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Assay Detail

CHEMBL2027645

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

Binding
Inhibition of human recombinant renin using H-Asp-Arg-Val-Tyr-Ile-His-Pro-Phe-His-Leu-Val-Ile-His-Asn-OH as substrate assessed as formation of angiotensin1 product after 2 hrs by competive radioimmunoassay
7
Total Activities
7
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

Renin (CHEMBL286)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of VTP-27999, an Alkyl Amine Renin Inhibitor with Potential for Clinical Utility.
Jia L, Simpson RD, Yuan J, Xu Z, Zhao W, Cacatian S, Tice CM, Guo J, Ishchenko A, Singh SB, Wu Z, McKeever BM, Bukhtiyarov Y, Johnson JA, Doe CP, Harrison RK, McGeehan GM, Dillard LW, Baldwin JJ, Claremon DA.
ACS Med Chem Lett (2011) 2 : 747 -751
PubMed 24900262 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 9.27 9.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2023123 1 9.82
CHEMBL2024249 1 9.57
CHEMBL1276678 VTP-27999 1.0 1 9.52
CHEMBL2024248 1 9.38
CHEMBL1639 ALISKIREN 4.0 1 9.28
CHEMBL2023124 1 8.77
CHEMBL2023122 1 8.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2023123 IC50 = 0.15 nM 9.82
CHEMBL2024249 IC50 = 0.27 nM 9.57
CHEMBL1276678 VTP-27999 IC50 = 0.3 nM 9.52
CHEMBL2024248 IC50 = 0.42 nM 9.38
CHEMBL1639 ALISKIREN IC50 = 0.53 nM 9.28
CHEMBL2023124 IC50 = 1.7 nM 8.77
CHEMBL2023122 IC50 = 2.7 nM 8.57