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Assay Detail

CHEMBL819376

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

Binding
Inhibition of 1 nM AVP-induced calcium mobilisation in cells expressing human vasopressin V1a receptor
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Potent nonpeptide vasopressin receptor antagonists based on oxazino- and thiazinobenzodiazepine templates.
Matthews JM, Hoekstra WJ, Dyatkin AB, Hecker LR, Hlasta DJ, Poulter BL, Andrade-Gordon P, de Garavilla L, Demarest KT, Ericson E, Gunnet JW, Hageman W, Look R, Moore JB, Reynolds CH, Maryanoff BE.
Bioorg Med Chem Lett (2004) 14 : 2747 -2752
PubMed 15125926 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 5.45 6.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL543854 1 6.22
CHEMBL93603 1 6.16
CHEMBL96731 1 5.89
CHEMBL314290 1 5.89
CHEMBL329903 1 5.85
CHEMBL96255 1 5.85
CHEMBL327242 1 5.80
CHEMBL329026 1 5.72
CHEMBL329141 1 5.72
CHEMBL328079 1 5.70
CHEMBL432043 1 5.47
CHEMBL330016 1 5.38
CHEMBL49429 LIXIVAPTAN 3.0 1 5.22
CHEMBL94133 1 5.19
CHEMBL327365 1 5.10
CHEMBL330094 1 4.96
CHEMBL539285 1 4.85
CHEMBL330494 1 4.85
CHEMBL2093899 1 4.85
CHEMBL93366 1 4.85
CHEMBL421180 1 4.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL543854 Ki = 600.0 nM 6.22
CHEMBL93603 Ki = 700.0 nM 6.16
CHEMBL96731 Ki = 1300.0 nM 5.89
CHEMBL314290 Ki = 1300.0 nM 5.89
CHEMBL329903 Ki = 1400.0 nM 5.85
CHEMBL96255 Ki = 1400.0 nM 5.85
CHEMBL327242 Ki = 1600.0 nM 5.80
CHEMBL329026 Ki = 1900.0 nM 5.72
CHEMBL329141 Ki = 1900.0 nM 5.72
CHEMBL328079 Ki = 2000.0 nM 5.70
CHEMBL432043 Ki = 3400.0 nM 5.47
CHEMBL330016 Ki = 4200.0 nM 5.38
CHEMBL49429 LIXIVAPTAN Ki = 6000.0 nM 5.22
CHEMBL94133 Ki = 6400.0 nM 5.19
CHEMBL327365 Ki = 8000.0 nM 5.10
CHEMBL330094 Ki = 11000.0 nM 4.96
CHEMBL539285 Ki = 14000.0 nM 4.85
CHEMBL330494 Ki = 14000.0 nM 4.85
CHEMBL2093899 Ki = 14000.0 nM 4.85
CHEMBL93366 Ki = 14000.0 nM 4.85
CHEMBL421180 Ki = 14000.0 nM 4.85