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Assay Detail

CHEMBL617927

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Binding
The binding affinity at 5-hydroxytryptamine 2A receptor was determined using [3H]ketanserin
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 2A (CHEMBL322)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and pharmacological testing of 1,2,3,4,10,14b-hexahydro-6-methoxy-2-methyldibenzo[c,f]pyrazino[1,2-a]azepin and its enantiomers in comparison with the two antidepressants mianserin and mirtazapine.
Wikström HV, Mensonides-Harsema MM, Cremers TI, Moltzen EK, Arnt J.
J Med Chem (2002) 45 : 3280 -3285
PubMed 12109911 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 8.50 9.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL111184 1 9.26
CHEMBL324270 1 9.15
CHEMBL113238 1 9.12
CHEMBL6437 MIANSERIN 4.0 1 8.82
CHEMBL654 MIRTAZAPINE 4.0 1 8.70
CHEMBL334270 1 7.92
CHEMBL109877 1 6.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL111184 Ki = 0.55 nM 9.26
CHEMBL324270 Ki = 0.7 nM 9.15
CHEMBL113238 Ki = 0.75 nM 9.12
CHEMBL6437 MIANSERIN Ki = 1.5 nM 8.82
CHEMBL654 MIRTAZAPINE Ki = 2.0 nM 8.70
CHEMBL334270 Ki = 12.0 nM 7.92
CHEMBL109877 Ki = 277.0 nM 6.56