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Assay Detail

CHEMBL615481

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

Binding
Tested for its binding affinity towards 5-hydroxytryptamine 1 receptor in rat cortical membrane homogenates using radioligand ([3H]5-HT) binding assay.
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Serotonin 1 (5-HT1) receptor (CHEMBL2095159)
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 11 7.54 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL288111 1 8.52
CHEMBL291097 1 8.30
CHEMBL36379 1 8.10
CHEMBL39947 1 7.82
CHEMBL285723 1 7.70
CHEMBL39604 1 7.70
CHEMBL285284 1 7.40
CHEMBL40047 1 7.10
CHEMBL449081 AGROCLAVINE 1 6.85
CHEMBL38058 1 6.80
CHEMBL291030 1 6.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL288111 IC50 = 3.0 nM 8.52
CHEMBL291097 IC50 = 5.0 nM 8.30
CHEMBL36379 IC50 = 8.0 nM 8.10
CHEMBL39947 IC50 = 15.0 nM 7.82
CHEMBL285723 IC50 = 20.0 nM 7.70
CHEMBL39604 IC50 = 20.0 nM 7.70
CHEMBL285284 IC50 = 40.0 nM 7.40
CHEMBL40047 IC50 = 80.0 nM 7.10
CHEMBL449081 AGROCLAVINE IC50 = 140.0 nM 6.85
CHEMBL38058 IC50 = 160.0 nM 6.80
CHEMBL291030 IC50 = 240.0 nM 6.62