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Assay Detail

CHEMBL1051576

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Functional
Antagonist activity at vasopressin V1a receptor in phenoxybenzamine-treated Wistar rat uterus assessed as inhibition of vasopressin-induced arterial vasopressor activity treated 1 min prior to vasopressin challenge
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Uterus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Vasopressin V1a receptor (CHEMBL2868)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Arginine vasopressin and its analogues--the influence of position 2 modification with 3,3-diphenylalanine enantiomers. Highly potent V2 agonists.
Kwiatkowska A, Sobolewski D, Prahl A, Borovicková L, Slaninová J, Lammek B.
Eur J Med Chem (2009) 44 : 2862 -2867
PubMed 19418631 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 6 6.94 8.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL553710 1 8.35
CHEMBL558950 1 7.40
CHEMBL538934 1 6.20
CHEMBL541246 1 5.80
CHEMBL555452 1 -
CHEMBL540754 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL553710 Kd = 4.467 nM 8.35
CHEMBL558950 Kd = 39.81 nM 7.40
CHEMBL538934 Kd = 630.96 nM 6.20
CHEMBL541246 Kd = 1584.89 nM 5.80
CHEMBL555452 Kd > 1584.89 nM -
CHEMBL540754 Kd > 1584.89 nM -