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Assay Detail

CHEMBL5733794

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Binding
Inhibition 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 ↗
654
Total Activities
210
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

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

Publication

Dihydropyridone P1 as factor XIa inhibitors
(2018)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 218 7.48 9.25
kon 218 - -
k_off 218 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4114881 — — 3 9.25
CHEMBL4107149 — — 3 9.00
CHEMBL4108223 — — 3 9.00
CHEMBL4110103 — — 3 9.00
CHEMBL4106988 — — 3 9.00
CHEMBL4107104 — — 3 9.00
CHEMBL4112597 — — 3 9.00
CHEMBL4111429 — — 3 9.00
CHEMBL4110812 — — 3 9.00
CHEMBL4110983 — — 3 9.00
CHEMBL4109665 — — 3 9.00
CHEMBL4114872 — — 3 9.00
CHEMBL4115159 — — 3 9.00
CHEMBL4112357 — — 3 8.96
CHEMBL4113427 — — 3 8.82
CHEMBL4108927 — — 3 8.75
CHEMBL4114332 — — 3 8.70
CHEMBL4115130 — — 3 8.70
CHEMBL4107368 — — 3 8.70
CHEMBL4115630 — — 3 8.70
CHEMBL4112648 — — 3 8.70
CHEMBL4110267 — — 3 8.64
CHEMBL4115353 — — 3 8.62
CHEMBL4113941 — — 3 8.60
CHEMBL4111663 — — 3 8.53
CHEMBL4115195 — — 3 8.52
CHEMBL3957332 — — 3 8.52
CHEMBL4114611 — — 3 8.52
CHEMBL4110926 — — 3 8.52
CHEMBL4113610 — — 3 8.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4114881 — Ki = 0.56 nM 9.25
CHEMBL4110812 — Ki = 1.0 nM 9.00
CHEMBL4111429 — Ki = 1.0 nM 9.00
CHEMBL4114872 — Ki = 1.0 nM 9.00
CHEMBL4107149 — Ki = 1.0 nM 9.00
CHEMBL4109665 — Ki = 1.0 nM 9.00
CHEMBL4115159 — Ki = 1.0 nM 9.00
CHEMBL4108223 — Ki = 1.0 nM 9.00
CHEMBL4112597 — Ki = 1.0 nM 9.00
CHEMBL4110983 — Ki = 1.0 nM 9.00
CHEMBL4107104 — Ki = 1.0 nM 9.00
CHEMBL4106988 — Ki = 1.0 nM 9.00
CHEMBL4110103 — 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
CHEMBL4115130 — Ki = 2.0 nM 8.70
CHEMBL4107368 — Ki = 2.0 nM 8.70
CHEMBL4115630 — Ki = 2.0 nM 8.70
CHEMBL4112648 — 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
CHEMBL4110926 — Ki = 3.0 nM 8.52
CHEMBL4113610 — Ki = 3.0 nM 8.52
CHEMBL4112483 — Ki = 3.0 nM 8.52
CHEMBL3957332 — Ki = 3.0 nM 8.52
CHEMBL4107398 — Ki = 3.0 nM 8.52
CHEMBL4109580 — Ki = 3.0 nM 8.52
CHEMBL4112773 — Ki = 3.0 nM 8.52
CHEMBL4114611 — Ki = 3.0 nM 8.52
CHEMBL4108491 — Ki = 3.0 nM 8.52
CHEMBL4115195 — 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
CHEMBL4114450 — Ki = 3.91 nM 8.41
CHEMBL5826162 — Ki = 3.9 nM 8.41
CHEMBL4113149 — Ki = 3.91 nM 8.41
CHEMBL4108998 — Ki = 4.0 nM 8.40
CHEMBL4109421 — Ki = 4.0 nM 8.40
CHEMBL4112921 — Ki = 4.02 nM 8.40
CHEMBL4107446 — Ki = 4.0 nM 8.40
CHEMBL4109906 — Ki = 4.0 nM 8.40
CHEMBL3948120 — Ki = 4.0 nM 8.40