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Assay Detail

CHEMBL648528

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Binding
In vitro inhibitory activity against rat serum angiotensin I converting enzyme using hippuryl-glycyl-glycine as substrate
ChEMBL ↗
48
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

1,2-Cyclomethylenecarboxylic monoamide hydroxamic derivatives. A novel class of non-amino acid angiotensin converting enzyme inhibitors.
Turbanti L, Cerbai G, Di Bugno C, Giorgi R, Garzelli G, Criscuoli M, Renzetti AR, Subissi A, Bramanti G, DePriest SA.
J Med Chem (1993) 36 : 699 -707
PubMed 8459398 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 48 6.23 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1560 CAPTOPRIL 4.0 1 8.52
CHEMBL354470 — — 6 8.15
CHEMBL349351 — — 6 7.85
CHEMBL159829 — — 2 6.82
CHEMBL352453 — — 1 6.30
CHEMBL351966 — — 1 6.22
CHEMBL159791 — — 2 5.85
CHEMBL434293 — — 1 5.85
CHEMBL161968 — — 2 5.82
CHEMBL163549 — — 2 5.00
CHEMBL163601 — — 1 4.96
CHEMBL351061 — — 1 4.28
CHEMBL163568 — — 2 4.12
CHEMBL159987 — — 1 -
CHEMBL159973 — — 1 -
CHEMBL351263 — — 1 -
CHEMBL159956 — — 2 -
CHEMBL351972 — — 4 -
CHEMBL351655 — — 4 -
CHEMBL159330 — — 1 -
CHEMBL161552 — — 2 -
CHEMBL159996 — — 2 -
CHEMBL159995 — — 1 -
CHEMBL302840 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1560 CAPTOPRIL IC50 = 3.0 nM 8.52
CHEMBL354470 — IC50 = 7.0 nM 8.15
CHEMBL354470 — IC50 = 12.0 nM 7.92
CHEMBL349351 — IC50 = 14.0 nM 7.85
CHEMBL349351 — IC50 = 18.0 nM 7.75
CHEMBL354470 — IC50 = 24.0 nM 7.62
CHEMBL349351 — IC50 = 28.0 nM 7.55
CHEMBL354470 — IC50 = 45.0 nM 7.35
CHEMBL349351 — IC50 = 57.0 nM 7.24
CHEMBL159829 — IC50 = 150.0 nM 6.82
CHEMBL159829 — IC50 = 400.0 nM 6.40
CHEMBL352453 — IC50 = 500.0 nM 6.30
CHEMBL351966 — IC50 = 600.0 nM 6.22
CHEMBL434293 — IC50 = 1400.0 nM 5.85
CHEMBL159791 — IC50 = 1400.0 nM 5.85
CHEMBL161968 — IC50 = 1500.0 nM 5.82
CHEMBL159791 — IC50 = 1700.0 nM 5.77
CHEMBL354470 — IC50 = 1800.0 nM 5.75
CHEMBL349351 — IC50 = 2900.0 nM 5.54
CHEMBL349351 — IC50 = 2900.0 nM 5.54
CHEMBL161968 — IC50 = 3000.0 nM 5.52
CHEMBL163549 — IC50 = 10000.0 nM 5.00
CHEMBL163601 — IC50 = 11000.0 nM 4.96
CHEMBL354470 — IC50 = 23500.0 nM 4.63
CHEMBL351061 — IC50 = 52000.0 nM 4.28
CHEMBL163568 — IC50 = 75000.0 nM 4.12
CHEMBL163568 — IC50 = 97000.0 nM 4.01
CHEMBL351655 — IC50 > 150000.0 nM -
CHEMBL159987 — IC50 > 150000.0 nM -
CHEMBL351263 — IC50 > 150000.0 nM -
CHEMBL159973 — IC50 > 150000.0 nM -
CHEMBL159956 — IC50 > 150000.0 nM -
CHEMBL159996 — IC50 > 150000.0 nM -
CHEMBL351655 — IC50 > 150000.0 nM -
CHEMBL163549 — IC50 > 150000.0 nM -
CHEMBL351655 — IC50 > 150000.0 nM -
CHEMBL351972 — IC50 > 150000.0 nM -
CHEMBL351972 — IC50 > 150000.0 nM -
CHEMBL351972 — IC50 > 150000.0 nM -
CHEMBL159330 — IC50 > 150000.0 nM -
CHEMBL351972 — IC50 > 150000.0 nM -
CHEMBL161552 — IC50 > 150000.0 nM -
CHEMBL351655 — IC50 > 150000.0 nM -
CHEMBL161552 — IC50 > 150000.0 nM -
CHEMBL159956 — IC50 > 150000.0 nM -
CHEMBL159995 — IC50 > 150000.0 nM -
CHEMBL302840 — IC50 = 624000.0 nM -
CHEMBL159996 — IC50 > 150000.0 nM -