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Assay Detail

CHEMBL889128

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Binding
Inhibition of renin
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Renin (CHEMBL286)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 6-ethyl-2,4-diaminopyrimidine-based small molecule renin inhibitors.
Holsworth DD, Jalaie M, Belliotti T, Cai C, Collard W, Ferreira S, Powell NA, Stier M, Zhang E, McConnell P, Mochalkin I, Ryan MJ, Bryant J, Li T, Kasani A, Subedi R, Maiti SN, Edmunds JJ.
Bioorg Med Chem Lett (2007) 17 : 3575 -3580
PubMed 17482464 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.00 10.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL390196 1 10.17
CHEMBL411885 1 9.30
CHEMBL230262 1 7.04
CHEMBL230261 1 6.92
CHEMBL230367 1 6.75
CHEMBL390642 1 6.70
CHEMBL230260 1 6.19
CHEMBL230153 1 5.40
CHEMBL390197 1 4.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL390196 IC50 = 0.067 nM 10.17
CHEMBL411885 IC50 = 0.5 nM 9.30
CHEMBL230262 IC50 = 91.0 nM 7.04
CHEMBL230261 IC50 = 120.0 nM 6.92
CHEMBL230367 IC50 = 178.0 nM 6.75
CHEMBL390642 IC50 = 198.0 nM 6.70
CHEMBL230260 IC50 = 650.0 nM 6.19
CHEMBL230153 IC50 = 4000.0 nM 5.40
CHEMBL390197 IC50 = 27000.0 nM 4.57