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Assay Detail

CHEMBL817081

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

Binding
In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2)
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type Fibroblast
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Vasopressin V2 receptor (CHEMBL1790)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

4,10-dihydro-5H-thieno[3,2-c][1]benzazepine derivatives and 9,10-dihydro-4H-thieno[2,3-c][1]benzazepine derivatives as orally active arginine vasopressin receptor antagonists.
Aranapakam V, Albright JD, Grosu GT, Chan PS, Coupet J, Saunders T, Ru X, Mazandarani H.
Bioorg Med Chem Lett (1999) 9 : 1733 -1736
PubMed 10406632 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.40 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL49322 1 9.15
CHEMBL49429 LIXIVAPTAN 3.0 1 8.92
CHEMBL48867 1 8.17
CHEMBL295014 1 8.05
CHEMBL297293 1 7.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL49322 IC50 = 0.7 nM 9.15
CHEMBL49429 LIXIVAPTAN IC50 = 1.2 nM 8.92
CHEMBL48867 IC50 = 6.8 nM 8.17
CHEMBL295014 IC50 = 9.0 nM 8.05
CHEMBL297293 IC50 = 19.0 nM 7.72