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Assay Detail

CHEMBL1837360

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Functional
Antagonist activity at human V2 receptor
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of PF-184563, a potent and selective V1a antagonist for the treatment of dysmenorrhoea. The influence of compound flexibility on microsomal stability.
Johnson PS, Ryckmans T, Bryans J, Beal DM, Dack KN, Feeder N, Harrison A, Lewis M, Mason HJ, Mills J, Newman J, Pasquinet C, Rawson DJ, Roberts LR, Russell R, Spark D, Stobie A, Underwood TJ, Ward R, Wheeler S.
Bioorg Med Chem Lett (2011) 21 : 5684 -5687
PubMed 21885275 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.52 6.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1837041 1 6.15
CHEMBL1837040 1 5.35
CHEMBL1837037 1 5.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1837041 IC50 = 715.0 nM 6.15
CHEMBL1837040 IC50 = 4500.0 nM 5.35
CHEMBL1837037 IC50 = 8490.0 nM 5.07