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Assay Detail

CHEMBL817841

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

Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel design of nonpeptide AVP V(2) receptor agonists: structural requirements for an agonist having 1-(4-aminobenzoyl)-2,3,4, 5-tetrahydro-1H-1-benzazepine as a template.
Kondo K, Ogawa H, Shinohara T, Kurimura M, Tanada Y, Kan K, Yamashita H, Nakamura S, Hirano T, Yamamura Y, Mori T, Tominaga M, Itai A.
J Med Chem (2000) 43 : 4388 -4397
PubMed 11087564 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 7.55 8.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL334376 1 8.39
CHEMBL343945 1 8.30
CHEMBL136644 1 8.23
CHEMBL342250 1 8.12
CHEMBL139863 1 8.06
CHEMBL340893 1 8.05
CHEMBL136109 1 7.89
CHEMBL335592 1 7.89
CHEMBL136628 1 7.80
CHEMBL136177 1 7.75
CHEMBL343935 1 7.75
CHEMBL334688 1 7.72
CHEMBL139415 1 7.66
CHEMBL137500 1 7.51
CHEMBL134525 1 7.47
CHEMBL337098 1 7.46
CHEMBL136790 1 7.29
CHEMBL136065 1 6.92
CHEMBL344848 1 6.75
CHEMBL335040 1 6.68
CHEMBL342251 1 6.50
CHEMBL343538 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL334376 IC50 = 4.1 nM 8.39
CHEMBL343945 IC50 = 5.0 nM 8.30
CHEMBL136644 IC50 = 5.9 nM 8.23
CHEMBL342250 IC50 = 7.5 nM 8.12
CHEMBL139863 IC50 = 8.8 nM 8.06
CHEMBL340893 IC50 = 9.0 nM 8.05
CHEMBL136109 IC50 = 13.0 nM 7.89
CHEMBL335592 IC50 = 13.0 nM 7.89
CHEMBL136628 IC50 = 16.0 nM 7.80
CHEMBL136177 IC50 = 18.0 nM 7.75
CHEMBL343935 IC50 = 18.0 nM 7.75
CHEMBL334688 IC50 = 19.0 nM 7.72
CHEMBL139415 IC50 = 22.0 nM 7.66
CHEMBL137500 IC50 = 31.0 nM 7.51
CHEMBL134525 IC50 = 34.0 nM 7.47
CHEMBL337098 IC50 = 35.0 nM 7.46
CHEMBL136790 IC50 = 51.0 nM 7.29
CHEMBL136065 IC50 = 120.0 nM 6.92
CHEMBL344848 IC50 = 180.0 nM 6.75
CHEMBL335040 IC50 = 210.0 nM 6.68
CHEMBL342251 IC50 = 320.0 nM 6.50
CHEMBL343538 IC50 = 1000.0 nM 6.00