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Assay Detail

CHEMBL4370024

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

Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Functional Selectivity Revealed by N-Methylation Scanning of Human Urotensin II and Related Peptides.
Merlino F, Billard É, Yousif AM, Di Maro S, Brancaccio D, Abate L, Carotenuto A, Bellavita R, d'Emmanuele di Villa Bianca R, Santicioli P, Marinelli L, Novellino E, Hébert TE, Lubell WD, Chatenet D, Grieco P.
J Med Chem (2019) 62 : 1455 -1467
PubMed 30615452 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 7.40 8.76

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4472928 1 8.76
CHEMBL4568153 1 8.76
CHEMBL4526244 1 8.66
CHEMBL4590360 1 8.53
CHEMBL4462940 1 8.45
CHEMBL4454498 1 8.45
CHEMBL218994 1 8.34
CHEMBL3104471 1 8.20
CHEMBL593662 UROTENSIN-II 1 8.11
CHEMBL4475783 1 7.69
CHEMBL4474481 1 7.64
CHEMBL4449844 1 7.31
CHEMBL4568539 1 6.64
CHEMBL4447811 1 6.61
CHEMBL4467241 1 6.09
CHEMBL4483461 1 5.82
CHEMBL4549818 1 5.68
CHEMBL4455086 1 5.67
CHEMBL4565187 1 5.27
CHEMBL4544618 1 -
CHEMBL4540501 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4472928 Ki = 1.738 nM 8.76
CHEMBL4568153 Ki = 1.738 nM 8.76
CHEMBL4526244 Ki = 2.188 nM 8.66
CHEMBL4590360 Ki = 2.951 nM 8.53
CHEMBL4462940 Ki = 3.548 nM 8.45
CHEMBL4454498 Ki = 3.548 nM 8.45
CHEMBL218994 Ki = 4.571 nM 8.34
CHEMBL3104471 Ki = 6.31 nM 8.20
CHEMBL593662 UROTENSIN-II Ki = 7.762 nM 8.11
CHEMBL4475783 Ki = 20.42 nM 7.69
CHEMBL4474481 Ki = 22.91 nM 7.64
CHEMBL4449844 Ki = 48.98 nM 7.31
CHEMBL4568539 Ki = 229.09 nM 6.64
CHEMBL4447811 Ki = 245.47 nM 6.61
CHEMBL4467241 Ki = 812.83 nM 6.09
CHEMBL4483461 Ki = 1513.56 nM 5.82
CHEMBL4549818 Ki = 2089.3 nM 5.68
CHEMBL4455086 Ki = 2137.96 nM 5.67
CHEMBL4565187 Ki = 5370.32 nM 5.27
CHEMBL4544618 Ki > 10000.0 nM -
CHEMBL4540501 Ki > 10000.0 nM -