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Assay Detail

CHEMBL5554473

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Functional
Modulation of human UTR stably expressed in HEK293 cells assessed as increase in Ca2+ level by Fura 2-AM dye based calcium mobilization assay
4
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Urotensin-2 receptor (CHEMBL3764)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Expanding Structure-Activity Relationships of Human Urotensin II Peptide Analogues: A Proposed Key Role of the N-Terminal Region for Novel Urotensin II Receptor Modulators.
Merlino F, Secondo A, Mitidieri E, Sorrentino R, Bellavita R, Grasso N, Chatenet D, Pannaccione A, Grieco P, d'Emmanuele di Villa Bianca R, Carotenuto A.
J Med Chem (2024) 67 : 13879 -13890
PubMed 39096311 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Activity 2 - -
EC50 2 9.07 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL593662 UROTENSIN-II 2 9.22
CHEMBL218994 2 8.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL593662 UROTENSIN-II EC50 = 0.6 nM 9.22
CHEMBL218994 EC50 = 1.2 nM 8.92
CHEMBL218994 Activity - -
CHEMBL593662 UROTENSIN-II Activity - -