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Assay Detail

CHEMBL915482

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

Binding
Displacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Urotensin-II receptor ligands. From agonist to antagonist activity.
Grieco P, Carotenuto A, Campiglia P, Marinelli L, Lama T, Patacchini R, Santicioli P, Maggi CA, Rovero P, Novellino E.
J Med Chem (2005) 48 : 7290 -7297
PubMed 16279788 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 8.21 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL390094 1 9.70
CHEMBL426020 1 9.60
CHEMBL437430 HUMAN UROTENSIN II 1 9.10
CHEMBL224616 1 8.90
CHEMBL388060 1 8.90
CHEMBL223905 URANTIDE 1 8.30
CHEMBL389654 1 8.00
CHEMBL387916 1 7.90
CHEMBL389653 1 7.80
CHEMBL439551 1 6.40
CHEMBL375241 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL390094 Ki = 0.1995 nM 9.70
CHEMBL426020 Ki = 0.2512 nM 9.60
CHEMBL437430 HUMAN UROTENSIN II Ki = 0.7943 nM 9.10
CHEMBL224616 Ki = 1.259 nM 8.90
CHEMBL388060 Ki = 1.259 nM 8.90
CHEMBL223905 URANTIDE Ki = 5.012 nM 8.30
CHEMBL389654 Ki = 10.0 nM 8.00
CHEMBL387916 Ki = 12.59 nM 7.90
CHEMBL389653 Ki = 15.85 nM 7.80
CHEMBL439551 Ki = 398.11 nM 6.40
CHEMBL375241 Ki = 1995.26 nM 5.70