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Assay Detail

CHEMBL907378

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Functional
Activity at OT receptor assessed as oxytocic activity in absence of magnesium
27
Total Activities
26
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Oxytocin receptor (CHEMBL2049)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8.
Pena A, Murat B, Trueba M, Ventura MA, Wo NC, Szeto HH, Cheng LL, Stoev S, Guillon G, Manning M.
J Med Chem (2007) 50 : 835 -847
PubMed 17300166 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Activity 22 - -
Kd 5 6.43 6.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL263090 1 6.55
CHEMBL221485 1 6.48
CHEMBL412742 1 6.35
CHEMBL375187 1 6.32
CHEMBL373742 VASOPRESSIN 4.0 1 -
CHEMBL265858 1 -
CHEMBL414074 1 -
CHEMBL435323 1 -
CHEMBL221436 1 -
CHEMBL1429 DESMOPRESSIN 4.0 2 -
CHEMBL439318 1 -
CHEMBL539417 1 -
CHEMBL376908 1 -
CHEMBL221847 1 -
CHEMBL265859 1 -
CHEMBL385068 1 -
CHEMBL385739 1 -
CHEMBL375324 1 -
CHEMBL219272 1 -
CHEMBL375323 1 -
CHEMBL375096 1 -
CHEMBL373968 1 -
CHEMBL412973 1 -
CHEMBL412972 1 -
CHEMBL375188 1 -
CHEMBL375325 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL263090 Kd = 281.84 nM 6.55
CHEMBL221485 Kd = 331.13 nM 6.48
CHEMBL412742 Kd = 446.68 nM 6.35
CHEMBL375187 Kd = 478.63 nM 6.32
CHEMBL373742 VASOPRESSIN Activity = 13.9 U/mg -
CHEMBL265858 Activity - -
CHEMBL414074 Activity - -
CHEMBL435323 Activity = 8.0 U/mg -
CHEMBL221436 Activity = 26.0 U/mg -
CHEMBL1429 DESMOPRESSIN Activity = 1.5 U/mg -
CHEMBL439318 Activity = 0.9 U/mg -
CHEMBL539417 Activity = 25.0 U/mg -
CHEMBL376908 Activity = 15.0 U/mg -
CHEMBL221847 Activity = 12.0 U/mg -
CHEMBL1429 DESMOPRESSIN Activity = 63.0 U/mg -
CHEMBL265859 Activity = 0.67 U/mg -
CHEMBL385739 Activity = 0.14 U/mg -
CHEMBL375325 Activity = 0.15 U/mg -
CHEMBL375324 Activity = 0.027 U/mg -
CHEMBL219272 Activity = 2.8 U/mg -
CHEMBL375323 Activity = 3.1 U/mg -
CHEMBL375096 Activity = 6.49 U/mg -
CHEMBL373968 Activity = 0.046 U/mg -
CHEMBL412973 Activity = 0.27 U/mg -
CHEMBL412972 Activity = 0.054 U/mg -
CHEMBL375188 Kd >= 12882.5 nM -
CHEMBL385068 Activity = 0.06 U/mg -