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Assay Detail

CHEMBL2026265

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

Binding
Displacement of [3H]ketanserin from human recombinant 5HT2A receptor expressed in CHO cells after 60 mins by liquid scintillation counting
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 2A (CHEMBL224)
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 13 7.08 8.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1113 AMOXAPINE 4.0 1 8.75
CHEMBL831 LOXAPINE 4.0 1 8.62
CHEMBL42 CLOZAPINE 4.0 1 8.31
CHEMBL2022273 1 7.04
CHEMBL716 QUETIAPINE 4.0 1 7.00
CHEMBL2022269 1 6.88
CHEMBL2022272 1 6.75
CHEMBL2022280 1 6.69
CHEMBL2022277 1 6.55
CHEMBL2022276 1 6.45
CHEMBL2022279 1 6.00
CHEMBL2022271 1 5.96
CHEMBL2022278 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1113 AMOXAPINE Ki = 1.77 nM 8.75
CHEMBL831 LOXAPINE Ki = 2.42 nM 8.62
CHEMBL42 CLOZAPINE Ki = 4.84 nM 8.31
CHEMBL2022273 Ki = 92.0 nM 7.04
CHEMBL716 QUETIAPINE Ki = 101.0 nM 7.00
CHEMBL2022269 Ki = 131.0 nM 6.88
CHEMBL2022272 Ki = 180.0 nM 6.75
CHEMBL2022280 Ki = 204.0 nM 6.69
CHEMBL2022277 Ki = 284.0 nM 6.55
CHEMBL2022276 Ki = 352.0 nM 6.45
CHEMBL2022279 Ki = 994.0 nM 6.00
CHEMBL2022271 Ki = 1106.0 nM 5.96
CHEMBL2022278 Ki > 1000.0 nM -