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Assay Detail

CHEMBL815212

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

Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Synthesis and structure-activity relationships of 5,6,7,8-tetrahydro-4H-thieno[3,2-b]azepine derivatives: novel arginine vasopressin antagonists.
Cho H, Murakami K, Nakanishi H, Fujisawa A, Isoshima H, Niwa M, Hayakawa K, Hase Y, Uchida I, Watanabe H, Wakitani K, Aisaka K.
J Med Chem (2004) 47 : 101 -109
PubMed 14695824 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.70 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL368354 1 9.00
CHEMBL369832 1 8.70
CHEMBL413748 1 8.22
CHEMBL177885 1 8.10
CHEMBL367323 1 8.05
CHEMBL368818 1 8.00
CHEMBL175212 1 7.70
CHEMBL430083 1 7.70
CHEMBL368353 1 7.52
CHEMBL177285 1 7.30
CHEMBL175182 1 7.22
CHEMBL177248 1 7.10
CHEMBL435331 1 7.10
CHEMBL366790 1 7.10
CHEMBL176146 1 6.70
CHEMBL369150 1 -
CHEMBL366816 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL368354 IC50 = 1.0 nM 9.00
CHEMBL369832 IC50 = 2.0 nM 8.70
CHEMBL413748 IC50 = 6.0 nM 8.22
CHEMBL177885 IC50 = 8.0 nM 8.10
CHEMBL367323 IC50 = 9.0 nM 8.05
CHEMBL368818 IC50 = 10.0 nM 8.00
CHEMBL175212 IC50 = 20.0 nM 7.70
CHEMBL430083 IC50 = 20.0 nM 7.70
CHEMBL368353 IC50 = 30.0 nM 7.52
CHEMBL177285 IC50 = 50.0 nM 7.30
CHEMBL175182 IC50 = 60.0 nM 7.22
CHEMBL177248 IC50 = 80.0 nM 7.10
CHEMBL435331 IC50 = 80.0 nM 7.10
CHEMBL366790 IC50 = 80.0 nM 7.10
CHEMBL176146 IC50 = 200.0 nM 6.70
CHEMBL369150 IC50 < 10.0 nM -
CHEMBL366816 IC50 > 10000.0 nM -