06
CHEMBL4110103 — Ki = 0.92 nM 9.04
CHEMBL4112921 — Ki = 0.92 nM 9.04
CHEMBL4113520 — Ki = 0.98 nM 9.01