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Assay Detail

CHEMBL673750

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

Binding
In vitro inhibition of endothelin converting enzyme.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Endothelin-converting enzyme 1 (CHEMBL4791)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

N-[2-(Indan-1-yl)-3-mercapto-propionyl] amino acids as highly potent inhibitors of the three vasopeptidases (NEP, ACE, ECE): In vitro and In vivo activities.
Inguimbert N, Poras H, Teffo F, Beslot F, Selkti M, Tomas A, Scalbert E, Bennejean C, Renard P, Fournié-Zaluski MC, Roques BP.
Bioorg Med Chem Lett (2002) 12 : 2001 -2005
PubMed 12113828 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 7.04 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL60439 1 8.00
CHEMBL301646 1 7.75
CHEMBL305089 1 7.66
CHEMBL285490 1 7.58
CHEMBL61713 1 7.55
CHEMBL302837 1 7.51
CHEMBL61016 1 7.46
CHEMBL304218 1 7.33
CHEMBL303302 1 7.10
CHEMBL262267 1 7.05
CHEMBL293685 1 7.05
CHEMBL304629 1 7.00
CHEMBL35643 1 7.00
CHEMBL304209 1 6.96
CHEMBL61640 1 6.85
CHEMBL305388 1 6.75
CHEMBL59674 1 6.68
CHEMBL60363 1 6.43
CHEMBL292534 1 6.25
CHEMBL59856 1 6.12
CHEMBL59762 1 5.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL60439 Ki = 10.0 nM 8.00
CHEMBL301646 Ki = 18.0 nM 7.75
CHEMBL305089 Ki = 22.0 nM 7.66
CHEMBL285490 Ki = 26.0 nM 7.58
CHEMBL61713 Ki = 28.0 nM 7.55
CHEMBL302837 Ki = 31.0 nM 7.51
CHEMBL61016 Ki = 35.0 nM 7.46
CHEMBL304218 Ki = 47.0 nM 7.33
CHEMBL303302 Ki = 79.0 nM 7.10
CHEMBL262267 Ki = 90.0 nM 7.05
CHEMBL293685 Ki = 90.0 nM 7.05
CHEMBL304629 Ki = 100.0 nM 7.00
CHEMBL35643 Ki = 100.0 nM 7.00
CHEMBL304209 Ki = 110.0 nM 6.96
CHEMBL61640 Ki = 140.0 nM 6.85
CHEMBL305388 Ki = 180.0 nM 6.75
CHEMBL59674 Ki = 210.0 nM 6.68
CHEMBL60363 Ki = 370.0 nM 6.43
CHEMBL292534 Ki = 560.0 nM 6.25
CHEMBL59856 Ki = 760.0 nM 6.12
CHEMBL59762 Ki = 1460.0 nM 5.84