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Assay Detail

CHEMBL754638

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

Binding
In vitro inhibition of purified rat kidney Neutral endopeptidase.
19
Total Activities
19
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. 6. Incorporation of bicyclic and substituted monocyclic azepinones as dipeptide surrogates in angiotensin-converting enzyme/neutral endopeptidase inhibitors.
Robl JA, Cimarusti MP, Simpkins LM, Brown B, Ryono DE, Bird JE, Asaad MM, Schaeffer TR, Trippodo NC.
J Med Chem (1996) 39 : 494 -502
PubMed 8558518 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.02 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL299639 1 8.22
CHEMBL434070 1 7.77
CHEMBL41201 1 7.75
CHEMBL39775 1 7.60
CHEMBL146371 1 7.51
CHEMBL357932 1 7.50
CHEMBL147043 1 7.40
CHEMBL104054 1 7.31
CHEMBL148155 1 7.19
CHEMBL299169 1 7.09
CHEMBL149442 1 7.07
CHEMBL144659 1 7.04
CHEMBL146823 1 6.85
CHEMBL318096 1 6.83
CHEMBL287896 1 6.40
CHEMBL343191 1 6.33
CHEMBL356577 1 6.00
CHEMBL345021 1 5.78
CHEMBL147153 1 5.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL299639 IC50 = 6.0 nM 8.22
CHEMBL434070 IC50 = 17.0 nM 7.77
CHEMBL41201 IC50 = 18.0 nM 7.75
CHEMBL39775 IC50 = 25.0 nM 7.60
CHEMBL146371 IC50 = 31.0 nM 7.51
CHEMBL357932 IC50 = 32.0 nM 7.50
CHEMBL147043 IC50 = 40.0 nM 7.40
CHEMBL104054 IC50 = 49.0 nM 7.31
CHEMBL148155 IC50 = 64.0 nM 7.19
CHEMBL299169 IC50 = 82.0 nM 7.09
CHEMBL149442 IC50 = 86.0 nM 7.07
CHEMBL144659 IC50 = 92.0 nM 7.04
CHEMBL146823 IC50 = 140.0 nM 6.85
CHEMBL318096 IC50 = 149.0 nM 6.83
CHEMBL287896 IC50 = 400.0 nM 6.40
CHEMBL343191 IC50 = 466.0 nM 6.33
CHEMBL356577 IC50 = 1000.0 nM 6.00
CHEMBL345021 IC50 = 1655.0 nM 5.78
CHEMBL147153 IC50 = 1653.0 nM 5.78