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Assay Detail

CHEMBL752993

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Binding
Inhibition of neutral endopeptidase
12
Total Activities
12
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

Ortho-substituted benzofused macrocyclic lactams as zinc metalloprotease inhibitors.
Ksander GM, de Jesus R, Yuan A, Ghai RD, Trapani A, McMartin C, Bohacek R.
J Med Chem (1997) 40 : 495 -505
PubMed 9046340 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.62 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL150222 1 9.05
CHEMBL342091 1 8.52
CHEMBL357311 1 8.40
CHEMBL10247 THIORPHAN -1.0 1 8.37
CHEMBL346424 1 8.15
CHEMBL146573 1 7.57
CHEMBL147755 1 7.17
CHEMBL148140 1 7.00
CHEMBL149367 1 6.87
CHEMBL149841 1 6.65
CHEMBL433702 1 6.05
CHEMBL423574 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL150222 IC50 = 0.9 nM 9.05
CHEMBL342091 IC50 = 3.0 nM 8.52
CHEMBL357311 IC50 = 4.0 nM 8.40
CHEMBL10247 THIORPHAN IC50 = 4.3 nM 8.37
CHEMBL346424 IC50 = 7.0 nM 8.15
CHEMBL146573 IC50 = 27.0 nM 7.57
CHEMBL147755 IC50 = 67.0 nM 7.17
CHEMBL148140 IC50 = 99.0 nM 7.00
CHEMBL149367 IC50 = 136.0 nM 6.87
CHEMBL149841 IC50 = 224.0 nM 6.65
CHEMBL433702 IC50 = 900.0 nM 6.05
CHEMBL423574 IC50 > 10000.0 nM -