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Assay Detail

CHEMBL818808

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

Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Structure-activity study of novel tricyclic benzazepine arginine vasopressin antagonists.
Sum FW, Dusza J, Santos ED, Grosu G, Reich M, Du X, Albright JD, Chan P, Coupet J, Ru X, Mazandarani H, Saunders T.
Bioorg Med Chem Lett (2003) 13 : 2195 -2198
PubMed 12798333 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 7.48 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL68085 1 8.82
CHEMBL49429 LIXIVAPTAN 3.0 1 8.64
CHEMBL418890 1 8.52
CHEMBL70981 1 8.40
CHEMBL71797 1 8.40
CHEMBL306970 1 8.40
CHEMBL302709 1 8.30
CHEMBL71355 1 8.15
CHEMBL304956 1 7.89
CHEMBL304060 1 7.89
CHEMBL73286 1 7.85
CHEMBL68948 1 7.85
CHEMBL302955 1 7.82
CHEMBL71305 1 7.66
CHEMBL308741 1 7.60
CHEMBL72945 1 7.54
CHEMBL71282 1 7.54
CHEMBL303176 1 7.48
CHEMBL442743 1 7.46
CHEMBL70949 1 7.38
CHEMBL68033 1 7.18
CHEMBL307271 1 7.17
CHEMBL309096 1 7.11
CHEMBL72342 1 6.27
CHEMBL71712 1 6.07
CHEMBL303376 1 6.07
CHEMBL71283 1 5.77
CHEMBL71626 1 4.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL68085 IC50 = 1.5 nM 8.82
CHEMBL49429 LIXIVAPTAN IC50 = 2.3 nM 8.64
CHEMBL418890 IC50 = 3.0 nM 8.52
CHEMBL70981 IC50 = 4.0 nM 8.40
CHEMBL71797 IC50 = 4.0 nM 8.40
CHEMBL306970 IC50 = 4.0 nM 8.40
CHEMBL302709 IC50 = 5.0 nM 8.30
CHEMBL71355 IC50 = 7.0 nM 8.15
CHEMBL304956 IC50 = 13.0 nM 7.89
CHEMBL304060 IC50 = 13.0 nM 7.89
CHEMBL73286 IC50 = 14.0 nM 7.85
CHEMBL68948 IC50 = 14.0 nM 7.85
CHEMBL302955 IC50 = 15.0 nM 7.82
CHEMBL71305 IC50 = 22.0 nM 7.66
CHEMBL308741 IC50 = 25.0 nM 7.60
CHEMBL72945 IC50 = 29.0 nM 7.54
CHEMBL71282 IC50 = 29.0 nM 7.54
CHEMBL303176 IC50 = 33.0 nM 7.48
CHEMBL442743 IC50 = 35.0 nM 7.46
CHEMBL70949 IC50 = 42.0 nM 7.38
CHEMBL68033 IC50 = 66.0 nM 7.18
CHEMBL307271 IC50 = 68.0 nM 7.17
CHEMBL309096 IC50 = 77.0 nM 7.11
CHEMBL72342 IC50 = 540.0 nM 6.27
CHEMBL71712 IC50 = 860.0 nM 6.07
CHEMBL303376 IC50 = 860.0 nM 6.07
CHEMBL71283 IC50 = 1700.0 nM 5.77
CHEMBL71626 IC50 = 50000.0 nM 4.30