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Assay Detail

CHEMBL616836

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

Binding
Tested for binding affinity against 5-hydroxytryptamine 1C receptor from rat frontal cortical regions using [3H]mesulergine as radioligand
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Antagonism of 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane stimulus with a newly identified 5-HT2- versus 5-HT1C-selective antagonist.
Ismaiel AM, De Los Angeles J, Teitler M, Ingher S, Glennon RA.
J Med Chem (1993) 36 : 2519 -2525
PubMed 8355253 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 5.72 6.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL86072 1 6.47
CHEMBL316004 LENPERONE 2.0 1 6.46
CHEMBL267930 SPIPERONE 2.0 1 6.00
CHEMBL82688 1 5.78
CHEMBL314430 1 5.64
CHEMBL315522 1 5.54
CHEMBL84542 1 5.50
CHEMBL83867 1 5.48
CHEMBL85507 1 5.44
CHEMBL79834 SPIRAMIDE 2.0 1 5.37
CHEMBL84079 1 5.22
CHEMBL85954 1 -
CHEMBL309484 1 -
CHEMBL82567 1 -
CHEMBL314702 1 -
CHEMBL82565 1 -
CHEMBL85392 1 -
CHEMBL82436 1 -
CHEMBL82519 PRIMAPERONE 2.0 1 -
CHEMBL81959 1 -
CHEMBL309711 1 -
CHEMBL313337 1 -
CHEMBL419848 1 -
CHEMBL309992 1 -
CHEMBL85508 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL86072 Ki = 335.0 nM 6.47
CHEMBL316004 LENPERONE Ki = 345.0 nM 6.46
CHEMBL267930 SPIPERONE Ki = 1000.0 nM 6.00
CHEMBL82688 Ki = 1650.0 nM 5.78
CHEMBL314430 Ki = 2300.0 nM 5.64
CHEMBL315522 Ki = 2870.0 nM 5.54
CHEMBL84542 Ki = 3200.0 nM 5.50
CHEMBL83867 Ki = 3300.0 nM 5.48
CHEMBL85507 Ki = 3600.0 nM 5.44
CHEMBL79834 SPIRAMIDE Ki = 4300.0 nM 5.37
CHEMBL84079 Ki = 6000.0 nM 5.22
CHEMBL85954 Ki > 10000.0 nM -
CHEMBL309484 Ki > 10000.0 nM -
CHEMBL82567 Ki > 100000.0 nM -
CHEMBL314702 Ki > 10000.0 nM -
CHEMBL82565 Ki > 10000.0 nM -
CHEMBL85392 Ki > 10000.0 nM -
CHEMBL82436 Ki > 10000.0 nM -
CHEMBL82519 PRIMAPERONE Ki > 10000.0 nM -
CHEMBL81959 Ki > 10000.0 nM -
CHEMBL309711 Ki > 10000.0 nM -
CHEMBL313337 Ki > 10000.0 nM -
CHEMBL419848 Ki > 10000.0 nM -
CHEMBL309992 Ki > 10000.0 nM -
CHEMBL85508 Ki > 10000.0 nM -