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Assay Detail

CHEMBL4390280

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Functional
Agonist activity at human V1A receptor expressed in HEK293 cells assessed as intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Vasopressin V1a receptor (CHEMBL1889)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of oxytocin derivatives lipidated via a carbonate or carbamate linkage as a long-acting therapeutic agent for social impairment-like behaviors.
Cherepanov SM, Miura R, Shabalova AA, Ichinose W, Yokoyama S, Fukuda H, Watanabe M, Higashida H, Shuto S.
Bioorg Med Chem (2019) 27 : 3358 -3363
PubMed 31229420 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 9.74 9.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL395429 OXYTOCIN 4.0 1 9.74
CHEMBL4550879 1 -
CHEMBL4442132 1 -
CHEMBL4447096 1 -
CHEMBL4460287 1 -
CHEMBL4469555 1 -
CHEMBL4453936 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL395429 OXYTOCIN EC50 = 0.18 nM 9.74
CHEMBL4550879 EC50 > 100000.0 nM -
CHEMBL4442132 EC50 > 100000.0 nM -
CHEMBL4447096 EC50 > 100000.0 nM -
CHEMBL4460287 EC50 > 100000.0 nM -
CHEMBL4469555 EC50 > 100000.0 nM -
CHEMBL4453936 EC50 > 100000.0 nM -