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Assay Detail

CHEMBL818586

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

Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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 22 7.78 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL93603 1 8.70
CHEMBL432043 1 8.70
CHEMBL329026 1 8.52
CHEMBL543854 1 8.40
CHEMBL314290 1 8.30
CHEMBL327242 1 8.22
CHEMBL330016 1 7.96
CHEMBL94133 1 7.92
CHEMBL328079 1 7.92
CHEMBL329903 1 7.82
CHEMBL93861 1 7.80
CHEMBL539285 1 7.77
CHEMBL330094 1 7.70
CHEMBL327365 1 7.70
CHEMBL93366 1 7.64
CHEMBL49429 LIXIVAPTAN 3.0 1 7.64
CHEMBL96255 1 7.40
CHEMBL96731 1 7.40
CHEMBL329141 1 7.16
CHEMBL421180 1 7.16
CHEMBL2093899 1 6.77
CHEMBL330494 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL93603 Ki = 2.0 nM 8.70
CHEMBL432043 Ki = 2.0 nM 8.70
CHEMBL329026 Ki = 3.0 nM 8.52
CHEMBL543854 Ki = 4.0 nM 8.40
CHEMBL314290 Ki = 5.0 nM 8.30
CHEMBL327242 Ki = 6.0 nM 8.22
CHEMBL330016 Ki = 11.0 nM 7.96
CHEMBL94133 Ki = 12.0 nM 7.92
CHEMBL328079 Ki = 12.0 nM 7.92
CHEMBL329903 Ki = 15.0 nM 7.82
CHEMBL93861 Ki = 16.0 nM 7.80
CHEMBL539285 Ki = 17.0 nM 7.77
CHEMBL330094 Ki = 20.0 nM 7.70
CHEMBL327365 Ki = 20.0 nM 7.70
CHEMBL93366 Ki = 23.0 nM 7.64
CHEMBL49429 LIXIVAPTAN Ki = 23.0 nM 7.64
CHEMBL96255 Ki = 40.0 nM 7.40
CHEMBL96731 Ki = 40.0 nM 7.40
CHEMBL329141 Ki = 70.0 nM 7.16
CHEMBL421180 Ki = 70.0 nM 7.16
CHEMBL2093899 Ki = 170.0 nM 6.77
CHEMBL330494 Ki = 300.0 nM 6.52