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Assay Detail

CHEMBL907381

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

Binding
Displacement of [3H]AVP from vasopressin V1a receptor in rat liver membrane
23
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Liver
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Expert

Target

Vasopressin V1a receptor (CHEMBL2868)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8.
Pena A, Murat B, Trueba M, Ventura MA, Wo NC, Szeto HH, Cheng LL, Stoev S, Guillon G, Manning M.
J Med Chem (2007) 50 : 835 -847
PubMed 17300166 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 6.39 8.81

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL373742 VASOPRESSIN 4.0 1 8.81
CHEMBL1429 DESMOPRESSIN 4.0 2 7.97
CHEMBL375324 1 7.89
CHEMBL385739 1 7.60
CHEMBL221436 1 7.22
CHEMBL385068 1 7.17
CHEMBL375325 1 6.89
CHEMBL435323 1 6.50
CHEMBL414074 1 6.35
CHEMBL375096 1 6.05
CHEMBL412973 1 6.00
CHEMBL265859 1 5.90
CHEMBL219272 1 5.89
CHEMBL375188 1 5.85
CHEMBL375187 1 5.75
CHEMBL265858 1 5.64
CHEMBL375323 1 5.55
CHEMBL263090 1 5.54
CHEMBL373968 1 5.48
CHEMBL412972 1 5.42
CHEMBL412742 1 5.36
CHEMBL221485 1 5.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL373742 VASOPRESSIN Ki = 1.54 nM 8.81
CHEMBL1429 DESMOPRESSIN Ki = 10.8 nM 7.97
CHEMBL375324 Ki = 12.9 nM 7.89
CHEMBL385739 Ki = 25.0 nM 7.60
CHEMBL221436 Ki = 60.0 nM 7.22
CHEMBL385068 Ki = 67.0 nM 7.17
CHEMBL1429 DESMOPRESSIN Ki = 100.0 nM 7.00
CHEMBL375325 Ki = 130.0 nM 6.89
CHEMBL435323 Ki = 316.0 nM 6.50
CHEMBL414074 Ki = 450.0 nM 6.35
CHEMBL375096 Ki = 900.0 nM 6.05
CHEMBL412973 Ki = 1000.0 nM 6.00
CHEMBL265859 Ki = 1252.0 nM 5.90
CHEMBL219272 Ki = 1300.0 nM 5.89
CHEMBL375188 Ki = 1400.0 nM 5.85
CHEMBL375187 Ki = 1800.0 nM 5.75
CHEMBL265858 Ki = 2300.0 nM 5.64
CHEMBL375323 Ki = 2800.0 nM 5.55
CHEMBL263090 Ki = 2900.0 nM 5.54
CHEMBL373968 Ki = 3300.0 nM 5.48
CHEMBL412972 Ki = 3800.0 nM 5.42
CHEMBL412742 Ki = 4400.0 nM 5.36
CHEMBL221485 Ki = 9100.0 nM 5.04