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Assay Detail

CHEMBL823112

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

Binding
Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.
7
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Canis lupus familiaris
Tissue Renal medulla
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

A minor modification of residue 1 in potent vasopressin antagonists dramatically reduces agonist activity.
Huffman WF, Albrightson-Winslow C, Brickson B, Bryan HG, Caldwell N, Dytko G, Eggleston DS, Kinter LB, Moore ML, Newlander KA.
J Med Chem (1989) 32 : 880 -884
PubMed 2522994 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 8.96 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2371605 1 9.30
CHEMBL2371604 1 9.15
CHEMBL3084974 1 9.00
CHEMBL262482 2 9.00
CHEMBL438014 1 9.00
CHEMBL384776 1 8.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2371605 Ki = 0.5 nM 9.30
CHEMBL2371604 Ki = 0.7 nM 9.15
CHEMBL3084974 Ki = 1.0 nM 9.00
CHEMBL262482 Ki = 0.99 nM 9.00
CHEMBL438014 Ki = 1.0 nM 9.00
CHEMBL384776 Ki = 1.1 nM 8.96
CHEMBL262482 Ki = 4.9 nM 8.31