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Assay Detail

CHEMBL751028

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

Binding
Inhibitory activity against neutral endopeptidase (NEP).
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Neprilysin (CHEMBL1944)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of potent, selective inhibitors of endothelin-converting enzyme.
Wallace EM, Moliterni JA, Moskal MA, Neubert AD, Marcopulos N, Stamford LB, Trapani AJ, Savage P, Chou M, Jeng AY.
J Med Chem (1998) 41 : 1513 -1523
PubMed 9554884 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 5.69 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL290698 1 9.00
CHEMBL285619 1 8.30
CHEMBL40028 1 7.85
CHEMBL479579 PHOSPHORAMIDON 1 7.52
CHEMBL39384 1 6.77
CHEMBL37052 1 6.60
CHEMBL434208 1 6.39
CHEMBL290332 1 6.19
CHEMBL446393 1 6.14
CHEMBL416234 1 6.07
CHEMBL288837 1 6.02
CHEMBL37542 1 5.92
CHEMBL39887 1 5.89
CHEMBL39828 1 5.68
CHEMBL40168 1 5.60
CHEMBL36753 1 5.39
CHEMBL147847 1 5.24
CHEMBL290868 1 5.21
CHEMBL36382 1 5.20
CHEMBL39777 1 5.20
CHEMBL39714 1 5.19
CHEMBL289150 1 5.17
CHEMBL37078 1 5.16
CHEMBL290256 1 5.07
CHEMBL35995 1 5.01
CHEMBL290304 1 5.00
CHEMBL37456 1 5.00
CHEMBL36809 1 4.97
CHEMBL448098 1 4.96
CHEMBL289638 1 4.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL290698 IC50 = 1.0 nM 9.00
CHEMBL285619 IC50 = 5.0 nM 8.30
CHEMBL40028 IC50 = 14.0 nM 7.85
CHEMBL479579 PHOSPHORAMIDON IC50 = 30.0 nM 7.52
CHEMBL39384 IC50 = 170.0 nM 6.77
CHEMBL37052 IC50 = 250.0 nM 6.60
CHEMBL434208 IC50 = 407.0 nM 6.39
CHEMBL290332 IC50 = 640.0 nM 6.19
CHEMBL446393 IC50 = 730.0 nM 6.14
CHEMBL416234 IC50 = 860.0 nM 6.07
CHEMBL288837 IC50 = 948.0 nM 6.02
CHEMBL37542 IC50 = 1200.0 nM 5.92
CHEMBL39887 IC50 = 1300.0 nM 5.89
CHEMBL39828 IC50 = 2070.0 nM 5.68
CHEMBL40168 IC50 = 2500.0 nM 5.60
CHEMBL36753 IC50 = 4060.0 nM 5.39
CHEMBL147847 IC50 = 5800.0 nM 5.24
CHEMBL290868 IC50 = 6200.0 nM 5.21
CHEMBL39777 IC50 = 6300.0 nM 5.20
CHEMBL36382 IC50 = 6300.0 nM 5.20
CHEMBL39714 IC50 = 6500.0 nM 5.19
CHEMBL289150 IC50 = 6700.0 nM 5.17
CHEMBL37078 IC50 = 7000.0 nM 5.16
CHEMBL290256 IC50 = 8600.0 nM 5.07
CHEMBL35995 IC50 = 9700.0 nM 5.01
CHEMBL37456 IC50 = 10000.0 nM 5.00
CHEMBL290304 IC50 = 10000.0 nM 5.00
CHEMBL36809 IC50 = 10700.0 nM 4.97
CHEMBL448098 IC50 = 11000.0 nM 4.96
CHEMBL289638 IC50 = 15000.0 nM 4.82
CHEMBL39997 IC50 = 19000.0 nM 4.72
CHEMBL287971 IC50 = 23000.0 nM 4.64
CHEMBL39812 IC50 = 26000.0 nM 4.58
CHEMBL417507 IC50 = 40000.0 nM 4.40
CHEMBL37861 IC50 = 55000.0 nM 4.26