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Assay Detail

CHEMBL5737779

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Binding
Plasma Kallikrein Activity Assay: Plasma kallikrein activity assay. The effect of compounds of the invention on human plasma kallikrein activity was determined using the chromogenic substrates (DiaPharma Group, Inc., West Chester, Ohio, USA). In these experiments, 2 nM kallikrein (Enzyme Research Laboratories, South Bend, Ind., USA) was incubated with 80 μM S2302 (H-D-Pro-Phe-Arg-p-nitroaniline) in the absence or presence of increasing concentrations of compounds of the invention in a final volume of 200 μL Tris-HCl buffer (200 mM NaCl; 2.5 mM CaCl2; 50 mM Tris-HCl, pH 7.8).After incubation at 30° C., the activity of kallikrein was measured as a change in absorbance at OD 405 nm using BioTek Power Wave X340 Microplate Reader (Winooski, Vt., USA). Data were analyzed using SigmaPlot software.
906
Total Activities
244
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

Human plasma kallikrein inhibitors
(2022)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 302 7.60 7.60
kon 302 - -
k_off 302 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5880741 3 7.60
CHEMBL4867028 3 7.60
CHEMBL5805068 3 7.60
CHEMBL6030905 3 7.60
CHEMBL5853740 3 7.60
CHEMBL4854896 3 7.60
CHEMBL5840895 3 7.60
CHEMBL4852994 9 7.60
CHEMBL5218665 3 7.60
CHEMBL4847070 9 7.60
CHEMBL5218770 9 7.60
CHEMBL5218471 3 7.60
CHEMBL6007256 3 7.60
CHEMBL5847996 3 7.60
CHEMBL5220941 3 7.60
CHEMBL5877277 3 7.60
CHEMBL5908529 3 7.60
CHEMBL5220737 9 7.60
CHEMBL5219216 9 7.60
CHEMBL5949523 3 7.60
CHEMBL4868429 9 7.60
CHEMBL5770259 3 7.60
CHEMBL5862639 3 7.60
CHEMBL5751462 3 7.60
CHEMBL4868583 3 7.60
CHEMBL5872982 3 7.60
CHEMBL5221062 3 7.60
CHEMBL5900782 9 7.60
CHEMBL5829884 9 7.60
CHEMBL5889251 3 7.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5219926 Ki = 25.1 nM 7.60
CHEMBL6007256 Ki = 25.1 nM 7.60
CHEMBL5762130 Ki = 25.1 nM 7.60
CHEMBL5880741 Ki = 25.1 nM 7.60
CHEMBL5966133 Ki = 25.1 nM 7.60
CHEMBL5800986 Ki = 25.1 nM 7.60
CHEMBL5929109 Ki = 25.1 nM 7.60
CHEMBL5825652 Ki = 25.1 nM 7.60
CHEMBL5908529 Ki = 25.1 nM 7.60
CHEMBL5992835 Ki = 25.1 nM 7.60
CHEMBL5770667 Ki = 25.1 nM 7.60
CHEMBL5759971 Ki = 25.1 nM 7.60
CHEMBL5939579 Ki = 25.1 nM 7.60
CHEMBL5885714 Ki = 25.1 nM 7.60
CHEMBL5218627 Ki = 25.1 nM 7.60
CHEMBL5899953 Ki = 25.1 nM 7.60
CHEMBL5830319 Ki = 25.1 nM 7.60
CHEMBL5220941 Ki = 25.1 nM 7.60
CHEMBL5848868 Ki = 25.1 nM 7.60
CHEMBL5906069 Ki = 25.1 nM 7.60
CHEMBL5829884 Ki = 25.1 nM 7.60
CHEMBL5847996 Ki = 25.1 nM 7.60
CHEMBL5796510 Ki = 25.1 nM 7.60
CHEMBL5218476 Ki = 25.1 nM 7.60
CHEMBL5751829 Ki = 25.1 nM 7.60
CHEMBL5829884 Ki = 25.1 nM 7.60
CHEMBL5827332 Ki = 25.1 nM 7.60
CHEMBL4852994 Ki = 25.1 nM 7.60
CHEMBL5885714 Ki = 25.1 nM 7.60
CHEMBL5784656 Ki = 25.1 nM 7.60
CHEMBL5218665 Ki = 25.1 nM 7.60
CHEMBL5899953 Ki = 25.1 nM 7.60
CHEMBL5899953 Ki = 25.1 nM 7.60
CHEMBL4847070 Ki = 25.1 nM 7.60
CHEMBL5850171 Ki = 25.1 nM 7.60
CHEMBL5796510 Ki = 25.1 nM 7.60
CHEMBL5288637 Ki = 25.1 nM 7.60
CHEMBL5219643 Ki = 25.1 nM 7.60
CHEMBL6001154 Ki = 25.1 nM 7.60
CHEMBL5218770 Ki = 25.1 nM 7.60
CHEMBL4846073 Ki = 25.1 nM 7.60
CHEMBL5997463 Ki = 25.1 nM 7.60
CHEMBL5820462 Ki = 25.1 nM 7.60
CHEMBL5219216 Ki = 25.1 nM 7.60
CHEMBL5999054 Ki = 25.1 nM 7.60
CHEMBL5918949 Ki = 25.1 nM 7.60
CHEMBL5780759 Ki = 25.1 nM 7.60
CHEMBL5219926 Ki = 25.1 nM 7.60
CHEMBL5218471 Ki = 25.1 nM 7.60
CHEMBL6023303 Ki = 25.1 nM 7.60