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Assay Detail

CHEMBL3816396

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Functional
Agonist activity at human oxytocin receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 90 sec by fluo-4 dye based FLIPR assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Oxytocin receptor (CHEMBL2049)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Systematic N-methylation of oxytocin: Impact on pharmacology and intramolecular hydrogen bonding network.
Sciabola S, Goetz GH, Bai G, Rogers BN, Gray DL, Duplantier A, Fonseca KR, Vanase-Frawley MA, Kablaoui NM.
Bioorg Med Chem (2016) 24 : 3513 -3520
PubMed 27297999 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 22 8.46 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL439044 1 10.40
CHEMBL395429 OXYTOCIN 4.0 1 10.40
CHEMBL3813771 1 9.54
CHEMBL3814633 1 9.33
CHEMBL3814744 1 9.28
CHEMBL3815099 1 9.23
CHEMBL3813894 1 9.00
CHEMBL3813707 1 8.62
CHEMBL3813883 1 8.37
CHEMBL3814395 1 8.32
CHEMBL3813722 1 8.26
CHEMBL3813729 1 8.16
CHEMBL3813982 1 8.10
CHEMBL3814120 1 7.97
CHEMBL3814126 1 7.83
CHEMBL3813858 1 7.81
CHEMBL3814165 1 7.62
CHEMBL3814617 1 7.58
CHEMBL3814232 1 6.76
CHEMBL3813879 1 6.55
CHEMBL3813714 1 -
CHEMBL3814904 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL439044 EC50 = 0.04 nM 10.40
CHEMBL395429 OXYTOCIN EC50 = 0.04 nM 10.40
CHEMBL3813771 EC50 = 0.29 nM 9.54
CHEMBL3814633 EC50 = 0.47 nM 9.33
CHEMBL3814744 EC50 = 0.52 nM 9.28
CHEMBL3815099 EC50 = 0.59 nM 9.23
CHEMBL3813894 EC50 = 0.99 nM 9.00
CHEMBL3813707 EC50 = 2.41 nM 8.62
CHEMBL3813883 EC50 = 4.23 nM 8.37
CHEMBL3814395 EC50 = 4.77 nM 8.32
CHEMBL3813722 EC50 = 5.52 nM 8.26
CHEMBL3813729 EC50 = 6.98 nM 8.16
CHEMBL3813982 EC50 = 7.98 nM 8.10
CHEMBL3814120 EC50 = 10.79 nM 7.97
CHEMBL3814126 EC50 = 14.74 nM 7.83
CHEMBL3813858 EC50 = 15.57 nM 7.81
CHEMBL3814165 EC50 = 23.93 nM 7.62
CHEMBL3814617 EC50 = 25.99 nM 7.58
CHEMBL3814232 EC50 = 174.86 nM 6.76
CHEMBL3813879 EC50 = 283.01 nM 6.55
CHEMBL3813714 EC50 > 1000.0 nM -
CHEMBL3814904 EC50 > 1000.0 nM -