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Assay Detail

CHEMBL755103

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

Binding
Inhibitory activity against Leu-enkeph of Neutral endopeptidase
16
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Neprilysin (CHEMBL3768)
Type SINGLE PROTEIN
Organism Oryctolagus cuniculus

Publication

Hydroxamic acids as potent inhibitors of endothelin-converting enzyme from human bronchiolar smooth muscle.
Bihovsky R, Levinson BL, Loewi RC, Erhardt PW, Polokoff MA.
J Med Chem (1995) 38 : 2119 -2129
PubMed 7783143 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 8.38 10.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL303159 1 10.52
CHEMBL66967 1 9.40
CHEMBL85320 KELATORPHAN 1 9.00
CHEMBL304939 1 9.00
CHEMBL303892 1 8.70
CHEMBL2372437 1 8.70
CHEMBL66284 1 8.70
CHEMBL63317 1 8.70
CHEMBL67000 1 8.52
CHEMBL10247 THIORPHAN -1.0 1 8.30
CHEMBL68128 2 8.30
CHEMBL479579 PHOSPHORAMIDON 1 8.22
CHEMBL69793 1 7.52
CHEMBL67348 1 6.77
CHEMBL65903 1 6.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL303159 IC50 = 0.03 nM 10.52
CHEMBL66967 IC50 = 0.4 nM 9.40
CHEMBL85320 KELATORPHAN IC50 = 1.0 nM 9.00
CHEMBL304939 IC50 = 1.0 nM 9.00
CHEMBL303892 IC50 = 2.0 nM 8.70
CHEMBL2372437 IC50 = 2.0 nM 8.70
CHEMBL66284 IC50 = 2.0 nM 8.70
CHEMBL63317 IC50 = 2.0 nM 8.70
CHEMBL67000 IC50 = 3.0 nM 8.52
CHEMBL10247 THIORPHAN IC50 = 5.0 nM 8.30
CHEMBL68128 IC50 = 5.0 nM 8.30
CHEMBL479579 PHOSPHORAMIDON IC50 = 6.0 nM 8.22
CHEMBL68128 IC50 = 18.0 nM 7.75
CHEMBL69793 IC50 = 30.0 nM 7.52
CHEMBL67348 IC50 = 170.0 nM 6.77
CHEMBL65903 IC50 = 950.0 nM 6.02