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Assay Detail

CHEMBL748035

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

Binding
Inhibitory activity on neutral endopeptidase (NEP) using DGNPA as substrate.
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Neprilysin (CHEMBL3768)
Type SINGLE PROTEIN
Organism Oryctolagus cuniculus

Publication

Phosphinic derivatives as new dual enkephalin-degrading enzyme inhibitors: synthesis, biological properties, and antinociceptive activities.
Chen H, Noble F, Mothé A, Meudal H, Coric P, Danascimento S, Roques BP, George P, Fournié-Zaluski MC.
J Med Chem (2000) 43 : 1398 -1408
PubMed 10753476 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 37 7.18 9.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1159952 1 9.03
CHEMBL1159940 1 8.92
CHEMBL1159933 1 8.85
CHEMBL1159942 1 8.70
CHEMBL1159925 1 8.66
CHEMBL1159930 1 8.64
CHEMBL1159927 1 8.54
CHEMBL1159936 1 8.48
CHEMBL1159939 1 8.31
CHEMBL1159953 1 7.93
CHEMBL1159932 1 7.81
CHEMBL1159950 1 7.49
CHEMBL1159919 1 7.37
CHEMBL1159941 1 7.29
CHEMBL1159924 1 7.16
CHEMBL1159921 1 7.10
CHEMBL1159954 1 6.98
CHEMBL1159928 1 6.96
CHEMBL1159931 1 6.85
CHEMBL1159947 1 6.84
CHEMBL1159934 1 6.82
CHEMBL1159955 1 6.80
CHEMBL1159937 1 6.80
CHEMBL1159961 1 6.75
CHEMBL1159926 1 6.73
CHEMBL1159916 1 6.72
CHEMBL1159949 1 6.72
CHEMBL1159920 1 6.72
CHEMBL1159956 1 6.64
CHEMBL1159935 1 6.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1159952 Ki = 0.94 nM 9.03
CHEMBL1159940 Ki = 1.2 nM 8.92
CHEMBL1159933 Ki = 1.4 nM 8.85
CHEMBL1159942 Ki = 2.0 nM 8.70
CHEMBL1159925 Ki = 2.2 nM 8.66
CHEMBL1159930 Ki = 2.3 nM 8.64
CHEMBL1159927 Ki = 2.9 nM 8.54
CHEMBL1159936 Ki = 3.3 nM 8.48
CHEMBL1159939 Ki = 4.9 nM 8.31
CHEMBL1159953 Ki = 11.8 nM 7.93
CHEMBL1159932 Ki = 15.5 nM 7.81
CHEMBL1159950 Ki = 32.5 nM 7.49
CHEMBL1159919 Ki = 43.0 nM 7.37
CHEMBL1159941 Ki = 51.0 nM 7.29
CHEMBL1159924 Ki = 70.0 nM 7.16
CHEMBL1159921 Ki = 80.0 nM 7.10
CHEMBL1159954 Ki = 104.0 nM 6.98
CHEMBL1159928 Ki = 110.0 nM 6.96
CHEMBL1159931 Ki = 140.0 nM 6.85
CHEMBL1159947 Ki = 146.0 nM 6.84
CHEMBL1159934 Ki = 150.0 nM 6.82
CHEMBL1159955 Ki = 160.0 nM 6.80
CHEMBL1159937 Ki = 158.0 nM 6.80
CHEMBL1159961 Ki = 180.0 nM 6.75
CHEMBL1159926 Ki = 185.0 nM 6.73
CHEMBL1159916 Ki = 190.0 nM 6.72
CHEMBL1159949 Ki = 190.0 nM 6.72
CHEMBL1159920 Ki = 190.0 nM 6.72
CHEMBL1159956 Ki = 230.0 nM 6.64
CHEMBL1159935 Ki = 290.0 nM 6.54
CHEMBL1159959 Ki = 540.0 nM 6.27
CHEMBL1159938 Ki = 560.0 nM 6.25
CHEMBL1159944 Ki = 790.0 nM 6.10
CHEMBL1159923 Ki = 1100.0 nM 5.96
CHEMBL1159922 Ki = 2200.0 nM 5.66
CHEMBL1159945 Ki = 4000.0 nM 5.40
CHEMBL1159917 Ki = 10000.0 nM 5.00