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Assay Detail

CHEMBL3888872

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Binding
In Vitro Assay: Plasma kallikrein determinations were made in 0.1 M sodium phosphate buffer at a pH of 7.5 containing 0.1-0.2 M sodium chloride and 0.5% PEG 8000. Determinations were made using purified human plasma kallikrein (Enzyme Research Laboratories) at a final assay concentration of 200 pM and the synthetic substrate S-2302 (H-(D)-Pro-Phe-Arg-pNA; CHROMOGENIX®) at a concentration of 0.00008-0.0004 M.
ChEMBL ↗
218
Total Activities
208
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

Plasma kallikrein (CHEMBL2000) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Dihydropyridone p1 as factor XIa inhibitors
(2016)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 218 7.48 9.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4114881 — — 1 9.25
CHEMBL4107149 — — 1 9.00
CHEMBL4108223 — — 1 9.00
CHEMBL4110103 — — 1 9.00
CHEMBL4106988 — — 1 9.00
CHEMBL4107104 — — 1 9.00
CHEMBL4112597 — — 1 9.00
CHEMBL4111429 — — 1 9.00
CHEMBL4110812 — — 1 9.00
CHEMBL4110983 — — 1 9.00
CHEMBL4109665 — — 1 9.00
CHEMBL4114872 — — 1 9.00
CHEMBL4115159 — — 1 9.00
CHEMBL4112357 — — 1 8.96
CHEMBL4113427 — — 1 8.82
CHEMBL4108927 — — 1 8.75
CHEMBL4114332 — — 1 8.70
CHEMBL4115130 — — 1 8.70
CHEMBL4107368 — — 1 8.70
CHEMBL4115630 — — 1 8.70
CHEMBL4112648 — — 1 8.70
CHEMBL4110267 — — 1 8.64
CHEMBL4115353 — — 1 8.62
CHEMBL4113941 — — 1 8.60
CHEMBL4111663 — — 1 8.53
CHEMBL4115195 — — 1 8.52
CHEMBL3957332 — — 1 8.52
CHEMBL4114611 — — 1 8.52
CHEMBL4110926 — — 1 8.52
CHEMBL4113610 — — 1 8.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4114881 — Ki = 0.56 nM 9.25
CHEMBL4107149 — Ki = 1.0 nM 9.00
CHEMBL4108223 — Ki = 1.0 nM 9.00
CHEMBL4110983 — Ki = 1.0 nM 9.00
CHEMBL4115159 — Ki = 1.0 nM 9.00
CHEMBL4110103 — Ki = 1.0 nM 9.00
CHEMBL4109665 — Ki = 1.0 nM 9.00
CHEMBL4106988 — Ki = 1.0 nM 9.00
CHEMBL4114872 — Ki = 1.0 nM 9.00
CHEMBL4107104 — Ki = 1.0 nM 9.00
CHEMBL4112597 — Ki = 1.0 nM 9.00
CHEMBL4111429 — Ki = 1.0 nM 9.00
CHEMBL4110812 — Ki = 1.0 nM 9.00
CHEMBL4112357 — Ki = 1.11 nM 8.96
CHEMBL4113427 — Ki = 1.52 nM 8.82
CHEMBL4108927 — Ki = 1.79 nM 8.75
CHEMBL4115630 — Ki = 2.0 nM 8.70
CHEMBL4112648 — Ki = 2.0 nM 8.70
CHEMBL4107368 — Ki = 2.0 nM 8.70
CHEMBL4115130 — Ki = 2.0 nM 8.70
CHEMBL4114332 — Ki = 2.0 nM 8.70
CHEMBL4110267 — Ki = 2.27 nM 8.64
CHEMBL4115353 — Ki = 2.42 nM 8.62
CHEMBL4113941 — Ki = 2.51 nM 8.60
CHEMBL4111663 — Ki = 2.96 nM 8.53
CHEMBL3957332 — Ki = 3.0 nM 8.52
CHEMBL4115195 — Ki = 3.0 nM 8.52
CHEMBL4114611 — Ki = 3.0 nM 8.52
CHEMBL4110926 — Ki = 3.0 nM 8.52
CHEMBL4113610 — Ki = 3.0 nM 8.52
CHEMBL4107398 — Ki = 3.0 nM 8.52
CHEMBL4112483 — Ki = 3.0 nM 8.52
CHEMBL4108491 — Ki = 3.0 nM 8.52
CHEMBL4109580 — Ki = 3.0 nM 8.52
CHEMBL4112773 — Ki = 3.0 nM 8.52
CHEMBL4111142 — Ki = 3.0 nM 8.52
CHEMBL4112300 — Ki = 3.1 nM 8.51
CHEMBL4109841 — Ki = 3.25 nM 8.49
CHEMBL4107808 — Ki = 3.29 nM 8.48
CHEMBL4111951 — Ki = 3.38 nM 8.47
CHEMBL4108033 — Ki = 3.61 nM 8.44
CHEMBL4113149 — Ki = 3.91 nM 8.41
CHEMBL4113712 — Ki = 3.9 nM 8.41
CHEMBL4114450 — Ki = 3.91 nM 8.41
CHEMBL4112921 — Ki = 4.02 nM 8.40
CHEMBL3948120 — Ki = 4.0 nM 8.40
CHEMBL4109421 — Ki = 4.0 nM 8.40
CHEMBL4107446 — Ki = 4.0 nM 8.40
CHEMBL4109906 — Ki = 4.0 nM 8.40
CHEMBL4108998 — Ki = 4.0 nM 8.40