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Assay Detail

CHEMBL815444

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

Binding
In vitro inhibition of [3H]- AVP binding to V1a receptor from human platelet membrane
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Vasopressin V1a receptor (CHEMBL1889)
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 4 7.38 8.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL49322 1 8.07
CHEMBL295014 1 7.44
CHEMBL297293 1 7.37
CHEMBL49429 LIXIVAPTAN 3.0 1 6.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL49322 IC50 = 8.5 nM 8.07
CHEMBL295014 IC50 = 36.0 nM 7.44
CHEMBL297293 IC50 = 43.0 nM 7.37
CHEMBL49429 LIXIVAPTAN IC50 = 230.0 nM 6.64