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Assay Detail

CHEMBL801750

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

Binding
In vitro inhibitory concentration against monkey plasma renin at pH 7.4
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cercopithecidae
Tissue Plasma
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Renin (CHEMBL286)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Studies directed toward the design of orally active renin inhibitors. 2. Development of the efficacious, bioavailable renin inhibitor (2S)-2-benzyl-3- [[(1-methylpiperazin-4-yl)sulfonyl]propionyl]-3-thiazol-4-yl-L-alanine amide of (2S,3R,4S)-2-amino-1-cyclohexyl-3,4-dihydroxy-6-methylheptane (A-72517).
Rosenberg SH, Spina KP, Condon SL, Polakowski J, Yao Z, Kovar P, Stein HH, Cohen J, Barlow JL, Klinghofer V.
J Med Chem (1993) 36 : 460 -467
PubMed 8474102 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 9.37 9.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL113841 ZANKIREN 2.0 1 9.62
CHEMBL343968 1 9.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL113841 ZANKIREN IC50 = 0.24 nM 9.62
CHEMBL343968 IC50 = 0.76 nM 9.12