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Assay Detail

CHEMBL4397501

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

Binding
Agonist activity at human OTR stably expressed in CHOK1 cells by NFAT-luciferase reporter gene assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Oxytocin receptor (CHEMBL2049)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Potent, Selective, and Short-Acting Peptidic V<sub>2</sub> Receptor Agonists.
Wiśniewski K, Qi S, Kraus J, Ly B, Srinivasan K, Tariga H, Croston G, La E, Wiśniewska H, Ortiz C, Laporte R, Rivière PJ, Neyer G, Hargrove DM, Schteingart CD.
J Med Chem (2019) 62 : 4991 -5005
PubMed 31022340 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 6.74 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1429 DESMOPRESSIN 4.0 1 6.96
CHEMBL4531053 1 6.85
CHEMBL4454891 1 6.80
CHEMBL4528032 1 6.64
CHEMBL435323 1 6.46
CHEMBL4462743 1 -
CHEMBL4474518 1 -
CHEMBL4532363 1 -
CHEMBL4435502 1 -
CHEMBL4552500 1 -
CHEMBL4521602 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1429 DESMOPRESSIN EC50 = 110.0 nM 6.96
CHEMBL4531053 EC50 = 140.0 nM 6.85
CHEMBL4454891 EC50 = 160.0 nM 6.80
CHEMBL4528032 EC50 = 230.0 nM 6.64
CHEMBL435323 EC50 = 350.0 nM 6.46
CHEMBL4462743 EC50 > 10000.0 nM -
CHEMBL4474518 EC50 > 10000.0 nM -
CHEMBL4532363 EC50 > 10000.0 nM -
CHEMBL4435502 EC50 > 10000.0 nM -
CHEMBL4552500 EC50 > 10000.0 nM -
CHEMBL4521602 EC50 > 10000.0 nM -