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Assay Detail

CHEMBL3789066

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

Binding
Displacement of [3H]-Asp-{Nomega-[N-(4-propanoylaminobutyl)aminocarbonyl]}Arg-ValTyr-Ile-His-Pro-Phe-OH Tris(hydrotrifluoroacetate) from human AT1 receptor transfected in CHO cells co-expressing Galpha16-mtAEQ after 2 hrs by liquid scintillation counting
14
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Type-1 angiotensin II receptor (CHEMBL227)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Mimicking of Arginine by Functionalized N(ω)-Carbamoylated Arginine As a New Broadly Applicable Approach to Labeled Bioactive Peptides: High Affinity Angiotensin, Neuropeptide Y, Neuropeptide FF, and Neurotensin Receptor Ligands As Examples.
Keller M, Kuhn KK, Einsiedel J, Hübner H, Biselli S, Mollereau C, Wifling D, Svobodová J, Bernhardt G, Cabrele C, Vanderheyden PM, Gmeiner P, Buschauer A.
J Med Chem (2016) 59 : 1925 -1945
PubMed 26824643 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 8.54 9.62
IC50 5 8.31 9.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL408403 ANGIOTENSIN II 4.0 2 9.62
CHEMBL3787243 2 9.15
CHEMBL3786145 2 8.68
CHEMBL3786986 1 8.55
CHEMBL3787379 1 8.51
CHEMBL1016 CANDESARTAN 3.0 2 8.46
CHEMBL3785563 2 8.05
CHEMBL191 LOSARTAN 4.0 1 7.92
CHEMBL4299329 1 7.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL408403 ANGIOTENSIN II Ki = 0.24 nM 9.62
CHEMBL3787243 Ki = 0.71 nM 9.15
CHEMBL408403 ANGIOTENSIN II IC50 = 0.7244 nM 9.14
CHEMBL3786145 Ki = 2.1 nM 8.68
CHEMBL3787243 IC50 = 2.188 nM 8.66
CHEMBL3786986 Ki = 2.8 nM 8.55
CHEMBL3787379 Ki = 3.1 nM 8.51
CHEMBL1016 CANDESARTAN Ki = 3.5 nM 8.46
CHEMBL3786145 IC50 = 6.166 nM 8.21
CHEMBL3785563 Ki = 9.0 nM 8.05
CHEMBL1016 CANDESARTAN IC50 = 10.72 nM 7.97
CHEMBL191 LOSARTAN Ki = 12.0 nM 7.92
CHEMBL4299329 Ki = 13.0 nM 7.89
CHEMBL3785563 IC50 = 28.18 nM 7.55