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Assay Detail

CHEMBL874235

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

Binding
Inhibition of rabbit lung angiotensin I converting enzyme (ACE) using hippuryl-histidyl-leucine as substrate
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Angiotensin-converting enzyme (CHEMBL4074)
Type SINGLE PROTEIN
Organism Oryctolagus cuniculus

Publication

(Phosphinyloxy)acyl amino acid inhibitors of angiotensin converting enzyme. 2. Terminal amino acid analogues of (S)-1-[6-amino-2 [[hydroxy(4-phenylbutyl)phosphinyl]oxy]-1-oxohexyl]-L-proline.
Karanewsky DS, Badia MC, Cushman DW, DeForrest JM, Dejneka T, Lee VG, Loots MJ, Petrillo EW.
J Med Chem (1990) 33 : 1459 -1469
PubMed 2329568 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 7.61 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL284843 1 9.00
CHEMBL34650 1 8.82
CHEMBL431707 1 8.59
CHEMBL34832 1 8.52
CHEMBL35309 1 8.46
CHEMBL284734 1 8.36
CHEMBL289022 1 8.03
CHEMBL433442 1 8.01
CHEMBL286339 1 7.96
CHEMBL445561 1 7.80
CHEMBL285935 1 7.66
CHEMBL35561 1 7.62
CHEMBL35419 1 7.60
CHEMBL35815 1 7.58
CHEMBL286111 1 7.55
CHEMBL287518 1 7.51
CHEMBL35682 1 7.46
CHEMBL36503 CERONAPRIL 2.0 1 7.44
CHEMBL35656 1 7.41
CHEMBL430918 1 7.37
CHEMBL34821 1 7.09
CHEMBL284135 1 7.04
CHEMBL33025 1 6.85
CHEMBL264758 1 6.84
CHEMBL285939 1 6.80
CHEMBL286659 1 6.77
CHEMBL284272 1 6.57
CHEMBL35310 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL284843 IC50 = 1.0 nM 9.00
CHEMBL34650 IC50 = 1.5 nM 8.82
CHEMBL431707 IC50 = 2.6 nM 8.59
CHEMBL34832 IC50 = 3.0 nM 8.52
CHEMBL35309 IC50 = 3.5 nM 8.46
CHEMBL284734 IC50 = 4.4 nM 8.36
CHEMBL289022 IC50 = 9.3 nM 8.03
CHEMBL433442 IC50 = 9.7 nM 8.01
CHEMBL286339 IC50 = 11.0 nM 7.96
CHEMBL445561 IC50 = 16.0 nM 7.80
CHEMBL285935 IC50 = 22.0 nM 7.66
CHEMBL35561 IC50 = 24.0 nM 7.62
CHEMBL35419 IC50 = 25.0 nM 7.60
CHEMBL35815 IC50 = 26.0 nM 7.58
CHEMBL286111 IC50 = 28.0 nM 7.55
CHEMBL287518 IC50 = 31.0 nM 7.51
CHEMBL35682 IC50 = 35.0 nM 7.46
CHEMBL36503 CERONAPRIL IC50 = 36.0 nM 7.44
CHEMBL35656 IC50 = 39.0 nM 7.41
CHEMBL430918 IC50 = 43.0 nM 7.37
CHEMBL34821 IC50 = 81.0 nM 7.09
CHEMBL284135 IC50 = 91.0 nM 7.04
CHEMBL33025 IC50 = 140.0 nM 6.85
CHEMBL264758 IC50 = 145.0 nM 6.84
CHEMBL285939 IC50 = 160.0 nM 6.80
CHEMBL286659 IC50 = 170.0 nM 6.77
CHEMBL284272 IC50 = 270.0 nM 6.57
CHEMBL35310 IC50 = 320.0 nM 6.50