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Assay Detail

CHEMBL1048828

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

Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL ↗
47
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type RMS13
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Nonpeptide urotensin-II receptor antagonists: a new ligand class based on piperazino-phthalimide and piperazino-isoindolinone subunits.
Lawson EC, Luci DK, Ghosh S, Kinney WA, Reynolds CH, Qi J, Smith CE, Wang Y, Minor LK, Haertlein BJ, Parry TJ, Damiano BP, Maryanoff BE.
J Med Chem (2009) 52 : 7432 -7445
PubMed 19731961 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 47 7.13 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL568637 — — 1 8.40
CHEMBL567713 — — 1 8.40
CHEMBL522770 — — 1 8.10
CHEMBL571625 — — 1 8.10
CHEMBL578205 — — 1 7.96
CHEMBL578203 — — 1 7.96
CHEMBL567759 — — 1 7.89
CHEMBL578206 — — 1 7.82
CHEMBL565395 — — 1 7.80
CHEMBL568123 — — 1 7.75
CHEMBL567075 — — 1 7.75
CHEMBL578207 — — 1 7.60
CHEMBL565806 — — 1 7.50
CHEMBL566433 — — 1 7.46
CHEMBL567303 PALOSURAN 2.0 1 7.39
CHEMBL571537 — — 1 7.36
CHEMBL567736 — — 1 7.35
CHEMBL568165 — — 1 7.31
CHEMBL565416 — — 1 7.31
CHEMBL578204 — — 1 7.23
CHEMBL567949 — — 1 7.23
CHEMBL566056 — — 1 7.21
CHEMBL566894 — — 1 7.19
CHEMBL568316 — — 1 7.12
CHEMBL565388 — — 1 7.06
CHEMBL569923 — — 1 7.01
CHEMBL565580 — — 1 6.92
CHEMBL568764 — — 1 6.89
CHEMBL566366 — — 1 6.82
CHEMBL566187 — — 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL568637 — Ki = 4.0 nM 8.40
CHEMBL567713 — Ki = 4.0 nM 8.40
CHEMBL571625 — Ki = 8.0 nM 8.10
CHEMBL522770 — Ki = 8.0 nM 8.10
CHEMBL578205 — Ki = 11.0 nM 7.96
CHEMBL578203 — Ki = 11.0 nM 7.96
CHEMBL567759 — Ki = 13.0 nM 7.89
CHEMBL578206 — Ki = 15.0 nM 7.82
CHEMBL565395 — Ki = 16.0 nM 7.80
CHEMBL568123 — Ki = 18.0 nM 7.75
CHEMBL567075 — Ki = 18.0 nM 7.75
CHEMBL578207 — Ki = 25.0 nM 7.60
CHEMBL565806 — Ki = 32.0 nM 7.50
CHEMBL566433 — Ki = 35.0 nM 7.46
CHEMBL567303 PALOSURAN Ki = 41.0 nM 7.39
CHEMBL571537 — Ki = 44.0 nM 7.36
CHEMBL567736 — Ki = 45.0 nM 7.35
CHEMBL568165 — Ki = 49.0 nM 7.31
CHEMBL565416 — Ki = 49.0 nM 7.31
CHEMBL578204 — Ki = 59.0 nM 7.23
CHEMBL567949 — Ki = 59.0 nM 7.23
CHEMBL566056 — Ki = 62.0 nM 7.21
CHEMBL566894 — Ki = 64.0 nM 7.19
CHEMBL568316 — Ki = 76.0 nM 7.12
CHEMBL565388 — Ki = 87.0 nM 7.06
CHEMBL569923 — Ki = 97.0 nM 7.01
CHEMBL565580 — Ki = 120.0 nM 6.92
CHEMBL568764 — Ki = 130.0 nM 6.89
CHEMBL566366 — Ki = 150.0 nM 6.82
CHEMBL566187 — Ki = 160.0 nM 6.80
CHEMBL577518 — Ki = 160.0 nM 6.80
CHEMBL569688 — Ki = 200.0 nM 6.70
CHEMBL571683 — Ki = 230.0 nM 6.64
CHEMBL566565 — Ki = 270.0 nM 6.57
CHEMBL569238 — Ki = 290.0 nM 6.54
CHEMBL566364 — Ki = 310.0 nM 6.51
CHEMBL565937 — Ki = 310.0 nM 6.51
CHEMBL566389 — Ki = 310.0 nM 6.51
CHEMBL567866 — Ki = 430.0 nM 6.37
CHEMBL568089 — Ki = 540.0 nM 6.27
CHEMBL572138 — Ki = 570.0 nM 6.24
CHEMBL566144 — Ki = 700.0 nM 6.16
CHEMBL569689 — Ki = 1400.0 nM 5.85
CHEMBL584545 — Ki = 3200.0 nM 5.50
CHEMBL571216 — Ki < 6.0 nM -
CHEMBL571535 — Ki < 5.0 nM -
CHEMBL568358 — Ki > 10000.0 nM -