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Assay Detail

CHEMBL4392279

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

Functional
Agonist activity at recombinant human OTR expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method
9
Total Activities
9
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

Oxytocin receptor (CHEMBL2049)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of a Highly Potent Analogue and a Long-Acting Analogue of Oxytocin for the Treatment of Social Impairment-Like Behaviors.
Ichinose W, Cherepanov SM, Shabalova AA, Yokoyama S, Yuhi T, Yamaguchi H, Watanabe A, Yamamoto Y, Okamoto H, Horike S, Terakawa J, Daikoku T, Watanabe M, Mano N, Higashida H, Shuto S.
J Med Chem (2019) 62 : 3297 -3310
PubMed 30896946 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 10.26 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL395429 OXYTOCIN 4.0 1 11.00
CHEMBL3354594 1 10.60
CHEMBL4474284 1 10.55
CHEMBL4583231 1 10.51
CHEMBL4458988 1 10.05
CHEMBL373742 VASOPRESSIN 4.0 1 10.00
CHEMBL4467042 1 9.82
CHEMBL3354579 1 9.57
CHEMBL3301668 CARBETOCIN 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL395429 OXYTOCIN EC50 = 0.01 nM 11.00
CHEMBL3354594 EC50 = 0.025 nM 10.60
CHEMBL4474284 EC50 = 0.028 nM 10.55
CHEMBL4583231 EC50 = 0.031 nM 10.51
CHEMBL4458988 EC50 = 0.089 nM 10.05
CHEMBL373742 VASOPRESSIN EC50 = 0.1 nM 10.00
CHEMBL4467042 EC50 = 0.15 nM 9.82
CHEMBL3354579 EC50 = 0.27 nM 9.57
CHEMBL3301668 CARBETOCIN EC50 = 0.01 nM -