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Assay Detail

CHEMBL748042

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

Binding
In vitro inhibition of rat kidney neutral endopeptidase (NEP) by fluorometric assay using Dansyl-Gly-Phe-Arg as substrate
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Neprilysin (CHEMBL3369)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Mercaptoacyl dipeptides as dual inhibitors of angiotensin-converting enzyme and neutral endopeptidase. Preliminary structure-activity studies
Delaney NG, Barrish JC, Neubeck R, Natarajan S, Cohen M, Rovnyak GC, Huber G, Murugesan N, Girotra R, Sieber-McMaster E, Robl JA, Asaad MM, Cheung HS, Bird J, Waldron T, Petrillo EW
Bioorg Med Chem Lett (1994) 4 : 1783 -1788
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.75 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL50625 1 8.80
CHEMBL51988 1 8.70
CHEMBL50312 1 8.66
CHEMBL50582 1 8.59
CHEMBL49920 1 8.41
CHEMBL51715 1 8.24
CHEMBL50914 1 8.21
CHEMBL299181 1 8.18
CHEMBL422403 1 8.18
CHEMBL51428 1 8.18
CHEMBL51466 1 8.03
CHEMBL50915 1 8.00
CHEMBL50954 1 7.60
CHEMBL50595 1 7.50
CHEMBL295936 1 7.40
CHEMBL50203 1 7.35
CHEMBL51301 1 7.06
CHEMBL440856 1 6.85
CHEMBL300880 1 6.80
CHEMBL50414 1 6.74
CHEMBL51625 1 6.54
CHEMBL287896 1 6.40
CHEMBL1560 CAPTOPRIL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL50625 IC50 = 1.6 nM 8.80
CHEMBL51988 IC50 = 2.0 nM 8.70
CHEMBL50312 IC50 = 2.2 nM 8.66
CHEMBL50582 IC50 = 2.6 nM 8.59
CHEMBL49920 IC50 = 3.9 nM 8.41
CHEMBL51715 IC50 = 5.7 nM 8.24
CHEMBL50914 IC50 = 6.2 nM 8.21
CHEMBL299181 IC50 = 6.6 nM 8.18
CHEMBL422403 IC50 = 6.6 nM 8.18
CHEMBL51428 IC50 = 6.6 nM 8.18
CHEMBL51466 IC50 = 9.4 nM 8.03
CHEMBL50915 IC50 = 10.0 nM 8.00
CHEMBL50954 IC50 = 25.0 nM 7.60
CHEMBL50595 IC50 = 32.0 nM 7.50
CHEMBL295936 IC50 = 40.0 nM 7.40
CHEMBL50203 IC50 = 45.0 nM 7.35
CHEMBL51301 IC50 = 87.0 nM 7.06
CHEMBL440856 IC50 = 140.0 nM 6.85
CHEMBL300880 IC50 = 160.0 nM 6.80
CHEMBL50414 IC50 = 182.0 nM 6.74
CHEMBL51625 IC50 = 285.0 nM 6.54
CHEMBL287896 IC50 = 400.0 nM 6.40
CHEMBL1560 CAPTOPRIL IC50 = 830000.0 nM -