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Assay Detail

CHEMBL1248770

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

Binding
Displacement of [3H]-WAY100635 from 5HT1A receptor in guinea pig brain cortex after 45 mins by liquid scintillation spectrometry
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Design and synthesis of novel tricyclic benzoxazines as potent 5-HT(1A/B/D) receptor antagonists leading to the discovery of 6-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-4H-imidazo[5,1-c][1,4]benzoxazine-3-carboxamide (GSK588045).
Bromidge SM, Arban R, Bertani B, Bison S, Borriello M, Cavanni P, Dal Forno G, Di-Fabio R, Donati D, Fontana S, Gianotti M, Gordon LJ, Granci E, Leslie CP, Moccia L, Pasquarello A, Sartori I, Sava A, Watson JM, Worby A, Zonzini L, Zucchelli V.
J Med Chem (2010) 53 : 5827 -5843
PubMed 20590088 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 10.24 10.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1241913 1 10.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1241913 Ki = 0.05754 nM 10.24