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Assay Detail

CHEMBL1686970

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

Binding
Displacement of [3H]AVP from human vasopressin V2 receptor
3
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Vasopressin V2 receptor (CHEMBL1790)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and SAR studies of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V1b receptor antagonists.
Napier SE, Letourneau JJ, Ansari N, Auld DS, Baker J, Best S, Campbell-Wan L, Chan JH, Craighead M, Desai H, Goan KA, Ho KK, Hulskotte EG, MacSweeney CP, Milne R, Morphy JR, Neagu I, Ohlmeyer MH, Peeters AW, Presland J, Riviello C, Ruigt GS, Thomson FJ, Zanetakos HA, Zhao J, Webb ML.
Bioorg Med Chem Lett (2011) 21 : 1871 -1875
PubMed 21353540 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 - -
Ki 1 6.49 6.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL582857 NELIVAPTAN 2.0 1 6.49
CHEMBL1684573 1 -
CHEMBL1684574 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL582857 NELIVAPTAN Ki = 325.0 nM 6.49
CHEMBL1684573 IC50 > 100000.0 nM -
CHEMBL1684574 IC50 > 100000.0 nM -