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Assay Detail

CHEMBL820876

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Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Vasopressin V2 receptor (CHEMBL3766)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design of potent and selective linear antagonists of vasopressor (V1-receptor) responses to vasopressin.
Manning M, Stoev S, Kolodziejczyk A, Klis WA, Kruszynski M, Misicka A, Olma A, Wo NC, Sawyer WH.
J Med Chem (1990) 33 : 3079 -3086
PubMed 2231609 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 14 7.35 8.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL408038 1 8.11
CHEMBL410838 1 7.99
CHEMBL267111 1 7.91
CHEMBL2370376 1 7.81
CHEMBL406184 1 7.81
CHEMBL2370381 1 7.70
CHEMBL2370380 1 7.66
CHEMBL2373516 1 7.36
CHEMBL411320 1 7.21
CHEMBL2373374 1 7.20
CHEMBL2373423 1 7.00
CHEMBL269251 1 6.60
CHEMBL2373441 1 5.20
CHEMBL2373502 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL408038 Kd = 7.762 nM 8.11
CHEMBL410838 Kd = 10.23 nM 7.99
CHEMBL267111 Kd = 12.3 nM 7.91
CHEMBL2370376 Kd = 15.49 nM 7.81
CHEMBL406184 Kd = 15.49 nM 7.81
CHEMBL2370381 Kd = 19.95 nM 7.70
CHEMBL2370380 Kd = 21.88 nM 7.66
CHEMBL2373516 Kd = 43.65 nM 7.36
CHEMBL411320 Kd = 61.66 nM 7.21
CHEMBL2373374 Kd = 63.1 nM 7.20
CHEMBL2373423 Kd = 100.0 nM 7.00
CHEMBL269251 Kd = 251.19 nM 6.60
CHEMBL2373441 Kd = 6309.57 nM 5.20
CHEMBL2373502 Kd ~ 58.88 nM -