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Assay Detail

CHEMBL648484

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Binding
In vitro inhibitory activity against angiotensin I converting enzyme of rats.
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Angiotensin-converting enzyme (CHEMBL2625)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Angiotensin-converting enzyme inhibitors. Mercaptan, carboxyalkyl dipeptide, and phosphinic acid inhibitors incorporating 4-substituted prolines.
Krapcho J, Turk C, Cushman DW, Powell JR, DeForrest JM, Spitzmiller ER, Karanewsky DS, Duggan M, Rovnyak G, Schwartz J.
J Med Chem (1988) 31 : 1148 -1160
PubMed 2836590 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 8.09 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL277976 1 8.70
CHEMBL16190 1 8.70
CHEMBL279763 1 8.70
CHEMBL16163 1 8.70
CHEMBL579 SPIRAPRILAT 2.0 1 8.70
CHEMBL15954 1 8.70
CHEMBL16138 1 8.55
CHEMBL279566 1 8.54
CHEMBL277951 1 8.52
CHEMBL577 ENALAPRILAT ANHYDROUS 4.0 1 8.40
CHEMBL417810 1 8.30
CHEMBL277074 1 8.30
CHEMBL15879 1 8.30
CHEMBL16139 1 8.19
CHEMBL276104 1 8.14
CHEMBL16332 ZOFENOPRILAT 2.0 1 8.10
CHEMBL417994 1 8.07
CHEMBL276505 1 7.96
CHEMBL15424 1 7.92
CHEMBL15775 1 7.89
CHEMBL276103 1 7.80
CHEMBL16166 1 7.77
CHEMBL1560 CAPTOPRIL 4.0 1 7.64
CHEMBL278428 1 7.58
CHEMBL15777 1 7.55
CHEMBL15977 1 7.52
CHEMBL279154 1 7.34
CHEMBL274988 1 7.02
CHEMBL278427 1 7.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL277976 IC50 = 2.0 nM 8.70
CHEMBL16190 IC50 = 2.0 nM 8.70
CHEMBL279763 IC50 = 2.0 nM 8.70
CHEMBL16163 IC50 = 2.0 nM 8.70
CHEMBL579 SPIRAPRILAT IC50 = 2.0 nM 8.70
CHEMBL15954 IC50 = 2.0 nM 8.70
CHEMBL16138 IC50 = 2.8 nM 8.55
CHEMBL279566 IC50 = 2.9 nM 8.54
CHEMBL277951 IC50 = 3.0 nM 8.52
CHEMBL577 ENALAPRILAT ANHYDROUS IC50 = 4.0 nM 8.40
CHEMBL417810 IC50 = 5.0 nM 8.30
CHEMBL277074 IC50 = 5.0 nM 8.30
CHEMBL15879 IC50 = 5.0 nM 8.30
CHEMBL16139 IC50 = 6.5 nM 8.19
CHEMBL276104 IC50 = 7.2 nM 8.14
CHEMBL16332 ZOFENOPRILAT IC50 = 8.0 nM 8.10
CHEMBL417994 IC50 = 8.6 nM 8.07
CHEMBL276505 IC50 = 11.0 nM 7.96
CHEMBL15424 IC50 = 12.0 nM 7.92
CHEMBL15775 IC50 = 13.0 nM 7.89
CHEMBL276103 IC50 = 16.0 nM 7.80
CHEMBL16166 IC50 = 17.0 nM 7.77
CHEMBL1560 CAPTOPRIL IC50 = 23.0 nM 7.64
CHEMBL278428 IC50 = 26.0 nM 7.58
CHEMBL15777 IC50 = 28.0 nM 7.55
CHEMBL15977 IC50 = 30.0 nM 7.52
CHEMBL279154 IC50 = 46.0 nM 7.34
CHEMBL274988 IC50 = 96.0 nM 7.02
CHEMBL278427 IC50 = 97.0 nM 7.01