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Assay Detail

CHEMBL857223

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

Functional
pA2 value was determined for antidiuretic V2 antagonistic activity in vivo in anesthetized rats pA2 value was determined for antidiuretic V2 antagonistic activity in vivo in anesthetized rats
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Urine
Confidence 1 — Organism
Curated By Intermediate

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
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 12 7.48 7.98

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2373993 1 7.98
CHEMBL2373992 1 7.81
CHEMBL2370382 1 7.77
CHEMBL2370377 1 7.73
CHEMBL387273 1 7.69
CHEMBL263860 1 7.54
CHEMBL2373370 1 7.00
CHEMBL2373442 1 6.30
CHEMBL2370378 1 -
CHEMBL2373510 1 -
CHEMBL2373521 1 -
CHEMBL384727 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2373993 Kd = 10.47 nM 7.98
CHEMBL2373992 Kd = 15.49 nM 7.81
CHEMBL2370382 Kd = 16.98 nM 7.77
CHEMBL2370377 Kd = 18.62 nM 7.73
CHEMBL387273 Kd = 20.42 nM 7.69
CHEMBL263860 Kd = 28.84 nM 7.54
CHEMBL2373370 Kd = 100.0 nM 7.00
CHEMBL2373442 Kd = 501.19 nM 6.30
CHEMBL2370378 Kd ~ 12.59 nM -
CHEMBL2373510 Kd ~ 141.25 nM -
CHEMBL2373521 Kd > 316.23 nM -
CHEMBL384727 Kd ~ 316.23 nM -