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Assay Detail

CHEMBL617499

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

Binding
The compound was tested for the binding affinity against 5-hydroxytryptamine 2C receptor using [3H]Mesulergine as radioligand.
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 2C (CHEMBL324)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Pyrroloquinoxaline derivatives as high-affinity and selective 5-HT(3) receptor agonists: synthesis, further structure-activity relationships, and biological studies.
Campiani G, Morelli E, Gemma S, Nacci V, Butini S, Hamon M, Novellino E, Greco G, Cagnotto A, Goegan M, Cervo L, Dalla Valle F, Fracasso C, Caccia S, Mennini T.
J Med Chem (1999) 42 : 4362 -4379
PubMed 10543880 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.90 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL12314 MESULERGINE 2.0 1 8.80
CHEMBL39 SEROTONIN 3.0 1 7.50
CHEMBL18772 QUIPAZINE 2.0 1 6.50
CHEMBL342690 1 6.00
CHEMBL136108 1 5.70
CHEMBL136978 1 -
CHEMBL337101 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL12314 MESULERGINE Ki = 1.585 nM 8.80
CHEMBL39 SEROTONIN Ki = 31.62 nM 7.50
CHEMBL18772 QUIPAZINE Ki = 316.23 nM 6.50
CHEMBL342690 Ki = 1000.0 nM 6.00
CHEMBL136108 Ki = 1995.26 nM 5.70
CHEMBL136978 Ki < 10000.0 nM -
CHEMBL337101 Ki < 10000.0 nM -