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Assay Detail

CHEMBL4397503

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Binding
Agonist activity at recombinant human V1B receptor expressed in HEK293 cells measured after 5 hrs by luciferase reporter gene assay
ChEMBL ↗
43
Total Activities
43
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

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 43 6.79 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1429 DESMOPRESSIN 4.0 1 7.96
CHEMBL435323 — — 1 7.62
CHEMBL4536454 — — 1 7.40
CHEMBL4557473 — — 1 7.34
CHEMBL4454891 — — 1 7.24
CHEMBL4474518 — — 1 7.19
CHEMBL4472007 — — 1 7.02
CHEMBL4439313 — — 1 7.00
CHEMBL4574065 — — 1 6.96
CHEMBL4468523 — — 1 6.96
CHEMBL4459424 — — 1 6.92
CHEMBL4455496 — — 1 6.92
CHEMBL4571464 — — 1 6.89
CHEMBL4462743 — — 1 6.85
CHEMBL4438723 — — 1 6.85
CHEMBL4544907 — — 1 6.85
CHEMBL4462616 — — 1 6.82
CHEMBL4555263 — — 1 6.82
CHEMBL4539100 — — 1 6.82
CHEMBL4533159 — — 1 6.80
CHEMBL4546884 — — 1 6.77
CHEMBL4454160 — — 1 6.75
CHEMBL4543908 — — 1 6.72
CHEMBL4521807 — — 1 6.68
CHEMBL4435502 — — 1 6.66
CHEMBL4445168 — — 1 6.60
CHEMBL4579754 — — 1 6.58
CHEMBL4473843 — — 1 6.50
CHEMBL4531053 — — 1 6.48
CHEMBL4451692 — — 1 6.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1429 DESMOPRESSIN EC50 = 11.0 nM 7.96
CHEMBL435323 — EC50 = 24.0 nM 7.62
CHEMBL4536454 — EC50 = 40.0 nM 7.40
CHEMBL4557473 — EC50 = 46.0 nM 7.34
CHEMBL4454891 — EC50 = 58.0 nM 7.24
CHEMBL4474518 — EC50 = 64.0 nM 7.19
CHEMBL4472007 — EC50 = 96.0 nM 7.02
CHEMBL4439313 — EC50 = 100.0 nM 7.00
CHEMBL4574065 — EC50 = 110.0 nM 6.96
CHEMBL4468523 — EC50 = 110.0 nM 6.96
CHEMBL4459424 — EC50 = 120.0 nM 6.92
CHEMBL4455496 — EC50 = 120.0 nM 6.92
CHEMBL4571464 — EC50 = 130.0 nM 6.89
CHEMBL4544907 — EC50 = 140.0 nM 6.85
CHEMBL4438723 — EC50 = 140.0 nM 6.85
CHEMBL4462743 — EC50 = 140.0 nM 6.85
CHEMBL4462616 — EC50 = 150.0 nM 6.82
CHEMBL4555263 — EC50 = 150.0 nM 6.82
CHEMBL4539100 — EC50 = 150.0 nM 6.82
CHEMBL4533159 — EC50 = 160.0 nM 6.80
CHEMBL4546884 — EC50 = 170.0 nM 6.77
CHEMBL4454160 — EC50 = 180.0 nM 6.75
CHEMBL4543908 — EC50 = 190.0 nM 6.72
CHEMBL4521807 — EC50 = 210.0 nM 6.68
CHEMBL4435502 — EC50 = 220.0 nM 6.66
CHEMBL4445168 — EC50 = 250.0 nM 6.60
CHEMBL4579754 — EC50 = 260.0 nM 6.58
CHEMBL4473843 — EC50 = 320.0 nM 6.50
CHEMBL4531053 — EC50 = 330.0 nM 6.48
CHEMBL4451692 — EC50 = 350.0 nM 6.46
CHEMBL4532363 — EC50 = 380.0 nM 6.42
CHEMBL4531173 — EC50 = 480.0 nM 6.32
CHEMBL4451555 — EC50 = 480.0 nM 6.32
CHEMBL4539370 — EC50 = 530.0 nM 6.28
CHEMBL4528032 — EC50 = 520.0 nM 6.28
CHEMBL4436571 — EC50 = 580.0 nM 6.24
CHEMBL4552500 — EC50 = 810.0 nM 6.09
CHEMBL4557118 — EC50 > 10000.0 nM -
CHEMBL4446853 — EC50 > 10000.0 nM -
CHEMBL4521602 — EC50 > 10000.0 nM -
CHEMBL4444891 — EC50 > 10000.0 nM -
CHEMBL4527761 — EC50 > 10000.0 nM -
CHEMBL4513567 — EC50 > 10000.0 nM -