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Assay Detail

CHEMBL3366922

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Binding
Agonist activity at human vasopressin V1b expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL ↗
67
Total Activities
67
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Vasopressin V1b receptor (CHEMBL1921) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

New, potent, and selective peptidic oxytocin receptor agonists.
Wiśniewski K, Alagarsamy S, Galyean R, Tariga H, Thompson D, Ly B, Wiśniewska H, Qi S, Croston G, Laporte R, Rivière PJ, Schteingart CD.
J Med Chem (2014) 57 : 5306 -5317
PubMed 24874785 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 67 6.39 8.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL373742 VASOPRESSIN 4.0 1 8.37
CHEMBL1429 DESMOPRESSIN 4.0 1 7.96
CHEMBL3354591 — — 1 7.08
CHEMBL3354592 — — 1 7.06
CHEMBL3354595 — — 1 7.04
CHEMBL3354588 — — 1 7.00
CHEMBL3354589 — — 1 7.00
CHEMBL3353946 — — 1 6.96
CHEMBL3353948 — — 1 6.85
CHEMBL3354598 — — 1 6.80
CHEMBL439044 — — 1 6.75
CHEMBL3354594 — — 1 6.75
CHEMBL3354601 — — 1 6.72
CHEMBL3353947 — — 1 6.70
CHEMBL3353956 — — 1 6.62
CHEMBL395429 OXYTOCIN 4.0 1 6.62
CHEMBL3353944 — — 1 6.58
CHEMBL3353945 — — 1 6.54
CHEMBL3353938 — — 1 6.43
CHEMBL3354600 — — 1 6.38
CHEMBL3353949 — — 1 6.36
CHEMBL3354590 — — 1 6.36
CHEMBL3354582 — — 1 6.35
CHEMBL3354597 — — 1 6.35
CHEMBL3353940 — — 1 6.33
CHEMBL3353932 — — 1 6.30
CHEMBL3354585 — — 1 6.30
CHEMBL3353953 — — 1 6.23
CHEMBL3354571 — — 1 6.22
CHEMBL3354593 — — 1 6.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL373742 VASOPRESSIN EC50 = 4.3 nM 8.37
CHEMBL1429 DESMOPRESSIN EC50 = 11.0 nM 7.96
CHEMBL3354591 — EC50 = 84.0 nM 7.08
CHEMBL3354592 — EC50 = 87.0 nM 7.06
CHEMBL3354595 — EC50 = 91.0 nM 7.04
CHEMBL3354588 — EC50 = 100.0 nM 7.00
CHEMBL3354589 — EC50 = 100.0 nM 7.00
CHEMBL3353946 — EC50 = 110.0 nM 6.96
CHEMBL3353948 — EC50 = 140.0 nM 6.85
CHEMBL3354598 — EC50 = 160.0 nM 6.80
CHEMBL439044 — EC50 = 180.0 nM 6.75
CHEMBL3354594 — EC50 = 180.0 nM 6.75
CHEMBL3354601 — EC50 = 190.0 nM 6.72
CHEMBL3353947 — EC50 = 200.0 nM 6.70
CHEMBL395429 OXYTOCIN EC50 = 240.0 nM 6.62
CHEMBL3353956 — EC50 = 240.0 nM 6.62
CHEMBL3353944 — EC50 = 260.0 nM 6.58
CHEMBL3353945 — EC50 = 290.0 nM 6.54
CHEMBL3353938 — EC50 = 370.0 nM 6.43
CHEMBL3354600 — EC50 = 420.0 nM 6.38
CHEMBL3353949 — EC50 = 440.0 nM 6.36
CHEMBL3354590 — EC50 = 440.0 nM 6.36
CHEMBL3354582 — EC50 = 450.0 nM 6.35
CHEMBL3354597 — EC50 = 450.0 nM 6.35
CHEMBL3353940 — EC50 = 470.0 nM 6.33
CHEMBL3353932 — EC50 = 500.0 nM 6.30
CHEMBL3354585 — EC50 = 500.0 nM 6.30
CHEMBL3353953 — EC50 = 590.0 nM 6.23
CHEMBL3354571 — EC50 = 600.0 nM 6.22
CHEMBL3354593 — EC50 = 620.0 nM 6.21
CHEMBL3353930 — EC50 = 660.0 nM 6.18
CHEMBL3353929 — EC50 = 700.0 nM 6.16
CHEMBL3353955 — EC50 = 720.0 nM 6.14
CHEMBL3354596 — EC50 = 750.0 nM 6.12
CHEMBL3353954 — EC50 = 770.0 nM 6.11
CHEMBL3354581 — EC50 = 820.0 nM 6.09
CHEMBL3354576 — EC50 = 830.0 nM 6.08
CHEMBL3354602 — EC50 = 850.0 nM 6.07
CHEMBL3354570 — EC50 = 930.0 nM 6.03
CHEMBL3353939 — EC50 = 980.0 nM 6.01
CHEMBL3354587 — EC50 = 1000.0 nM 6.00
CHEMBL3353931 — EC50 = 1000.0 nM 6.00
CHEMBL3353935 — EC50 = 1100.0 nM 5.96
CHEMBL3353951 — EC50 = 1300.0 nM 5.89
CHEMBL3354599 — EC50 = 1500.0 nM 5.82
CHEMBL3353950 — EC50 = 1800.0 nM 5.75
CHEMBL3353952 — EC50 = 2600.0 nM 5.58
CHEMBL3353942 — EC50 = 2800.0 nM 5.55
CHEMBL3354575 — EC50 = 3200.0 nM 5.50
CHEMBL3354586 — EC50 = 3600.0 nM 5.44