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Assay Detail

CHEMBL2026264

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

Binding
Displacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation counting
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Alpha-2A adrenergic receptor (CHEMBL1867)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

New pyridobenzoxazepine derivatives derived from 5-(4-methylpiperazin-1-yl)-8-chloro-pyrido[2,3-b][1,5]benzoxazepine (JL13): chemical synthesis and pharmacological evaluation.
Liégeois JF, Deville M, Dilly S, Lamy C, Mangin F, Résimont M, Tarazi FI.
J Med Chem (2012) 55 : 1572 -1582
PubMed 22268448 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 6.46 6.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2022280 1 6.75
CHEMBL42 CLOZAPINE 4.0 1 6.73
CHEMBL2022272 1 6.43
CHEMBL2022273 1 6.38
CHEMBL2022275 1 6.34
CHEMBL2022269 1 6.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2022280 Ki = 180.0 nM 6.75
CHEMBL42 CLOZAPINE Ki = 185.0 nM 6.73
CHEMBL2022272 Ki = 374.0 nM 6.43
CHEMBL2022273 Ki = 412.0 nM 6.38
CHEMBL2022275 Ki = 452.0 nM 6.34
CHEMBL2022269 Ki = 729.0 nM 6.14