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Assay Detail

CHEMBL616485

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

Binding
Binding affinity at 5-hydroxytryptamine 2 receptor from rat frontal cortex homogenates by [3H]-spiperone displacement.
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Frontal cortex
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Serotonin 2 (5-HT2) receptor (CHEMBL2093870)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Ergolines as selective 5-HT1 agonists.
Ward JS, Fuller RW, Merritt L, Snoddy HD, Paschal JW, Mason NR, Horng JS.
J Med Chem (1988) 31 : 1512 -1519
PubMed 2456389 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.20 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL291097 1 6.96
CHEMBL288111 1 6.96
CHEMBL40047 1 6.89
CHEMBL39604 1 6.85
CHEMBL39947 1 6.80
CHEMBL36379 1 6.68
CHEMBL449081 AGROCLAVINE 1 6.57
CHEMBL13866 1 6.36
CHEMBL290217 1 6.35
CHEMBL38058 1 5.90
CHEMBL291044 1 5.88
CHEMBL285284 1 5.79
CHEMBL37867 1 5.78
CHEMBL291218 1 5.73
CHEMBL285723 1 5.67
CHEMBL288480 1 5.58
CHEMBL36980 1 5.42
CHEMBL39769 1 5.38
CHEMBL291030 1 -
CHEMBL289517 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL291097 IC50 = 110.0 nM 6.96
CHEMBL288111 IC50 = 110.0 nM 6.96
CHEMBL40047 IC50 = 130.0 nM 6.89
CHEMBL39604 IC50 = 140.0 nM 6.85
CHEMBL39947 IC50 = 160.0 nM 6.80
CHEMBL36379 IC50 = 210.0 nM 6.68
CHEMBL449081 AGROCLAVINE IC50 = 270.0 nM 6.57
CHEMBL13866 IC50 = 440.0 nM 6.36
CHEMBL290217 IC50 = 450.0 nM 6.35
CHEMBL38058 IC50 = 1250.0 nM 5.90
CHEMBL291044 IC50 = 1330.0 nM 5.88
CHEMBL285284 IC50 = 1620.0 nM 5.79
CHEMBL37867 IC50 = 1665.0 nM 5.78
CHEMBL291218 IC50 = 1850.0 nM 5.73
CHEMBL285723 IC50 = 2120.0 nM 5.67
CHEMBL288480 IC50 = 2650.0 nM 5.58
CHEMBL36980 IC50 = 3820.0 nM 5.42
CHEMBL39769 IC50 = 4220.0 nM 5.38
CHEMBL291030 IC50 > 1000.0 nM -
CHEMBL289517 IC50 > 1000.0 nM -