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Assay Detail

CHEMBL818375

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

Binding
Binding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from rats
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Kidney
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Vasopressin V2 receptor (CHEMBL3766)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

1-(1-[4-[(N-acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]piperidin-4- yl)-4H-3,1-benzoxazin-2(1H)-one (L-371,257): a new, orally bioavailable, non-peptide oxytocin antagonist.
Williams PD, Clineschmidt BV, Erb JM, Freidinger RM, Guidotti MT, Lis EV, Pawluczyk JM, Pettibone DJ, Reiss DR, Veber DF.
J Med Chem (1995) 38 : 4634 -4636
PubMed 7473590 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 4.79 4.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL344752 1 4.96
CHEMBL142324 1 4.96
CHEMBL358793 1 4.46
CHEMBL24781 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL344752 Ki = 11000.0 nM 4.96
CHEMBL142324 Ki = 11000.0 nM 4.96
CHEMBL358793 Ki = 35000.0 nM 4.46
CHEMBL24781 Ki > 30000.0 nM -