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Assay Detail

CHEMBL4015769

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

Binding
Displacement of [125I] phenylacetyl-D-Tyr(Me)-Phe-Gln-Asn-Arg-Pro-Arg-Tyr-NH2 from human recombinant vasopressin V1a receptor expressed in HEK293 after 2 hrs by liquid scintillation counting method
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Vasopressin V1a receptor (CHEMBL1889)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Tolvaptan-Type Vasopressin Receptor Ligands: Important Role of Axial Chirality in the Active Form.
Tabata H, Yoneda T, Oshitari T, Takahashi H, Natsugari H.
J Med Chem (2017) 60 : 4503 -4509
PubMed 28475329 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 8.40 8.99

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4075127 1 8.99
CHEMBL118271 1 8.80
CHEMBL4104877 1 8.73
CHEMBL4094707 1 8.69
CHEMBL4064556 1 8.55
CHEMBL4086079 1 8.33
CHEMBL4102459 1 8.20
CHEMBL4076436 1 8.17
CHEMBL4078185 1 7.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4075127 Ki = 1.03 nM 8.99
CHEMBL118271 Ki = 1.58 nM 8.80
CHEMBL4104877 Ki = 1.85 nM 8.73
CHEMBL4094707 Ki = 2.06 nM 8.69
CHEMBL4064556 Ki = 2.84 nM 8.55
CHEMBL4086079 Ki = 4.68 nM 8.33
CHEMBL4102459 Ki = 6.26 nM 8.20
CHEMBL4076436 Ki = 6.75 nM 8.17
CHEMBL4078185 Ki = 78.0 nM 7.11