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Assay Detail

CHEMBL1039597

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

Binding
Displacement of [3H]mesulergine from 5HT2C in Sprague-Dawley rat brain cortex by liquid scintillation counting
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

5-hydroxytryptamine receptor 2C (CHEMBL324)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Efficient microwave combinatorial synthesis of novel indolic arylpiperazine derivatives as serotoninergic ligands.
Frecentese F, Fiorino F, Perissutti E, Severino B, Magli E, Esposito A, De Angelis F, Massarelli P, Nencini C, Viti B, Santagada V, Caliendo G.
Eur J Med Chem (2010) 45 : 752 -759
PubMed 19954866 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.21 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL566533 1 8.89
CHEMBL12314 MESULERGINE 2.0 1 8.72
CHEMBL586050 1 7.40
CHEMBL583422 1 7.36
CHEMBL568284 1 7.35
CHEMBL565707 1 7.30
CHEMBL567649 1 6.98
CHEMBL565484 1 6.61
CHEMBL584919 1 6.51
CHEMBL568285 1 5.00
CHEMBL566331 1 -
CHEMBL567834 1 -
CHEMBL567648 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL566533 Ki = 1.28 nM 8.89
CHEMBL12314 MESULERGINE Ki = 1.9 nM 8.72
CHEMBL586050 Ki = 39.7 nM 7.40
CHEMBL583422 Ki = 43.6 nM 7.36
CHEMBL568284 Ki = 45.1 nM 7.35
CHEMBL565707 Ki = 50.4 nM 7.30
CHEMBL567649 Ki = 104.0 nM 6.98
CHEMBL565484 Ki = 247.0 nM 6.61
CHEMBL584919 Ki = 309.0 nM 6.51
CHEMBL568285 Ki = 10000.0 nM 5.00
CHEMBL566331 Ki - -
CHEMBL567834 Ki - -
CHEMBL567648 Ki - -