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Assay Detail

CHEMBL754357

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

Binding
In vitro inhibition of Neutral Endopeptidase isolated from rat kidney.
18
Total Activities
18
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

Dual metalloprotease inhibitors. IV. Utilization of thiazepines and thiazines as constrained peptidomimetic surrogates in mercaptoacyl dipeptides
Das J, Robl JA, Reid JA, Sun C, Misra RN, Brown BR, Ryono DE, Asaad MM, Bird J, Trippodo NC, Petrillo EW, Karanewsky DS
Bioorg Med Chem Lett (1994) 4 : 2193 -2198
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.04 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL69836 1 9.05
CHEMBL51780 1 9.00
CHEMBL305020 1 8.62
CHEMBL305050 1 8.60
CHEMBL71769 1 8.57
CHEMBL304148 1 7.40
CHEMBL298388 1 7.19
CHEMBL68849 1 7.00
CHEMBL71711 1 6.90
CHEMBL306461 1 6.61
CHEMBL71496 1 6.60
CHEMBL71746 1 6.42
CHEMBL67804 1 6.27
CHEMBL71538 1 5.87
CHEMBL71351 1 5.81
CHEMBL420192 1 5.70
CHEMBL306938 1 5.69
CHEMBL67924 1 5.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL69836 IC50 = 0.9 nM 9.05
CHEMBL51780 IC50 = 1.0 nM 9.00
CHEMBL305020 IC50 = 2.4 nM 8.62
CHEMBL305050 IC50 = 2.5 nM 8.60
CHEMBL71769 IC50 = 2.7 nM 8.57
CHEMBL304148 IC50 = 40.0 nM 7.40
CHEMBL298388 IC50 = 64.0 nM 7.19
CHEMBL68849 IC50 = 99.0 nM 7.00
CHEMBL71711 IC50 = 126.0 nM 6.90
CHEMBL306461 IC50 = 244.0 nM 6.61
CHEMBL71496 IC50 = 251.0 nM 6.60
CHEMBL71746 IC50 = 380.0 nM 6.42
CHEMBL67804 IC50 = 535.0 nM 6.27
CHEMBL71538 IC50 = 1352.0 nM 5.87
CHEMBL71351 IC50 = 1559.0 nM 5.81
CHEMBL420192 IC50 = 2020.0 nM 5.70
CHEMBL306938 IC50 = 2043.0 nM 5.69
CHEMBL67924 IC50 = 3820.0 nM 5.42