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Assay Detail

CHEMBL4056822

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

Binding
Inhibition of recombinant human neprilysin using Suc-Ala-Ala-Phe-AMC as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by fluorescence assay
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neprilysin (CHEMBL1944)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Substituted α-mercaptoketones, new types of specific neprilysin inhibitors.
Poras H, Patouret R, Leiris S, Ouimet T, Fournié-Zaluski MC, Roques BP.
Bioorg Med Chem Lett (2017) 27 : 3883 -3890
PubMed 28676269 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 37 7.33 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4075182 1 8.70
CHEMBL4091227 1 8.38
CHEMBL4080935 1 8.34
CHEMBL4089776 1 8.15
CHEMBL4069278 1 8.05
CHEMBL4077560 1 7.92
CHEMBL4085997 1 7.75
CHEMBL4066184 1 7.70
CHEMBL4075187 1 7.66
CHEMBL19621 1 7.64
CHEMBL4073385 1 7.58
CHEMBL4066384 1 7.54
CHEMBL4074531 1 7.52
CHEMBL4096514 1 7.50
CHEMBL4070297 1 7.44
CHEMBL4094037 1 7.44
CHEMBL4074608 1 7.40
CHEMBL4087357 1 7.34
CHEMBL4067507 1 7.31
CHEMBL4086067 1 7.30
CHEMBL4088816 1 7.28
CHEMBL4102672 1 7.27
CHEMBL4078411 1 7.27
CHEMBL4098968 1 7.21
CHEMBL4095593 1 7.21
CHEMBL4064153 1 7.11
CHEMBL4088709 1 7.07
CHEMBL4075680 1 7.02
CHEMBL4094929 1 7.02
CHEMBL4100250 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4075182 Ki = 2.0 nM 8.70
CHEMBL4091227 Ki = 4.2 nM 8.38
CHEMBL4080935 Ki = 4.6 nM 8.34
CHEMBL4089776 Ki = 7.0 nM 8.15
CHEMBL4069278 Ki = 9.0 nM 8.05
CHEMBL4077560 Ki = 12.0 nM 7.92
CHEMBL4085997 Ki = 18.0 nM 7.75
CHEMBL4066184 Ki = 20.0 nM 7.70
CHEMBL4075187 Ki = 22.0 nM 7.66
CHEMBL19621 Ki = 23.0 nM 7.64
CHEMBL4073385 Ki = 26.0 nM 7.58
CHEMBL4066384 Ki = 29.0 nM 7.54
CHEMBL4074531 Ki = 30.0 nM 7.52
CHEMBL4096514 Ki = 32.0 nM 7.50
CHEMBL4094037 Ki = 36.0 nM 7.44
CHEMBL4070297 Ki = 36.0 nM 7.44
CHEMBL4074608 Ki = 40.0 nM 7.40
CHEMBL4087357 Ki = 46.0 nM 7.34
CHEMBL4067507 Ki = 49.0 nM 7.31
CHEMBL4086067 Ki = 50.0 nM 7.30
CHEMBL4088816 Ki = 52.0 nM 7.28
CHEMBL4102672 Ki = 54.0 nM 7.27
CHEMBL4078411 Ki = 54.0 nM 7.27
CHEMBL4098968 Ki = 61.0 nM 7.21
CHEMBL4095593 Ki = 61.0 nM 7.21
CHEMBL4064153 Ki = 78.0 nM 7.11
CHEMBL4088709 Ki = 86.0 nM 7.07
CHEMBL4094929 Ki = 95.0 nM 7.02
CHEMBL4075680 Ki = 95.0 nM 7.02
CHEMBL4100250 Ki = 140.0 nM 6.85
CHEMBL4061434 Ki = 162.0 nM 6.79
CHEMBL4082357 Ki = 252.0 nM 6.60
CHEMBL4101421 Ki = 260.0 nM 6.58
CHEMBL4067370 Ki = 470.0 nM 6.33
CHEMBL4091335 Ki = 1650.0 nM 5.78
CHEMBL4063351 Ki = 1750.0 nM 5.76
CHEMBL4076819 Ki > 1e-05 nM -