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Assay Detail

CHEMBL3789064

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Functional
Agonist activity at human AT1 receptor transfected in CHO cells co-expressing Galpha16-mtAEQ assessed as induction of intracellular Ca2+ mobilization by bioluminescence assay
12
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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
EC50 12 8.88 9.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL408403 ANGIOTENSIN II 4.0 2 9.31
CHEMBL3787243 2 8.96
CHEMBL3786145 2 8.85
CHEMBL3786986 2 8.69
CHEMBL3787379 2 8.63
CHEMBL3785563 1 -
CHEMBL4299329 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL408403 ANGIOTENSIN II EC50 = 0.4898 nM 9.31
CHEMBL408403 ANGIOTENSIN II EC50 = 0.52 nM 9.28
CHEMBL3787243 EC50 = 1.1 nM 8.96
CHEMBL3787243 EC50 = 1.096 nM 8.96
CHEMBL3786145 EC50 = 1.4 nM 8.85
CHEMBL3786145 EC50 = 1.413 nM 8.85
CHEMBL3786986 EC50 = 2.042 nM 8.69
CHEMBL3786986 EC50 = 2.1 nM 8.68
CHEMBL3787379 EC50 = 2.344 nM 8.63
CHEMBL3787379 EC50 = 2.4 nM 8.62
CHEMBL3785563 EC50 - -
CHEMBL4299329 EC50 - -