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Assay Detail

CHEMBL1787849

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

Binding
Displacement of [3H]AL-11 from IRAP of CHO-K1 cell membrane after 30 mins by scintillation counting in presence of 30 mM EDTA and 600 uM 1,10-Phenantrone
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cricetulus griseus
Cell Type CHO-K1
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Potent macrocyclic inhibitors of insulin-regulated aminopeptidase (IRAP) by olefin ring-closing metathesis.
Andersson H, Demaegdt H, Johnsson A, Vauquelin G, Lindeberg G, Hallberg M, Erdelyi M, Karlen A, Hallberg A.
J Med Chem (2011) 54 : 3779 -3792
PubMed 21476495 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.41 8.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL261120 ANGIOTENSIN IV 1 8.03
CHEMBL1782887 1 8.01
CHEMBL1782882 1 7.90
CHEMBL1782888 1 7.61
CHEMBL1782886 1 7.61
CHEMBL1782883 1 7.54
CHEMBL1782885 1 7.43
CHEMBL1782881 1 7.33
CHEMBL1782890 1 6.54
CHEMBL1782889 1 6.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL261120 ANGIOTENSIN IV Ki = 9.3 nM 8.03
CHEMBL1782887 Ki = 9.8 nM 8.01
CHEMBL1782882 Ki = 12.5 nM 7.90
CHEMBL1782888 Ki = 24.5 nM 7.61
CHEMBL1782886 Ki = 24.8 nM 7.61
CHEMBL1782883 Ki = 28.9 nM 7.54
CHEMBL1782885 Ki = 36.8 nM 7.43
CHEMBL1782881 Ki = 46.8 nM 7.33
CHEMBL1782890 Ki = 287.0 nM 6.54
CHEMBL1782889 Ki = 719.0 nM 6.14