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Assay Detail

CHEMBL930369

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

Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL ↗
45
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

2-Aminomethyl piperidines as novel urotensin-II receptor antagonists.
Jin J, Wang Y, Wang F, Shi D, Erhard KF, Wu Z, Guida BF, Lawrence SK, Behm DJ, Disa J, Vaidya KS, Evans C, McMillan LJ, Rivero RA, Neeb MJ, Douglas SA.
Bioorg Med Chem Lett (2008) 18 : 2860 -2864
PubMed 18420409 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 45 6.65 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL404177 — — 2 8.40
CHEMBL402303 — — 2 8.20
CHEMBL403947 — — 1 8.10
CHEMBL255927 — — 1 7.80
CHEMBL257337 — — 1 7.60
CHEMBL255665 — — 1 7.50
CHEMBL256138 — — 1 7.50
CHEMBL256160 — — 1 7.50
CHEMBL256365 — — 1 7.30
CHEMBL257349 — — 1 7.20
CHEMBL402304 — — 1 7.10
CHEMBL256300 — — 1 7.10
CHEMBL256299 — — 1 7.10
CHEMBL256773 — — 1 7.00
CHEMBL437216 — — 1 6.80
CHEMBL403833 — — 1 6.70
CHEMBL256516 — — 1 6.70
CHEMBL256140 — — 1 6.70
CHEMBL257563 — — 1 6.60
CHEMBL253749 — — 1 6.40
CHEMBL254154 — — 1 6.40
CHEMBL256774 — — 1 6.30
CHEMBL254994 — — 1 6.30
CHEMBL255664 — — 1 6.20
CHEMBL253747 — — 1 6.10
CHEMBL404244 — — 1 6.10
CHEMBL257552 — — 1 6.10
CHEMBL257365 — — 1 6.00
CHEMBL446717 — — 1 5.90
CHEMBL254153 — — 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL404177 — Ki = 3.981 nM 8.40
CHEMBL402303 — Ki = 6.31 nM 8.20
CHEMBL404177 — Ki = 7.943 nM 8.10
CHEMBL403947 — Ki = 7.943 nM 8.10
CHEMBL402303 — Ki = 15.85 nM 7.80
CHEMBL255927 — Ki = 15.85 nM 7.80
CHEMBL257337 — Ki = 25.12 nM 7.60
CHEMBL256160 — Ki = 31.62 nM 7.50
CHEMBL256138 — Ki = 31.62 nM 7.50
CHEMBL255665 — Ki = 31.62 nM 7.50
CHEMBL256365 — Ki = 50.12 nM 7.30
CHEMBL257349 — Ki = 63.1 nM 7.20
CHEMBL402304 — Ki = 79.43 nM 7.10
CHEMBL256300 — Ki = 79.43 nM 7.10
CHEMBL256299 — Ki = 79.43 nM 7.10
CHEMBL256773 — Ki = 100.0 nM 7.00
CHEMBL437216 — Ki = 158.49 nM 6.80
CHEMBL403833 — Ki = 199.53 nM 6.70
CHEMBL256140 — Ki = 199.53 nM 6.70
CHEMBL256516 — Ki = 199.53 nM 6.70
CHEMBL257563 — Ki = 251.19 nM 6.60
CHEMBL253749 — Ki = 398.11 nM 6.40
CHEMBL254154 — Ki = 398.11 nM 6.40
CHEMBL254994 — Ki = 501.19 nM 6.30
CHEMBL256774 — Ki = 501.19 nM 6.30
CHEMBL255664 — Ki = 630.96 nM 6.20
CHEMBL253747 — Ki = 794.33 nM 6.10
CHEMBL257552 — Ki = 794.33 nM 6.10
CHEMBL404244 — Ki = 794.33 nM 6.10
CHEMBL257365 — Ki = 1000.0 nM 6.00
CHEMBL446717 — Ki = 1258.93 nM 5.90
CHEMBL256159 — Ki = 1584.89 nM 5.80
CHEMBL254153 — Ki = 1584.89 nM 5.80
CHEMBL258017 — Ki = 1995.26 nM 5.70
CHEMBL402543 — Ki = 2511.89 nM 5.60
CHEMBL412746 — Ki = 3162.28 nM 5.50
CHEMBL439244 — Ki = 3162.28 nM 5.50
CHEMBL253540 — Ki = 3981.07 nM 5.40
CHEMBL257187 — Ki = 7943.28 nM 5.10
CHEMBL254995 — Ki = 7943.28 nM 5.10
CHEMBL402028 — Ki < 7943.28 nM -
CHEMBL258220 — Ki < 7943.28 nM -
CHEMBL402175 — Ki < 7943.28 nM -
CHEMBL403397 — Ki < 7943.28 nM -
CHEMBL402233 — Ki < 7943.28 nM -