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Assay Detail

CHEMBL801066

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

Binding
In vitro inhibition of purified Human kidney renin (250 pg/mL) incubated with angiotensinogen at pH 7.2
13
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Kidney
Confidence 9 — Direct single protein target
Curated By Expert

Target

Renin (CHEMBL286)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological activity of some transition-state inhibitors of human renin.
Bühlmayer P, Caselli A, Fuhrer W, Göschke R, Rasetti V, Rüeger H, Stanton JL, Criscione L, Wood JM.
J Med Chem (1988) 31 : 1839 -1846
PubMed 3137345 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 8.17 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL53139 3 8.70
CHEMBL52833 1 8.70
CHEMBL291787 1 8.40
CHEMBL52929 1 8.40
CHEMBL292812 1 8.22
CHEMBL55787 1 8.15
CHEMBL407670 1 8.00
CHEMBL435178 1 7.82
CHEMBL54655 1 7.70
CHEMBL52395 1 7.70
CHEMBL54322 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL53139 IC50 = 2.0 nM 8.70
CHEMBL52833 IC50 = 2.0 nM 8.70
CHEMBL53139 IC50 = 2.0 nM 8.70
CHEMBL291787 IC50 = 4.0 nM 8.40
CHEMBL52929 IC50 = 4.0 nM 8.40
CHEMBL292812 IC50 = 6.0 nM 8.22
CHEMBL55787 IC50 = 7.0 nM 8.15
CHEMBL53139 IC50 = 10.0 nM 8.00
CHEMBL407670 IC50 = 10.0 nM 8.00
CHEMBL435178 IC50 = 15.0 nM 7.82
CHEMBL54655 IC50 = 20.0 nM 7.70
CHEMBL52395 IC50 = 20.0 nM 7.70
CHEMBL54322 IC50 = 20.0 nM 7.70