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Assay Detail

CHEMBL818587

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

Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
32
Total Activities
32
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 (CHEMBL1790)
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 32 8.16 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL543854 1 9.05
CHEMBL327242 1 8.85
CHEMBL93603 1 8.72
CHEMBL49429 LIXIVAPTAN 3.0 1 8.64
CHEMBL329026 1 8.55
CHEMBL328079 1 8.55
CHEMBL328791 1 8.49
CHEMBL329903 1 8.49
CHEMBL432043 1 8.43
CHEMBL93861 1 8.43
CHEMBL330005 1 8.43
CHEMBL539285 1 8.43
CHEMBL330016 1 8.38
CHEMBL314290 1 8.38
CHEMBL327365 1 8.30
CHEMBL330094 1 8.30
CHEMBL93366 1 8.10
CHEMBL92470 1 8.05
CHEMBL93195 1 8.00
CHEMBL423868 1 8.00
CHEMBL93205 1 8.00
CHEMBL90657 1 7.96
CHEMBL94133 1 7.96
CHEMBL329141 1 7.89
CHEMBL2093899 1 7.82
CHEMBL93209 1 7.82
CHEMBL328227 1 7.77
CHEMBL92187 1 7.75
CHEMBL96731 1 7.60
CHEMBL421180 1 7.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL543854 Ki = 0.9 nM 9.05
CHEMBL327242 Ki = 1.4 nM 8.85
CHEMBL93603 Ki = 1.9 nM 8.72
CHEMBL49429 LIXIVAPTAN Ki = 2.3 nM 8.64
CHEMBL329026 Ki = 2.8 nM 8.55
CHEMBL328079 Ki = 2.8 nM 8.55
CHEMBL328791 Ki = 3.2 nM 8.49
CHEMBL329903 Ki = 3.2 nM 8.49
CHEMBL432043 Ki = 3.7 nM 8.43
CHEMBL93861 Ki = 3.7 nM 8.43
CHEMBL330005 Ki = 3.7 nM 8.43
CHEMBL539285 Ki = 3.7 nM 8.43
CHEMBL330016 Ki = 4.2 nM 8.38
CHEMBL314290 Ki = 4.2 nM 8.38
CHEMBL330094 Ki = 5.0 nM 8.30
CHEMBL327365 Ki = 5.0 nM 8.30
CHEMBL93366 Ki = 8.0 nM 8.10
CHEMBL92470 Ki = 9.0 nM 8.05
CHEMBL93195 Ki = 10.0 nM 8.00
CHEMBL423868 Ki = 10.0 nM 8.00
CHEMBL93205 Ki = 10.0 nM 8.00
CHEMBL90657 Ki = 11.0 nM 7.96
CHEMBL94133 Ki = 11.0 nM 7.96
CHEMBL329141 Ki = 13.0 nM 7.89
CHEMBL2093899 Ki = 15.0 nM 7.82
CHEMBL93209 Ki = 15.0 nM 7.82
CHEMBL328227 Ki = 17.0 nM 7.77
CHEMBL92187 Ki = 18.0 nM 7.75
CHEMBL96731 Ki = 25.0 nM 7.60
CHEMBL421180 Ki = 37.0 nM 7.43
CHEMBL330494 Ki = 60.0 nM 7.22
CHEMBL96255 Ki = 65.0 nM 7.19