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Assay Detail

CHEMBL4141652

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

Binding
Displacement of [3H]-vasopressin from human vasopressin V1a receptor expressed in HEK293 cell membranes after 90 mins by radioligand binding assay
16
Total Activities
16
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 V1a receptor (CHEMBL1889)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Conformationally rigid derivatives of WAY-267,464: Synthesis and pharmacology at the human oxytocin and vasopressin-1a receptors.
Jorgensen WT, Gulliver DW, Katte TA, Werry EL, Reekie TA, Connor M, Kassiou M.
Eur J Med Chem (2018) 143 : 1644 -1656
PubMed 29126725 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 6.14 7.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3763342 1 7.57
CHEMBL3763951 1 7.21
CHEMBL3763823 1 7.19
CHEMBL3763174 1 6.71
CHEMBL4166008 1 6.60
CHEMBL4162565 1 6.19
CHEMBL4173250 1 6.10
CHEMBL4176616 1 6.06
CHEMBL4159182 1 5.97
CHEMBL4169435 1 5.75
CHEMBL4169830 1 5.72
CHEMBL4169825 1 5.71
CHEMBL4162568 1 5.68
CHEMBL4161507 1 5.48
CHEMBL4169437 1 5.20
CHEMBL4173255 1 5.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3763342 Ki = 27.0 nM 7.57
CHEMBL3763951 Ki = 62.0 nM 7.21
CHEMBL3763823 Ki = 64.1 nM 7.19
CHEMBL3763174 Ki = 194.7 nM 6.71
CHEMBL4166008 Ki = 250.7 nM 6.60
CHEMBL4162565 Ki = 642.8 nM 6.19
CHEMBL4173250 Ki = 795.1 nM 6.10
CHEMBL4176616 Ki = 874.1 nM 6.06
CHEMBL4159182 Ki = 1062.0 nM 5.97
CHEMBL4169435 Ki = 1756.0 nM 5.75
CHEMBL4169830 Ki = 1910.0 nM 5.72
CHEMBL4169825 Ki = 1938.0 nM 5.71
CHEMBL4162568 Ki = 2095.0 nM 5.68
CHEMBL4161507 Ki = 3343.0 nM 5.48
CHEMBL4169437 Ki = 6250.0 nM 5.20
CHEMBL4173255 Ki = 6807.0 nM 5.17