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Assay Detail

CHEMBL998011

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

Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
20
Total Activities
20
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 Autocuration

Target

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

Publication

New insight into the binding mode of peptide ligands at Urotensin-II receptor: structure-activity relationships study on P5U and urantide.
Grieco P, Carotenuto A, Campiglia P, Gomez-Monterrey I, Auriemma L, Sala M, Marcozzi C, d'Emmanuele di Villa Bianca R, Brancaccio D, Rovero P, Santicioli P, Meini S, Maggi CA, Novellino E.
J Med Chem (2009) 52 : 3927 -3940
PubMed 19432421 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 8.40 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL390094 1 9.70
CHEMBL426020 1 9.60
CHEMBL504097 1 9.55
CHEMBL437430 HUMAN UROTENSIN II 1 9.10
CHEMBL509604 1 9.10
CHEMBL510618 1 9.05
CHEMBL448403 1 8.78
CHEMBL524855 1 8.58
CHEMBL507406 1 8.41
CHEMBL223905 URANTIDE 1 8.30
CHEMBL452403 1 8.19
CHEMBL509009 1 8.03
CHEMBL501794 1 8.03
CHEMBL504723 1 8.02
CHEMBL509042 1 7.93
CHEMBL508811 1 7.87
CHEMBL500949 1 7.80
CHEMBL501579 1 7.71
CHEMBL505358 1 7.58
CHEMBL505288 1 6.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL390094 Ki = 0.1995 nM 9.70
CHEMBL426020 Ki = 0.2512 nM 9.60
CHEMBL504097 Ki = 0.2818 nM 9.55
CHEMBL437430 HUMAN UROTENSIN II Ki = 0.7943 nM 9.10
CHEMBL509604 Ki = 0.7943 nM 9.10
CHEMBL510618 Ki = 0.8913 nM 9.05
CHEMBL448403 Ki = 1.66 nM 8.78
CHEMBL524855 Ki = 2.63 nM 8.58
CHEMBL507406 Ki = 3.89 nM 8.41
CHEMBL223905 URANTIDE Ki = 5.012 nM 8.30
CHEMBL452403 Ki = 6.457 nM 8.19
CHEMBL509009 Ki = 9.333 nM 8.03
CHEMBL501794 Ki = 9.333 nM 8.03
CHEMBL504723 Ki = 9.55 nM 8.02
CHEMBL509042 Ki = 11.75 nM 7.93
CHEMBL508811 Ki = 13.49 nM 7.87
CHEMBL500949 Ki = 15.85 nM 7.80
CHEMBL501579 Ki = 19.5 nM 7.71
CHEMBL505358 Ki = 26.3 nM 7.58
CHEMBL505288 Ki = 218.78 nM 6.66